Search Result
Results for "
Oral
" in MedChemExpress (MCE) Product Catalog:
9757
Inhibitors & Agonists
68
Biochemical Assay Reagents
693
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-14401
-
|
CLTX-305
|
CaSR
|
Others
|
|
Encaleret (CLTX-305) is an orally active CaSR antagonist .
|
-
-
- HY-147136
-
|
|
YAP
|
Cancer
|
|
MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration .
|
-
-
- HY-W023144
-
-
-
- HY-12422B
-
|
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CDK
|
Cancer
|
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(2S,3R)-Voruciclib hydrochloride is the enantiomer of Voruciclib hydrochloride. Voruciclib is an orally active CDK inhibitor.
|
-
-
- HY-162877
-
-
-
- HY-111755
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Oral antiplatelet agent 1 is a potent P2Y12 receptor antagonist. Oral antiplatelet agent 1 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. Oral antiplatelet agent 1 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. Oral antiplatelet agent 1 can be used to research thromboembolic disorders .
|
-
-
- HY-127028
-
|
M-7204
|
Parasite
|
Infection
|
|
Tripynadine is an anti-malarial compound with oral activity .
|
-
-
- HY-125441
-
-
-
- HY-125694
-
|
|
Fungal
|
Infection
|
|
MFB-1041 is an orally active antifungal agent, but exhibits poor oral absorption. MFB-1041 induces the binding of drug to serum albumin .
|
-
-
- HY-123452
-
-
-
- HY-19596
-
-
-
- HY-120730
-
-
-
- HY-124208A
-
-
-
- HY-124208
-
-
-
- HY-W764737
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
Methylboronic acid pinacol ester is an orally administered compound that inhibits the activity of peptidases and imidazole derivatives. Methylboronic acid pinacol ester is used as a medicinal preparation for cancer .
|
-
-
- HY-N7718
-
-
-
- HY-105216
-
-
-
- HY-129661
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
AH 7959 is an orally active N-substituted cyclohexyl methyl benzamide compound that has analgesic effects, the oral and subcutaneous ED50 of AH 7959 in mice is greater than 100 mg/kg .
|
-
-
- HY-141711
-
|
|
mAChR
|
Neurological Disease
|
|
VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4 .
|
-
-
- HY-119844A
-
-
-
- HY-131433
-
|
|
Parasite
|
Infection
|
|
Teroxalene hydrochloride is an orally active schistosomiasis agent .
|
-
-
- HY-119844
-
-
-
- HY-123631
-
-
-
- HY-119169
-
|
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Microtubule/Tubulin
|
Cancer
|
|
Tubulozole is an orally active synthetic microtubule inhibitor. Tubulozole can be used for the research of tumor .
|
-
-
- HY-A0232
-
|
Medomin
|
Drug Derivative
|
Neurological Disease
|
|
Heptabarbital (Medomin) is an oral activity Barbituric acid derivative. Heptabarbital has the potential for the research of insomnia .
|
-
-
- HY-B0224
-
-
-
- HY-B0224A
-
-
-
- HY-164138
-
|
|
17β-HSD
|
Cancer
|
|
17β-HSD5 inhibitor 3 (Compound 31) is an orally active inhibitor for 17β-HSD5 with an IC50 of 69 nM .
|
-
-
- HY-76511
-
-
-
- HY-107787
-
-
-
- HY-124419
-
|
|
mGluR
|
Neurological Disease
|
|
RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM .
|
-
-
- HY-18966
-
-
-
- HY-120703
-
|
|
Androgen Receptor
|
Endocrinology
|
|
RU 58642 is an orally active non-steroidal antiandrogen, which displays a strong and selective affinity for androgen receptor .
|
-
-
- HY-164648
-
-
-
- HY-132824
-
-
-
- HY-106499
-
-
-
- HY-136842
-
-
-
- HY-77591
-
-
-
- HY-124225
-
-
-
- HY-15531
-
|
ABT-199; GDC-0199; RG7601
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy .
|
-
-
- HY-105440
-
-
-
- HY-13723A
-
|
SDZ-ASM 981 hydrate
|
Phosphatase
|
Inflammation/Immunology
|
|
Pimecrolimus hydrate (SDZ-ASM 981 hydrate) is a potent, nonsteroid and orally active calcineurin inhibitor. Pimecrolimus hydrate shows anti-inflammatory activity. Pimecrolimus hydrate has the potential for the research of atopic dermatitis and oral erosive lichen planus .
|
-
-
- HY-106141
-
|
UR 9825
|
Fungal
|
Infection
|
|
Albaconazole (UR 9825) is a broad-spectrum triazole and oral activity antifungal agent .
|
-
-
- HY-W173220
-
-
-
- HY-137442
-
|
EOS-850
|
Adenosine Receptor
|
Cancer
|
|
Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity .
|
-
-
- HY-16259
-
|
Ricainide hydrochloride; LY 135837
|
Sodium Channel
|
Cardiovascular Disease
|
|
Indecainide hydrochloride is a potent and orally active class I local anesthetic antiarrhythmic agent. Indecainide hydrochloride has Na +-channel-blocking activity .
|
-
-
- HY-106571
-
|
Ro 19-5248; T-2588
|
Bacterial
Antibiotic
|
Infection
|
|
Cefteram pivoxil (Ro 19-5248), an orally active cephalosporin antibiotic, is used for bacterial infections .
|
-
-
- HY-117891
-
-
-
- HY-147041A
-
|
(2S)-GB1211
|
Galectin
|
Cancer
|
|
(2S)-Selvigaltin is the S-enantiomer of Selvigaltin (HY-147041). Selvigaltin is an orally active galectin-3 (Gal-3) inhibitor .
|
-
-
- HY-106067
-
|
UK 37248 free base
|
Prostaglandin Receptor
|
|
|
Dazoxiben is a potent and orally active thromboxane synthetase inhibitor. Dazoxiben has the potential for the research of Raynaud's syndrome .
|
-
- HY-107647A
-
-
- HY-155652
-
|
|
BCRP
|
Cancer
|
|
ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC50 of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice .
|
-
- HY-59059
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
5-(2-Aminopropyl)indole is an orally active psychoactive substance, that shows inhibitory activity against monoamine oxidase (MAO) and long-lasting stimulatory properties .
|
-
- HY-168047
-
|
|
Virus Protease
|
Infection
|
EBOV-IN-10 is an orally active Ebola virus (EBOV) inhibitor with an EC50 value of 0.19 μM .
|
-
- HY-114929
-
-
- HY-105332
-
|
|
CRFR
|
Neurological Disease
|
|
CRA1000 is an orally active, selective and competitive CRF1 receptor antagonist with anxiolytic- and antidepressant-like properties .
|
-
- HY-10913
-
-
- HY-10913A
-
|
GAP-134 Hydrochloride; ZP 1609 Hydrochloride
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Danegaptide Hydrochloride (GAP-134 Hydrochloride) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect .
|
-
- HY-15383
-
|
|
Others
|
Others
|
|
Glyparamide is an orally active chlorophenyl-containing sulfonylurea. Glyparamide shows hypoglycemic activity and rarely causes hepatic injury .
|
-
- HY-154436
-
-
- HY-120486
-
-
- HY-139346
-
-
- HY-100411
-
|
|
LRRK2
|
Neurological Disease
|
|
MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease .
|
-
- HY-107533
-
|
|
GnRH Receptor
|
Endocrinology
|
|
T-98475 (Compound 26d) is a potent, orally active, non-peptide luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.2 nM .
|
-
- HY-76511S
-
|
MK-679-d6; L 668019-d6
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
|
-
- HY-W018475
-
|
MK 462 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Rizatriptan (MK 462 free base) is an orally active, potent and selective 5-HT1D receptor agonist. Rizatriptan is promising for research of migraine .
|
-
- HY-106769C
-
|
GR50360 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Fluparoxan hydrochloride is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan hydrochloride is an anti-depressant agent .
|
-
- HY-139566
-
|
3-Nitroxypropanol; 3-NOP
|
Others
|
Others
|
|
Abrucomstat (3-Nitroxypropanol) is an orally active methyl coenzyme M reductase inhibitor. Abrucomstat decreases ruminal methanogenesis .
|
-
- HY-16735
-
|
BCX4161
|
Kallikrein
|
Others
|
|
Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research .
|
-
- HY-106769
-
-
- HY-110274
-
-
- HY-162911
-
|
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Phosphodiesterase (PDE)
|
Cancer
|
|
Enpp-1-IN-22 is an orally bioavailable prodrug of the potent ENPP1 inhibitor paraformaldehyde with antitumor activity .
|
-
- HY-B1343
-
-
- HY-B1343A
-
-
- HY-145704
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria .
|
-
- HY-B1316
-
-
- HY-155299
-
-
- HY-106538
-
-
- HY-W011651
-
-
- HY-15531R
-
|
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
Venetoclax (Standard) is the analytical standard of Venetoclax. This product is intended for research and analytical applications. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy .
|
-
- HY-132894
-
|
|
Influenza Virus
|
Infection
|
|
Pixavir marboxilo is an orally active cap-dependent endonuclease inhibitor with high potency. Pixavir marboxilo can be used for the research of influenza .
|
-
- HY-124560
-
|
|
Others
|
Metabolic Disease
|
|
Lifibrol is a potent and oral activity hypolipidemic agent. Lifibrol decreases the plasma total cholesterol. Lifibrol has the potential for the research of hypercholesterolemia .
|
-
- HY-107072A
-
-
- HY-161106
-
|
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GPR84
|
Inflammation/Immunology
Cancer
|
|
OX04528 (compound 68) is a potent, G-protein biased, and orally active GPR84 agonist. OX04528 no cytotoxicity. OX04528 inhibits cAMP production with an EC50 value of 0.00598 nM .
|
-
- HY-118635
-
-
- HY-112736
-
-
- HY-A0165
-
-
- HY-100704A
-
-
- HY-126038
-
-
- HY-101566S
-
|
BAY 1895344-d3
|
ATM/ATR
|
Cancer
|
|
Elimusertib-d3 (BAY 1895344-d3) is the deuterium labeled Elimusertib (BAY 1895344). Elimusertib is a potent, orally active and selective ATR inhibitor and has anti-tumor activity .
|
-
- HY-170362
-
|
|
Cyclic GMP-AMP Synthase
|
Inflammation/Immunology
|
|
cGAS-IN-4 (Compound 36) is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) with IC50 of 32 nM and 5.8 nM for h-cGAS and m-cGAS. cGAS-IN-4 inhibits the cGAMP in THP-1 cell with an IC50 of 60 nM, which improves the cellular potency. cGAS-IN-4 exhibits anti-inflammatory efficacy in Concanavalin A (HY-P2149)-induced acute liver injury in mouse models .
orally active, THP-1, C57Bl/6 mouse, orally active
|
-
- HY-W017758
-
-
- HY-101245
-
|
SUN-1165; Pilzicainide(hydrochloride)
|
Sodium Channel
|
Cardiovascular Disease
|
|
Pilsicainide hydrochloride (SUN-1165) is an orally active sodium channel blocker and potent class Ic antiarrhythmic agent .
|
-
- HY-N12595
-
|
|
Others
|
Others
|
|
22,23-dihydroergosterol is an orally active natural product that can be isolated from Flammulina velutipes .
|
-
- HY-W010593
-
|
|
Drug Metabolite
|
Cancer
|
|
Ethylenethiourea is a degradation product of the ethylenebisthiocarbamate group of fungicides. Ethylenethiourea is tumorigenic and teratogenic. Ethylenethiourea is orally active .
|
-
- HY-107318
-
-
- HY-14560
-
-
- HY-131914A
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain .
|
-
- HY-101234
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
ICI 162846 is an orally active antagonist of H2 receptor. ICI 162846 inhibits acid production accompanied by an increase in the secretion of histamine in chronic duodenal ulcer (CDU) models. ICI 162846 is effective in preventing CDU .
|
-
- HY-10162
-
|
AZD2281; KU0059436
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator .
|
-
- HY-170428
-
|
|
Molecular Glues
Ras
|
Cancer
|
|
IPS-06061 is an orally active molecule glue, that forms a ternary complex of CRBN-KRASG12D-IPS06061, and degrades KRAS G12D with a DC50 <500 nM .
|
-
- HY-151141
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-17 (Compound 12B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.79 μM. α-Glucosidase-IN-17 shows antidiabetic activity .
|
-
- HY-120192
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP 62349 is a selective and orally active GABAB receptor antagonist that improves cognitive performance in multiple learning paradigms .
|
-
- HY-148684
-
|
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 10 is an orally active, potent AMPK activator with EC150 of 44.3 nM by cell-ELISA. AMPK activator 10 increases the phosphorylation levels of ACC. AMPK activator 10 exhibits a glucose lowering effect .
|
-
- HY-153113
-
|
DJT1116PG
|
SGLT
|
Endocrinology
|
|
Rongliflozin (DJT1116PG) is a selective and orally active inhibitor of sodium-glucose co-transporter-2 (SGLT-2). Rongliflozin can be used for the research of type 2 diabetes mellitus (T2DM) .
|
-
- HY-163300
-
-
- HY-120634
-
|
|
HCV
|
Infection
|
|
BMS-929075 is a potent and orally active HCV NS5B replicase palm site allosteric inhibitor. BMS-929075 shows high oral bioavailability. BMS-929075 shows cytotoxicity .
|
-
- HY-131705
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research .
|
-
- HY-77591R
-
-
- HY-163082
-
|
|
Galectin
|
Cancer
|
|
GB1490 is an orally active galectin inhibitor with Kd values of 0.4 μM and 2.7 μM for galectin-1 and galectin-3, respectively .
|
-
- HY-A0165R
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Tofisopam (Standard) is the analytical standard of Tofisopam. This product is intended for research and analytical applications. Tofisopam, a 2,3-benzodiazepine compound, is an orally active anxiolytic agent .
|
-
- HY-10320G
-
|
BIRB 796 (GMP)
|
p38 MAPK
|
Cancer
|
|
Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity .
|
-
- HY-106506
-
|
BW A515U
|
HSV
Apoptosis
Antibiotic
Bacterial
|
Infection
|
|
Desciclovir is a potent and orally active proagent of the antiherpetic agent Acyclovir (ACV). Desciclovir is converted to acyclovir in vivo by xanthine oxidase .
|
-
- HY-106325
-
-
- HY-124073
-
|
|
TRP Channel
|
Metabolic Disease
|
|
Dihydrocapsiate, as a compound of capsinoid family, is an orally active TRPV1 agonist. Dihydrocapsiate can be used for the research of metabolism disease .
|
-
- HY-B1682
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Loracarbef, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class .
|
-
- HY-114638A
-
|
BRL 40015 hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diproteverine hydrochloride is an oral activity calcium channel blocker. Diproteverine hydrochloride embryonic toxicity. Diproteverine hydrochloride also shows antianginal properties .
|
-
- HY-B1682A
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Loracarbef hydrate, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class .
|
-
- HY-137463
-
-
- HY-163669
-
-
- HY-135655A
-
|
SPR720; pVXc-486
|
Bacterial
|
Infection
|
|
Fobrepodacin (SPR720) is an orally active and potent phosphate proagent of SPR719 (VXc-486; HY-12930). Fobrepodacin has potent bactericidal activities in vivo .
|
-
- HY-169953
-
|
|
Pyk2
|
Metabolic Disease
|
|
BT-Amide is the orally active inhibitor for Pyk2 kinase with IC50 of 44.69 nM. BT-Amide prevents glucocorticoid-induced bone loss, exhibits bone protective activity in C57BL/6 mouse .
|
-
- HY-123571
-
-
- HY-117507
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity . U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM) .
|
-
- HY-142618
-
-
- HY-W013378
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Carbamazepine 10,11-epoxide is an orally active metabolite of Carbamazepine (HY-B0246). Carbamazepine has anticonvulsant effect. Carbamazepine can be used for the research of seizures .
|
-
- HY-129914
-
|
KY-109 free base
|
Bacterial
|
Infection
|
|
Cefcanel daloxate (KY-109 (free base)) is an orally active cephalosporin prodrug against Gram-positive bacteria and Haemophilus influenzae. Cefcanel daloxate is promising for research of uremia .
|
-
- HY-129708
-
|
|
Drug Metabolite
|
Neurological Disease
|
|
LU 2443 is an orally active antiepileptic mesoionic. LU 2443 is extensively absorbed, in the maximum 18% are eliminated unabsorbed in rats. The half-time of the activity in plasma is 13.17 h .
|
-
- HY-12177S
-
-
- HY-138453
-
|
LPA1 receptor antagonist 2
|
LPL Receptor
|
Inflammation/Immunology
|
|
ACT-1016-0707 (Compound 49) is an orally active and selective LPA1 receptor antagonist. ACT-1016-0707 can be used for the research of fibrotic diseases .
|
-
- HY-137448
-
|
SHR3680
|
Androgen Receptor
|
Cancer
|
|
Rezvilutamide (SHR3680) is an orally active androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer .
|
-
- HY-132815
-
|
MIV-818
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Fostroxacitabine bralpamide (MIV-818) is an orally active Troxacitabine-based nucleotide proagent. Fostroxacitabine bralpamide has anticancer effects .
|
-
- HY-118234
-
|
|
Bacterial
|
Others
|
|
(Rac)-PD 138312 is the racemate of PD 138312. PD 138312 is a potent and orally active antibacterial agent against Gram-positive bacteria .
|
-
- HY-108685
-
|
Alendronic acid monosodium salt
|
Others
|
Metabolic Disease
Cancer
|
|
Alendronate sodium is an orally active nitrogen-containing bisphosphonate. Alendronate sodium potently inhibits bone resorption. Alendronate sodium is used for the research of postmenopausal osteoporosis .
|
-
- HY-14486
-
|
PRT060128 potassium
|
P2Y Receptor
|
Inflammation/Immunology
|
|
Elinogrel (PRT060128) potassium is a reversible, competitive and orally active P2Y12 antagonist. Elinogrel potassium inhibits thrombosis .
|
-
- HY-159962
-
|
|
Glutaminase
|
Metabolic Disease
|
|
TGase2-IN-1 (Compound 22) is an orally active inhibitor for TGase2 with an IC50 of 1.12 μM. TGase2-IN-1 inhibits TGase2 in human retinal microvascular endothelial cells with an IC50 of 0.07 μM. TGase2-IN-1 exhibits 74.6% oral bioavailability. TGase2-IN-1 inhibits retinal vascular leakage in mouse Streptozotocin (HY-13753)-induced diabetic model .
|
-
- HY-120662
-
|
|
mGluR
|
Neurological Disease
|
|
GSK1331268 is a selective, orally active agonist for mGluR2 with a pEC50 of 6.9. GSK1331268 exhibits good blood-brain barrier penetration. GSK1331268 regulates glutamate signaling, and can be used in research of neurodegenerative and neuropsychiatric diseases .
|
-
- HY-14383
-
-
- HY-17597
-
|
|
Parasite
|
Infection
|
|
Febantel is an oral dewormer used to treat gastrointestinal nematodes in sheep, as well as roundworm and tapeworm infections in poultry and livestock, and it also inhibits the embryonic development of mouse hairworms and whipworm eggs .
|
-
- HY-133013
-
|
|
CFTR
|
Inflammation/Immunology
|
|
GLPG-3221 is a potent, orally active corrector of CFTR (cystic fibrosis transmembrane conductance regulator), with an EC50 of 105 nM. GLPG-3221 can be uesd for the treatment of cystic fibrosis .
|
-
- HY-147993
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity .
|
-
- HY-137979
-
|
|
UGT
|
Neurological Disease
|
|
Flunitrazolam is an orally active designer Benzodiazepine. Flunitrazolam is biologically toxic, class in psychoactive substances .
|
-
- HY-109099
-
|
INCB054828
|
FGFR
|
Cancer
|
|
Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma .
|
-
- HY-114638
-
|
BRL 40015
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diproteverine (BRL 40015) is an oral activity calcium channel blocker. Diproteverine embryonic toxicity. Diproteverine also shows antianginal properties .
|
-
- HY-B0467S
-
-
- HY-50856A
-
|
S-Ruxolitinib; S-INCB18424
|
JAK
|
Cancer
|
|
Ruxolitinib (S enantiomer) (S-Ruxolitinib) is the S-enantiomer of Ruxolitinib (HY-50856). Ruxolitinib (S enantiomer) is an orally active, potent JAK inhibitor .
|
-
- HY-144110
-
|
|
HCV
|
Infection
|
|
HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage .
|
-
- HY-106571R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Cefteram pivoxil (Standard) is the analytical standard of Cefteram pivoxil. This product is intended for research and analytical applications. Cefteram pivoxil (Ro 19-5248), an orally active cephalosporin antibiotic, is used for bacterial infections .
|
-
- HY-144393
-
|
|
BCRP
|
Cancer
|
|
P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel) .
|
-
- HY-171174
-
|
|
CDK
STAT
Wnt
|
Cancer
|
|
CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1 SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57% .
|
-
- HY-106816
-
-
- HY-B1800
-
-
- HY-14230
-
|
|
CCR
HIV
|
Infection
|
|
INCB9471 is a potent, selective and orally active CCR5 antagonist. INCB9471 shows anti-HIV-1 activity .
|
-
- HY-B0487
-
|
Pregneninolone; 17α-Ethynyltestosterone
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Ethisterone (Pregneninolone), a synthetic steroidal estrogen, is an orally active steroidal contraceptive agent. Ethisterone is reported for androgenic activity, used for the research of the gynecological disorders .
|
-
- HY-13236
-
-
- HY-148348
-
|
|
HBV
|
Infection
|
|
AB-836 is an orally active HBV capsid inhibitor. AB-836 inhibits viral replication by interacting with HBV core protein .
|
-
- HY-108504
-
|
V 102862
|
Sodium Channel
|
Neurological Disease
|
|
Co 102862 (V 102862) is a potent, broad-spectrum, state-dependent Na + channel blocker. Co 102862 is also an orally active anticonvulsant .
|
-
- HY-167894
-
-
- HY-106578
-
|
LM 208
|
5-HT Receptor
|
Neurological Disease
|
|
Quinupramine is an orally active antidepressant. Quinupramine can penetrate into the CNS and affect some of the processes of neurotransmission. The antidepressant activity of quinupramine is associated with the central serotonin system, but not with the β-adrenergic system[1][2].
|
-
- HY-19947
-
|
Glucagon receptor antagonists-4
|
GCGR
|
Metabolic Disease
|
|
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM) .
|
-
- HY-145483
-
|
KYM-001; PROTAC IRAK4 degrader-7
|
PROTACs
IRAK
Apoptosis
|
Cancer
|
|
KT-474 (KYM-001) is an orally active PROTAC IRAK4 degrader with antitumor activities . KT-474 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17359
-
|
ICL 670
|
Bacterial
Ferroptosis
|
Cancer
|
|
Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload .
|
-
- HY-W013331
-
|
|
Others
|
Inflammation/Immunology
|
|
Deoxy artemisinin, a orally bioavailable compound separated from Artemisinin annua L., shows anti-inflammatory and antiulcer activities .
|
-
- HY-W392925
-
|
d-Aminoglutethimide
|
Cytochrome P450
|
Cancer
|
|
(R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. (R)-(+)-Aminoglutethimide has the potential for the research of breast cancer .
|
-
- HY-A0252
-
-
- HY-101820A
-
|
|
EGFR
|
Cancer
|
|
Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
|
-
- HY-B1363
-
|
Bendrofluazide
|
Others
|
Cardiovascular Disease
|
|
Bendroflumethiazide is an orally active diuretic. Bendroflumethiazide is an antihypertensive agent. Bendroflumethiazide has the potential for the research of arterial hypertensive disease .
|
-
- HY-101820
-
|
|
EGFR
|
Cancer
|
|
Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
|
-
- HY-132196
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities .
|
-
- HY-A0175
-
|
Butriptylene
|
5-HT Receptor
|
Neurological Disease
|
|
Butriptyline (Butriptylene) is an orally active tricyclic antidepressant that slightly enhances central 5-HT effects. Butriptyline does not inhibit brain norepinephrine uptake .
|
-
- HY-129695
-
|
|
Renin
|
Cardiovascular Disease
|
|
PD 132002 is an orally active, potent renin inhibitor. PD 132002 weakly inhibits pepsin. PD 132002 produces substantial reductions in blood pressure .
|
-
- HY-129347
-
|
T-2636E
|
Antibiotic
Bacterial
|
Infection
|
|
Lankacyclinol A is an orally active antibiotic isolated from Streptomyces rochei. Lankacyclinol A has broad-spectrum antimicrobial activity against both Gram-positive and Gram-negative bacteria. Lankacyclinol A exhibits low toxicity in mice .
|
-
- HY-121080
-
|
|
TRP Channel
|
Neurological Disease
|
|
AMG8163 is an orally active antagonist for TRPV1. AMG8163 inhibits Capsaicin (HY-10448)-induced flinch in rats models, and exhibits anti-hyperalgesia effects in multiple pain models .
|
-
- HY-116746
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Clopimozide is an orally active antischizophrenic agent that inhibits [ 3H]nitrendipine binding with IC50 value of 17 nM. Clopimozide is a calcium channel antagonist. Clopimozide can be used for the research of negative and positive schizophrenic symptoms .
|
-
- HY-12104
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
PF-514273 is an orally active, selective antagonist for cannabinoid-1 receptor (CB1) with IC50 of 1 nM. PF-514273 reduces the food uptake in mice, and can be used for obesity research .
|
-
- HY-159642
-
|
|
FGFR
|
Cancer
|
|
TYRA-300 is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM in Ba/F3. TYRA-300 exhibits antitumor efficacy against urothelial cancers and solid tumors .
|
-
- HY-107730
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor .
|
-
- HY-161573A
-
|
|
YAP
|
Cancer
|
|
(7S)-BAY-593 is the S-enantiomer of BAY-593 (HY-161573). BAY-593 is an orally active GGTase-I inhibitor. BAY-593 can block YAP1/TAZ signaling in animals and has antitumor activity .
|
-
- HY-12586
-
|
|
Thrombin
|
Others
|
|
AZD6564 is an orally active inhibitor for fibrinolysis through disruption of plasma kinase-fibrin interaction. AZD6564 dissolves human plasma clot with an IC50 of 0.44 μM. AZD6564 ameliorates hemorrhage in rats with EC50 of 1.62 μM, and exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-114766
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Pumafentrine is an orally active, potent dual PDE3/PDE4 inhibitor. Pumafentrine dose-dependently ameliorates the clinical score and colonic TNFα production in murine Dextran sulphate sodium (DSS; HY-116282C)-induced colitis in a preventive setting .
|
-
- HY-116437
-
|
|
EGFR
|
Cancer
|
|
Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects .
|
-
- HY-B1343R
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Pridinol (mesylate) (Standard) is the analytical standard of Pridinol (mesylate). This product is intended for research and analytical applications. Pridinol mesylate is an orally active and potent central anticholinergic agent, and acts as muscle relaxant .
|
-
- HY-120474
-
|
|
Drug Derivative
|
Neurological Disease
|
|
Ro 23-0364 is an oral active imidazobenzodiazepine agent with mixed benzodiazepine. Ro 23-0364 shows sedative and can be used for study of neurological disease .
|
-
- HY-109022
-
|
MK-8031; AGN-241689
|
CGRP Receptor
|
Neurological Disease
|
|
Atogepant (MK-8031) is an orally active and selective calcitonin gene–related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine .
|
-
- HY-17487
-
|
Y 0213; Y 9213
|
COX
|
Neurological Disease
Inflammation/Immunology
|
|
Miroprofen (Y 0213) is an orally active nonsteroidal anti-inflammatory analgesic (NSAID). Miroprofen exhibits anti-inflammatory, analgesic and anti-platelet activities .
|
-
- HY-153711
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPA1-IN-2 (compound 1) is a potent and orally active TRPA1 inhibitor with an IC50 value of 0.04 µM. TRPA1-IN-2 shows anti-inflammation activity .
|
-
- HY-169423
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 17 (Compound 250) is an orally active Werner Syndrome ATP dependent helicase enzyme (WRN) inhibitor, in particular inhibit WRN helicase domain activity. WRN inhibitor 17 is promising for research of cancers .
|
-
- HY-A0107
-
|
MK-801 maleate
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Tetracycline is a broad-spectrum antibiotic with oral activity. Tetracycline exhibits activity against a wide range of bacteria including gram-positive, gram-negative bacteria, chlamydiae, mycoplasmas and rickettsiae. Tetracycline can be used for the research of infections .
|
-
- HY-162892
-
|
|
Epigenetic Reader Domain
|
Cancer
|
BRD4-IN-9 is an orally active BRD4 inhibitor with an IC50 value of 9.4 nM. BRD4-IN-9 can suppress tumor growth in a mouse melanoma xenograft model .
|
-
- HY-151135
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-15 (Compound 14B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.34 μM. α-Glucosidase-IN-15 shows antidiabetic activity .
|
-
- HY-146075
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
β-Lactamase-IN-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor. β-Lactamase-IN-8 can be used for researching antibacteria .
|
-
- HY-161731
-
|
|
EGFR
|
Cancer
|
|
DS08701581 is an inhibitor of FER tyrosine kinase with IC50. DS08701581 has anti-tumor activity and oral activity .
|
-
- HY-113671
-
|
|
Calcium Channel
Acyltransferase
|
Others
|
|
Belfosdil is an orally active and highly specific calcium channel blocker that also inhibits the activity of acyl coenzyme A cholesterol acyltransferase .
|
-
- HY-10162R
-
|
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib (Standard) is the analytical standard of Olaparib. This product is intended for research and analytical applications. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator .
|
-
- HY-B1209
-
|
7-(β-Hydroxyethyl)theophylline
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Etofylline (7-(β-Hydroxyethyl) theophylline) is an oral bronchodilator with anti-inflammatory effects. Etofylline inhibits phosphodiesterase and prevents the degradation of cAMP (cyclic adenosine monophosphate), leading to smooth muscle relaxation, reducing inflammatory responses and improving respiratory function. Etofylline affects the development of zebrafish embryos .
|
-
- HY-B0996
-
|
NSC-17764
|
Bacterial
Fungal
|
Infection
Inflammation/Immunology
|
|
Hexetidine (NSC-17764) is an orally active antibacterial and antifungal agent with broad antibacterial and antifungal activity. Hexetidine combined with IPBC potentiates strong fungal growth inhibition properties. Hexetidine at concentrations greater than 0.1% can cause oral ulceration. Additionally, Hexetidine improves its plaque inhibiting activities combined with zinc and has been confirmed the effectiveness on purulent wound along with ultrasound. Hexetidine is a promising candidate for research in fungus-related diseases and soft tissue purulent-inflammatory
|
-
- HY-162853
-
|
|
Bacterial
|
Infection
|
|
Mtb-IN-8 (compound 5jb) is an orally active inhibitor of Mycobacterium tuberculosis (Mtb) with MIC values of 0.03 μg/mL for H37Rv and 0.125-0.06 μg/mL for MDR-Mtb, respectively .
|
-
- HY-B0714R
-
|
|
COX
|
Neurological Disease
|
|
Dexketoprofen (trometamol) (Standard) is the analytical standard of Dexketoprofen (trometamol). This product is intended for research and analytical applications. Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective COX inhibitor. Dexketoprofen trometamol has a pain-relieving effect .
|
-
- HY-W115798
-
|
Magnesium citrate tribasic nonahydrate, 99%
|
Biochemical Assay Reagents
|
Others
|
|
Trimagnesium dicitrate nonahydrate, 99% (Magnesium citrate tribasic nonahydrate, 99%) is an orally active magnesium salt of citric acid in the nonahydrate form. Trimagnesium dicitrate nonahydrate, 99% used as a stabilizer and anticaking agent in food supplements in solid and chewable forms .
|
-
- HY-168522
-
|
|
Integrin
|
Inflammation/Immunology
|
|
αvβ6-IN-2 (compound 20) is a potent and orally active αvβ6 integrin inhibitor with a pIC50 value of 7.8. αvβ6-IN-2 has the potential for the research of idiopathic pulmonary fibrosis .
|
-
- HY-109155
-
|
CRN00808
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine can be used in research on acromegaly and neuroendocrine tumors .
|
-
- HY-109155A
-
|
CRN00808 hydrochloride
|
Somatostatin Receptor
|
Neurological Disease
Endocrinology
|
|
Paltusotine (CRN00808) hydrochloride is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine hydrochloride has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine hydrochloride can be used in research on acromegaly and neuroendocrine tumors .
|
-
- HY-119245
-
|
BMS-986166
|
LPL Receptor
|
Inflammation/Immunology
|
|
Udifitimod (BMS-986166) is a potent, selective and orally active S1P1R modulator. Udifitimod has the potential for the research of autoimmune diseases .
|
-
- HY-W011651R
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Carbutamide (Standard) is the analytical standard of Carbutamide. This product is intended for research and analytical applications. Carbutamide (BZ-55) is an orally active and first-generation sulfonylurea with hypoglycemic activity .
|
-
- HY-153800
-
-
- HY-119270
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
PD 130908 is an orally active hypoxic cell radiosensitizer with potent radiosensitizing activity. PD 130908 can be utilized in cancer research .
|
-
- HY-122075
-
|
|
Others
|
Metabolic Disease
|
|
FR 78844 is a potent and orally active bone resorption inhibitor. FR 78844 has the potential for the research of diabetes associated osteopenia .
|
-
- HY-18345
-
-
- HY-B1481B
-
|
Isoetarine hydrochloride
|
Adrenergic Receptor
|
Infection
|
|
Isoetharine hydrochloride is selective, short-acting and orally active β-agonist which is widely used as a bronchodilator in the research of inhalation research .
|
-
- HY-B1656
-
-
- HY-103459
-
|
PD156707
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration .
|
-
- HY-118911
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC50: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors .
|
-
- HY-155787
-
|
|
CDK
|
Cancer
|
|
SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM) .
|
-
- HY-W099437
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Diethylene glycol monobutyl ether acetate is an orally available high molecular weight glycol ether solvent that can be used as a coalescing agent for polyvinyl acetate (latex) coatings, the acute oral LD in mice and rats is about 7 g/kg .
|
-
- HY-160532
-
|
|
Casein Kinase
|
Cancer
|
|
CK1α degrader-1 (Compound 82) is an orally active CK1α degrader with a DC50 of 0.105 μM. CK1α degrader-1 can be used for the research of cancer .
|
-
- HY-106115
-
|
RGH 2981; RT-3003
|
Others
|
Cardiovascular Disease
|
|
Vintoperol (RGH 2981; RT-3003) is a potent and orally active antithrombotic agent. Vintoperol interferes with platelet aggregation and has antithrombotic effects, protecting mice from retrograde and anterograde amnesia induced by traumatic brain injury .
|
-
- HY-162553
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
GNE7599 is a high-affinity and orally active von Hippel-Lindau (VHL) ligand with a Kd of 540 pM. GNE7599 can be connected to the ligand for protein by a linker to form PROTACs .
|
-
- HY-146223
-
|
|
Ras
|
Cancer
|
|
AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
- HY-163832
-
|
|
Farnesyl Transferase
|
Metabolic Disease
|
|
FPPS-IN-2 (compound 4a) is a potent and orally active HFPPS inhibitor with an IC50 value of 1.108 µM. FPPS-IN-2 has the potential for the research of osteoporosis .
|
-
- HY-W105835
-
|
Trimagnesium dicitrate
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
Magnesium citrate is a magnesium salt form that provides efficient penetration into brain and muscle tissue. Magnesium citrate increases pain threshold and reduces TLR4 concentration in the brain. Orally active .
|
-
- HY-139588
-
-
- HY-N10379
-
-
- HY-119605
-
|
|
GABA Receptor
|
Neurological Disease
|
|
DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects .
|
-
- HY-10267
-
|
PD-0348292
|
Factor Xa
|
Cardiovascular Disease
|
|
Eribaxaban (PD-0348292) is an orally active and selective FXa inhibitor with a Ki value of 0.32 nM. Eribaxaban reduces thrombus formation .
|
-
- HY-151568
-
|
|
Parasite
|
Infection
|
|
UCB7362 is an orally active and potent antimalarial plasmepsin X (PMX) inhibitor, with an IC50 of 7 nM. UCB7362 inhibits parasite growth .
|
-
- HY-B1429
-
-
- HY-167675
-
|
|
5-HT Receptor
|
Others
|
|
R-137696 is an orally active serotonin-1A (5-HT1A) receptor agonist which relaxes the proximal stomach. R-137696 can be utilized in research related to functional dyspepsia .
|
-
- HY-143200
-
-
- HY-122661
-
|
MPH
|
PARP
Apoptosis
|
Cancer
|
|
Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo .
|
-
- HY-N7557
-
|
|
Others
|
Cancer
|
|
(E)-2'-Hydroxy-3,4-dimethoxychalcone (compound 7) is a Chalcone derivative with orally active. (E)-2'-Hydroxy-3,4-dimethoxychalcone has anti-tumour activities .
|
-
- HY-103179
-
|
WAG-994; N6-Cyclohexy-2'-0-methyladenosine
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
SDZ-WAG994 (WAG-994) is a stable, long-acting, selective and orally active A1-adenosine receptor agonist with a KD of 23 nM. SDZ-WAG994 can be used for the research of atrial fibrillation .
|
-
- HY-114966
-
-
- HY-139585
-
|
LC350189
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Tigulixostat (LC350189) is an orally active, non-purine selective xanthine oxidase inhibitor. Tigulixostat lowers the production of uric acid. Tigulixostat can be used for gout and hyperuricemia study .
|
-
- HY-142687
-
|
|
SGK
|
Inflammation/Immunology
|
|
SGK1-IN-4 (compound 17a) is a highly selective, orally active SGK1 inhibitor. SGK1-IN-4 can be used for osteoarthritis research .
|
-
- HY-N11407
-
|
|
Antibiotic
Bacterial
Fungal
|
Infection
|
|
Bagougeramine B is an orally active nucleoside antibiotic with antimicrobial activity, which is found in Bacillus circulans. Bagougeramine B inhibits the growth of Gram-positive and Gram-negative bacteria and some fungi .
|
-
- HY-117858
-
-
- HY-121776
-
|
|
Drug Derivative
|
Cardiovascular Disease
|
|
Nicomol is an orally active hypolipidemic agent that can increase the high density lipoprotein cholesterol (HDL-C) level. Nicomol inhibits the rapid rise of plasma free fatty acids .
|
-
- HY-W010593R
-
|
|
Drug Metabolite
|
Cancer
|
|
Ethylenethiourea (Standard) is the analytical standard of Ethylenethiourea. This product is intended for research and analytical applications. Ethylenethiourea is a degradation product of the ethylenebisthiocarbamate group of fungicides. Ethylenethiourea is tumorigenic and teratogenic. Ethylenethiourea is orally active .
|
-
- HY-10852A
-
|
OZ 277 maleate; RBx 11160 maleate
|
Parasite
|
Infection
|
|
Arterolane (OZ 277) (maleate) is an orally active antimalarial. Arterolane exhibits potent activity against erythrocytic stages of P. falciparum and Plasmodium vivax. Arterolane (maleate) is promising for research of falciparum malaria .
|
-
- HY-116726
-
|
|
Glutathione S-transferase
|
Cancer
|
|
Crambene is an orally active cyanide compound isolated from cruciferous vegetables. Crambene has a cancer-preventive effect and induces significant upregulation of quinone reductase and glutathione S-transferase in vitro and in vivo .
|
-
- HY-100125A
-
|
SR1368 hydrochloride
|
COX
|
Inflammation/Immunology
|
|
Timegadine hydrochloride (SR1368 hydrochloride) is the hydrochloride salt form of Timegadine (HY-100125). Timegadine hydrochloride is an orally active inhibitor for COX and lipo-oxygenase, that inhibits COX in washed rabbit platelets and rat brain with IC50 of 5 nM and 20 μM, inhibits lipo-oxygenase in in horse and washed rabbit platelets with IC50 of 100 μM. Timegadine hydrochloride exhibits anti-arthritis activity .
|
-
- HY-170396
-
|
|
BCRP
|
Inflammation/Immunology
|
|
ABCG2-IN-4 (Compound K31) is an orally active inhibitor for ABCG2, which reduces the release of Protoporphyrin IX (PPIX) (HY-B1247) from erythrocytes into plasma, and prevents the reduces phototoxicity. ABCG2-IN-4 exhibits anti-inflammatory and antioxidant activity in mouse models .
|
-
- HY-109099R
-
|
|
FGFR
|
Cancer
|
|
Pemigatinib (Standard) is the analytical standard of Pemigatinib. This product is intended for research and analytical applications. Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma .
|
-
- HY-N12353
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Stevisalioside A (Compound 2) can be isolated from Stevia serrata roots. Stevisalioside A is an orally active antidiabetic agent. Stevisaliosides A inhibits PTP1B (IC50: 526.8 μM). Stevisalioside A reduces blood glucose levels and the postprandial peak in oral glucose and insulin tolerance tests in Streptozotocin (HY-13753) induced hyperglycemic mice .
|
-
- HY-A0287
-
|
Clomiphene
|
Isocitrate Dehydrogenase (IDH)
|
Endocrinology
|
|
Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation .
|
-
- HY-14568
-
|
|
GlyT
|
Neurological Disease
|
|
DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey .
|
-
- HY-A0287A
-
|
Clomiphene hydrochloride
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Clomifene hydrochloride is an orally active compound used for infertility. Clomifene hydrochloride is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation .
|
-
- HY-139398
-
TBI-223
1 Publications Verification
|
Antibiotic
Bacterial
|
Infection
|
|
TBI-223 is an orally bioavailable oxazolidinone antibiotic and an antimicrobial. TBI-223 shows activity against Mycobacterium tuberculosis (Mtb) .
|
-
- HY-112318A
-
|
|
Cathepsin
|
Inflammation/Immunology
|
|
GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis .
|
-
- HY-157250
-
|
|
Apoptosis
|
Endocrinology
|
|
BHD is an effective, orally active and reversible contraceptive agent. BHD induces the apoptosis of spermatogenic cells rapidly and disruptes the blood-testis barrier effectively .
|
-
- HY-155457
-
|
|
Phosphodiesterase (PDE)
STING
|
Cancer
|
|
Enpp-1-IN-19 (compound 29f) is an orally active ENPP1 inhibitor that inhibits cGAMP hydrolysis by ENPP1 (IC50=68 nM). Enpp-1-IN-19 increases anti-PD-L1 responses and inhibits tumor growth in CT26 syngeneic models. Enpp-1-IN-19 also enhances STING-mediated type I interferon responses, induces immune memory, and prevents tumor recurrence .
|
-
- HY-B1390B
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Saccharin sodium hydrate is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium hydrate has bacteriostatic and microbiome-modulating properties .
|
-
- HY-B0925
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Oxacillin sodium salt is an orally active synthetic penicillin with good bactericidal activity against staphylococci and other gram-positive pathogens .
|
-
- HY-N0465
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Olaquindox, a quinoxalin derivative, is an orally active antibiotic. Olaquindox stimulates growth and decreases intestinal mucosal immunity of piglets .
|
-
- HY-B0925A
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Oxacillin is an orally active synthetic penicillin with good bactericidal activity against staphylococci and other gram-positive pathogens .
|
-
- HY-Y0272
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties .
|
-
- HY-B1390A
-
|
|
Bacterial
|
Infection
|
|
Saccharin sodium is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium has bacteriostatic and microbiome-modulating properties .
|
-
- HY-12174
-
|
A-72517
|
Renin
|
Cardiovascular Disease
|
|
Zankiren (A-72517) is an orally active inhibitor for renin. Zankiren exhibits renal vasodilator effect, through reduction of angiotensin II formation without affecting other vasodilator mechanisms .
|
-
- HY-144073
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM). HPK1-IN-21 also has orally active .
|
-
- HY-141482
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects .
|
-
- HY-141525
-
-
- HY-120494
-
|
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
sEH inhibitor-1 (compound TCPU ) is a potent and oral active inhibitor of sEH (soluble epoxide hydrolase) with IC50s of 0.4 and 5.3 nM in human and murine, respectively .
|
-
- HY-10756
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
BMS-740808 is a potent, selective and orally active factor Xa inhibitor with a Ki of 30 pM. BMS-740808 shows >1000-fold for factor Xa than other proteases .
|
-
- HY-12222
-
|
INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid
|
FXR
Autophagy
|
Others
|
|
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
|
-
- HY-105860
-
|
BGG 492
|
iGluR
|
Neurological Disease
|
|
Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research .
|
-
- HY-143216A
-
|
S-217622 fumarate
|
SARS-CoV
Virus Protease
|
Infection
|
|
Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM) .
|
-
- HY-32345
-
|
BXL-628; Ro-26-9228
|
VD/VDR
|
Inflammation/Immunology
Cancer
|
|
Elocalcitol (BXL-628) is a selective, orally active vitamin D receptor (VDR) agonist. Elocalcitol shows anti-inflammatory activity. Elocalcitol inhibits growth of prostate cancer cells .
|
-
- HY-143216
-
|
S-217622
|
SARS-CoV
Virus Protease
|
Infection
|
|
Ensitrelvir (S-217622) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM) .
|
-
- HY-42990
-
|
HSPC; Hydrogenated soybean phosphatidylcholine
|
Liposome
|
Metabolic Disease
|
|
Hydrogenated soya phosphatidylcholine (hydrogenated soybean phosphatidylcholine) is a natural product. Hydrogenated soya phosphatidylcholine can extend drug release in regard to drug loading and solubility for oral drug delivery of watersoluble drugs .
|
-
- HY-139573
-
|
FT-4202
|
Pyruvate Kinase
|
Cardiovascular Disease
|
|
Etavopivat is a potent, selective, and orally active erythrocyte pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects that can be used in studies of sickle cell disease and other haemoglobinopathies .
|
-
- HY-106554A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Trimazosin hydrochloride hydrate is an orally active, quinazoline derivative which is structurally related to prazosin. Trimazosin shows hypotensive effect by selectively block α1-adrenergic receptor .
|
-
- HY-137892
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood .
|
-
- HY-124593
-
PTC299
2 Publications Verification
|
VEGFR
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
|
Cancer
|
|
PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies .
|
-
- HY-B0317
-
|
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
|
-
- HY-B0317C
-
|
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer .
|
-
- HY-170777
-
|
|
Parasite
|
Infection
|
|
SLU-10906 (Compound 63) is an orally active and potent Cryptosporidium inhibitor. SLU-10906 is active against the parasite in a cell-based infection model (EC50= 0.19 μM) and non-cytotoxic. SLU-10906 is promising for research of cryptosporidiosis .
|
-
- HY-12383
-
-
- HY-143793
-
|
|
Lipocalin Family
|
Metabolic Disease
|
|
RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice .
|
-
- HY-159158
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-1/2-IN-8 (compound 11f) is an orally active and potent inhibitor of COX-1 and COX-2, with IC50 values of 2.14 and 0.58 µM, respectively. COX-1/2-IN-8 displays a higher significant anti-inflammatory activity than Celecoxib (HY-14398) .
|
-
- HY-B0265
-
-
- HY-149290
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
AMX12006 is a potent, selective and orally active EP4 antagonist with an IC50 value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity .
|
-
- HY-150721
-
-
- HY-19415
-
|
|
Phospholipase
|
Metabolic Disease
|
|
SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM .
|
-
- HY-13723
-
|
SDZ-ASM 981
|
Phosphatase
|
Inflammation/Immunology
|
|
Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrolimus shows anti-inflammatory activity .
|
-
- HY-15975
-
|
|
Parasite
|
Infection
|
|
GNF179 is an optimized 8,8-dimethyl imidazolopiperazine analog that exhibits antimalarial potency (IC50 of 4.8 nM against the multidrug resistant strain W2). GNF179 is orally active .
|
-
- HY-B0089
-
|
BAY g 5421
|
Glycosidase
|
Metabolic Disease
Cancer
|
|
Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
|
-
- HY-160700
-
|
|
Deubiquitinase
JNK
|
Cancer
|
|
TNG348 is an orally active ubiquitin-specific protease USP1 inhibitor that can be used in research on cancers with BRCA1/2 mutations or HRD+ (Homologous Recombination Deficiency positive) status .
|
-
- HY-162249
-
|
|
Ras
|
Cancer
|
|
ASP6918 is a potent and orally active KRAS G12C inhibitor with an IC50 value of 0.028 µM. ASP6918 inhibits cell growth. ASP6918 shows antitumor activity .
|
-
- HY-147411
-
|
MK-8507
|
Reverse Transcriptase
HIV
|
Infection
|
|
Ulonivirine (MK-8507) is an orally active non-nucleoside reverse transcriptase inhibitor with high antiviral activity. Ulonivirine can be used for the research of HIV-1 infection .
|
-
- HY-124073R
-
|
|
TRP Channel
|
Metabolic Disease
|
|
Dihydrocapsiate (Standard) is the analytical standard of Dihydrocapsiate. This product is intended for research and analytical applications. Dihydrocapsiate, as a compound of capsinoid family, is an orally active TRPV1 agonist. Dihydrocapsiate can be used for the research of metabolism disease .
|
-
- HY-139875
-
|
|
CDK
|
Cancer
|
|
JH-XVI-178 is a highly efficient and selective CDK8/19 inhibitor, with IC50 values of 1 and 2 nM for CDK8 and CDK19, respectively. JH-XVI-178 has a low clearance rate and moderate oral pharmacokinetic properties .
|
-
- HY-149409
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-31 (compound R1) is an orally active, potent α-Glucosidase inhibitor with an IC50 value of 10.1 μM. α-Glucosidase-IN-31 significantly reduces the blood glucose level and has antidiabetic activity .
|
-
- HY-B0250A
-
|
BCH-189 salicylate
|
HIV
Reverse Transcriptase
HBV
|
Infection
Cancer
|
|
Lamivudine (BCH-189) salicylate is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine salicylate can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
|
-
- HY-156978
-
|
Wy-48252
|
Leukotriene Receptor
|
Others
|
|
Ritolukast (Wy-48252) is an orally active aerosol leukotriene (LTD4/E4) receptor antagonist. Ritolukast can be used to inhibit the bronchoconstriction caused by aerosol LTD4 in guinea pigs, with an ID50 of 0.5mg/kg .
|
-
- HY-19054
-
|
|
Parasite
|
Infection
|
|
CGP-20376, a 5-methoxyl-6-dithiocarbamic-S- (2-carboxy-ethyl) ester derivative of Benzothiazole (HY-W012634), is an orally active and potent antifilarial drug. CGP-20376 has anthelmintic activity .
|
-
- HY-B0911
-
-
- HY-119055
-
|
|
Leukotriene Receptor
|
Others
|
|
Sch 33303 is an orally active antiallergy agent that inhibits the release of the sulfidopeptide leukotrienes. Sch 33303 is promising for research of asthma .
|
-
- HY-148159
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Safrazine is an irreversible, non-specific and orally active monoamine oxidase (MAO) inhibitor. Safrazine can be used for the research of depression .
|
-
- HY-143439
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity .
|
-
- HY-138639
-
|
|
GPR52
|
Neurological Disease
|
|
PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior .
|
-
- HY-15651A
-
|
AZD9668 tosylate
|
Elastase
|
Inflammation/Immunology
|
|
Alvelestat (tosylate) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM .
|
-
- HY-122168
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively .
|
-
- HY-139784
-
|
(R)-2-Hydroxyoleic acid; (R)-2-OHOA; (R)-LAM561
|
Endogenous Metabolite
|
Cancer
|
|
Idroxioleic acid ((R)-2-Hydroxyoleic acid; (R)-2-OHOA), the R enantiomer of (Rac)-Idroxioleic acid, is an orally active fatty acid that modulates the lipid composition and structure of the membranes. Idroxioleic acid has antitumor activities .
|
-
- HY-125721
-
|
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Tetranactin is an orally active antibiotic that has insecticidal properties and can inhibit the growth of Gram-positive bacteria and plant pathogenic fungal in vitro. Tetranactin LD50 for intraperitoneal injection in mice is greater than 300 mg/kg, and the LD50 is greater than 15,000 mg/kg .
|
-
- HY-144878
-
|
|
c-Myc
|
Cancer
|
|
VPC-70619 is a potent, orally active N-Myc inhibitor. VPC-70619 blocks the N-Myc-Max heterocomplex from binding to DNA E-boxes and demonstrated strong inhibition activity against N-Myc-dependent cell lines as well as high bioavailability in both oral and intraperitoneal administration .
|
-
- HY-13705
-
-
- HY-157049
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Caprylocaproyl Macrogolglycerides is a lipoidic excipient/vehicle in an oral capsule formulation. Caprylocaproyl Macrogolglycerides can enhance the absorption of small molecule compounds .
|
-
- HY-B1711
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Norfenefrine is an orally active, endogenously found α-adrenergic agonist and can be used for the research of female stress incontinence .
|
-
- HY-141795
-
|
Co 134444
|
Others
|
Neurological Disease
|
|
Posovolone (Co 134444) is an orally active, neuroactive steroid. Posovolone has anticonvulsant and anxiolytic-like activity as well as ataxic effects .
|
-
- HY-19343
-
|
BMS-908662
|
Raf
|
Cancer
|
|
XL-281 (BMS-908662) is an orally active inhibitor for RAF kinase, with IC50s of 2.6, 4.5 and 6 nM, for CRAF, B-RAF, and B-RAFV600E, respectively. XL-281 exhibits antitumor activity .
|
-
- HY-B0317B
-
|
Amlodipine benzenesulfonate
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
|
-
- HY-116552
-
|
|
Parasite
|
Infection
|
|
KAR425 is a potent and orally active antimalarial agent. KAR425 shows antimalarial activity against the Chloroquine-sensitive (CQS) D6, the Chloroquine-resistant (CQR) Dd2, and 7G8 strains of Plasmodium falciparum, with IC50 values of 62 nM, 55 nM, and 60 nM, respectively .
|
-
- HY-161065
-
|
|
Bacterial
|
Infection
|
|
HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacterium tuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacterium tuberculosis infection .
|
-
- HY-10716
-
|
|
GlyT
|
Neurological Disease
|
|
PF-03463275 hydrochloride is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 hydrochloride has the potential for Schizophrenia research .
|
-
- HY-50898C
-
|
GW572016 tosylate; GW2016 tosylate
|
EGFR
Ferroptosis
Autophagy
|
Cancer
|
|
Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
- HY-131973
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
Metabolic Disease
|
|
PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research .
|
-
- HY-120608
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities .
|
-
- HY-121341
-
|
Ro 10-5970
|
Bacterial
|
Infection
|
|
Brodimoprim (Ro 10-5970), a trimethoprim analogue, is an orally active dihydrofolate reductase inhibitor. Brodimoprim is highly active against a broad spectrum of gram-negative and gram-positive bacteria .
|
-
- HY-15386
-
|
MD 780515
|
Monoamine Oxidase
|
Metabolic Disease
|
|
Cimoxatone (MD 780515) is a reversible, selectively and orally active type A monoamine oxidase (MAO-A) inhibitor. Cimoxatone enhances the anorectic action of Serotonin (HY-B1473A) .
|
-
- HY-B0338
-
|
1-Rimantadine
|
Influenza Virus
Autophagy
|
Infection
|
|
Rimantadine is an orally active inhibitor for M2 protein, that blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity .
|
-
- HY-B0698
-
|
Sch 39720
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
Ceftibuten (Sch39720), an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens .
|
-
- HY-108920
-
|
4-Cl-KYN; AV-101
|
iGluR
|
Neurological Disease
|
|
4-Chlorokynurenine is a prodrug of a NMDA receptor antagonist. 4-Chlorokynurenine has orally active and blood-brain permeability that can be used for the research of depression .
|
-
- HY-12713
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Lisuride is an orally active dopamine D2 receptors agonist. Lisuride, as an ergot derivative, can be used for the research of Parkinson's disease, migraine, and high prolactin levels .
|
-
- HY-122230
-
|
|
Integrin
|
Cardiovascular Disease
|
|
UR-3216 is a selective, and orally active platelet surface glycoprotein (GPIIb/IIIa) receptor antagonist. UR-3216 has the potential for cardiovascular diseases research .
|
-
- HY-132494S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Perazine-d8 is a deuterated form of Perazine. Perazine is a potent and orally active antidepressant agent. Perazine has the potential for the research of acute schizophrenics[1][2].
|
-
- HY-107611
-
-
- HY-B0698B
-
|
Sch 39720 monohydrate
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
Ceftibuten (Sch39720) monohydrate, an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens .
|
-
- HY-15796
-
GNE0877
2 Publications Verification
|
LRRK2
|
Neurological Disease
|
|
GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC50 of 3 nM and a Ki of 0.7 nM. GNE0877 can be used for the research of neuroscience .
|
-
- HY-118803
-
|
|
Factor Xa
|
Others
|
|
AS1468240 is an orally active inhibitor for anticoagulant factor Xa (fXa), that inhibits human fXa with IC50 of 8.7 nM. AS1468240 prolongs the coagulation time in mice .
|
-
- HY-10158
-
|
SKI-606
|
Src
Bcr-Abl
Autophagy
|
Cancer
|
|
Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively .
|
-
- HY-106499A
-
-
- HY-153392
-
|
|
Oxidative Phosphorylation
HDAC
|
Cardiovascular Disease
|
|
TYA-018 is an orally active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect heart function in mice. TYA-018 also enhances energetics in mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation .
|
-
- HY-119104
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action .
|
-
- HY-153700
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM .
|
-
- HY-170831
-
|
|
Histone Methyltransferase
GLP Receptor
|
Others
|
|
DS79932728 is an orally active inhibitor for G9a and GLP with IC50 of 12.6 nM and 75.7 nM. DS79932728 induces the production of γ-globin, thereby increasing the level of fetal hemoglobin (HbF). DS79932728 increases F-reticulocytes (F-rets) proportion and exhibits good oral absorption characteristics in cynomolgus monkey models .
|
-
- HY-167875
-
|
HRP 913
|
Dopamine Receptor
|
Neurological Disease
|
|
Neflumozide (HRP 913) is an orally active benzisoxazole derivative and a potent dopamine antagonist with antipsychotic activity. Neflumozide can be utilized in psychosis research .
|
-
- HY-162560
-
|
|
Others
|
Cancer
|
|
Antitumor agent-162 (compound 52a) is a potent and orally active antitumor agent. Antitumor agent-162 shows cytotoxicity .
|
-
- HY-17020
-
-
- HY-19687
-
|
CP73850
|
Aldose Reductase
|
Metabolic Disease
|
|
Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications .
|
-
- HY-130762
-
-
- HY-122133
-
|
|
Others
|
Metabolic Disease
|
|
CI 750 is a potent and orally active antidiarrheal agent. CI 750 increases the motor pattern of the gastrointestinal tract. CI 750 shows a constipating activity. CI 750 shows no analgesic, addiction liability, or anticholinergic pharmacological activity .
|
-
- HY-172371
-
|
|
Reactive Oxygen Species
|
Others
|
|
Hypoxystat increases the affinity of hemoglobin for oxygen and reduces the release of oxygen to tissues, thereby inducing the tissue hypoxia. Hypoxystat alleviates the mitochondrial disease Leigh syndrome in Ndufs4 knockout mouse models. Hypoxystat exhibits orally activity .
|
-
- HY-168498
-
|
|
Glutathione S-transferase
|
Inflammation/Immunology
|
|
GJG057 is a selective, orally active inhibitor for leukotriene C4 synthase (LTC4S) with an IC50 of 44 nM. GJG057 exhibits anti-inflammatory activity in mouse skin inflammation model and mouse asthma model .
|
-
- HY-131336
-
|
|
mGluR
|
Neurological Disease
|
|
MGS0274, an ester-based lipophilic proagent of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia .
|
-
- HY-B0487R
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Ethisterone (Standard) is the analytical standard of Ethisterone. This product is intended for research and analytical applications. Ethisterone (Pregneninolone), a synthetic steroidal estrogen, is an orally active steroidal contraceptive agent. Ethisterone is reported for androgenic activity, used for the research of the gynecological disorders .
|
-
- HY-108620
-
|
GR259653X
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys .
|
-
- HY-14950
-
|
JTT-705; RO4607381
|
CETP
|
Cardiovascular Disease
Cancer
|
|
Dalcetrapib (JTT-705) is an orally active cholesteryl ester transfer protein (CETP) inhibitor with IC50s of 204.6 nM and 6 μM against recombinant human (rh) CETP and human plasma CETP, respectively .
|
-
- HY-16346
-
-
- HY-B1062
-
|
S-(+)-Chlorpheniramine maleate salt
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Dexchlorpheniramine maleate is an orally taken anti-histamine that has anti-inflammatory, anti-irritant, anti-allergic, and skin barrier effects. Dexchlorpheniramine maleate inhibits myocardial contraction in rats. Dexchlorpheniramine maleate can be used in studies of allergic rhinitis .
|
-
- HY-B0255
-
-
- HY-17463
-
-
- HY-15352
-
|
DPC 083
|
Reverse Transcriptase
HIV
|
Infection
|
|
BMS 561390 (DPC 083) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains .
|
-
- HY-B0338A
-
|
|
Influenza Virus
Autophagy
|
Infection
|
|
Rimantadine hydrochloride (Flumadine hydrochloride) is an orally active inhibitor for M2 protein, that blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity .
|
-
- HY-163652
-
|
|
Others
|
Metabolic Disease
|
|
Glicetanile is an orally active hypoglycemic agent, that stimulates the release of insulin from pancreatic beta cells, and lowers the blood sugar. Glicetanile exhibits potential in ameliorating the type 2 diabetes .
|
-
- HY-157149
-
|
|
MAP4K
|
Cancer
|
|
DS21150768 is a potent, orally active HPK1 inhibitor. DS21150768 shows potent activity to enhance T-cell function. DS21150768 has anticancer effects .
|
-
- HY-137432A
-
|
BEY1107 trihydrochloride
|
CDK
|
Cancer
|
|
Avotaciclib (BEY1107) trihydrochloride is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib trihydrochloride can be used for the research of locally advanced or metastatic pancreatic cancer .
|
-
- HY-117668
-
|
|
Elastase
|
Infection
Inflammation/Immunology
|
|
MDL 101146 is an orally active neutrophil elastase inhibitor. MDL 101146 inhibits neutrophil elastase for human with a Ki value of 25 nM. MDL 101146 can be used for the research of arthritis .
|
-
- HY-137432
-
|
BEY1107
|
CDK
|
Cancer
|
|
Avotaciclib (BEY1107) is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib can be used for the research of locally advanced or metastatic pancreatic cancer .
|
-
- HY-W133967
-
-
- HY-160848
-
|
|
FLT3
|
Cancer
|
|
FLT3/ITD-IN-5 (Example 6) is an orally active FLT3 and FLT3-ITD inhibitor, with IC50 values of 0.088 and 0.348 nM, respectively. FLT3/ITD-IN-5 can be used for the research of cancer .
|
-
- HY-162655A
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
SLF80821178 hydrochloride is an orally active inhibitor for sphingosine-1-phosphate transporter (Spns2), that inhibits the sphingosine-1-phosphate (S1P) release in HeLa with an IC50 of 51 nM. SLF80821178 hydrochloride reduces the circulating lymphocyte without affecting plasma S1P levels in mice .
|
-
- HY-A0107R
-
|
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Tetracycline (Standard) is the analytical standard of Tetracycline. This product is intended for research and analytical applications. Tetracycline is a broad-spectrum antibiotic with oral activity. Tetracycline exhibits activity against a wide range of bacteria including gram-positive, gram-negative bacteria, chlamydiae, mycoplasmas and rickettsiae. Tetracycline can be used for the research of infections .
|
-
- HY-144303
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-4 (compound 19a) is an orally active and potent xanthine oxidase (XO) inhibitor, with an IC50 of 0.039 μM. Xanthine oxidase-IN-4 exhibits hypouricemic potency in potassium oxonate induced hyperuricemia rats. Xanthine oxidase-IN-4 can be used for hyperuricemia and gout research .
|
-
- HY-162110
-
-
- HY-B1651
-
|
Ferrous fumarate
|
Transferrin Receptor
|
Metabolic Disease
Cancer
|
|
Iron (II) fumarate is an orally effective active dietary supplement. Iron (II) fumarate can alleviate metabolic damage and damage to silkworms caused by cypermethrin (HY-123178). Iron (II) fumarate can be used for research on iron deficiency anemia .
|
-
- HY-134956B
-
|
|
YAP
|
Cancer
|
|
(R)-VT104 is the R-enantiomer of VT104. (R)-VT104 shows an IC50 value of 0.1-1 μΜ for firefly luciferase. VT104 is an orally active and pan-TEAD auto-palmitoylation inhibitor .
|
-
- HY-145887
-
|
|
Bcr-Abl
|
Neurological Disease
|
|
BCR-ABL1-IN-1 is a potent, orally active, and specific inhibitor of ABL kinase. BCR-ABL1-IN-1 has potential for elucidating the role of ABL kinases in the brain in non-clinical studies .
|
-
- HY-N12689
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-56 (compound 1) is an orally active, potent α‐glucosidase inhibitor with an IC50 value of 45.86 μM. α-Glucosidase-IN-56 has potent anti-glycation activities .
|
-
- HY-13672
-
-
- HY-148238
-
|
|
IRAK
|
Inflammation/Immunology
|
|
GNE-2256 (molecule 19) is an orally active IRAK4 (Interleukin 1 receptor associated kinase 4) inhibitor (IRAK4 Ki=1.4 nM; IL-6 IC50=190 nM) .
|
-
- HY-W017758R
-
|
|
Others
|
Others
|
|
1,3-Propanediol (Standard) is the analytical standard of 1,3-Propanediol. This product is intended for research and analytical applications. 1,3-Propanediol is produced in nature by the fermentation of glycerol in microorganism, which has orally active .
|
-
- HY-107013
-
|
|
MMP
|
Inflammation/Immunology
|
|
CP-544439 is a potent and orally active matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 0.75 nM .
|
-
- HY-17020A
-
-
- HY-119868
-
|
Butoxamin
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Butaxamine (Butoxamin) is a potent, selective and orally active β2-adrenoceptor antagonist. Butaxamine shows antiosteoporotic activity .
|
-
- HY-133937
-
|
|
Bacterial
HIV
|
Infection
|
|
Sulfametrole is an orally active and potent antibacterial. Sulfametrole can be used for infections research, such as HIV, severe pneumonia and UTIs (urinary tract infections) .
|
-
- HY-132294
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer .
|
-
- HY-159642G
-
|
|
FGFR
|
Cancer
|
|
TYRA-300 GMP is TYRA-300 (HY-159642) produced by using GMP guidelines. TYRA-300 GMP is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM. TYRA-300 GMP exhibits antitumor efficacy against urothelial cancers and solid tumors .
|
-
- HY-131723
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P450 3A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults .
|
-
- HY-13728B
-
|
(Rac)-ZD 9331; (Rac)-BGC9331
|
Thymidylate Synthase
|
Cancer
|
|
(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331)?is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor. (Rac)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-112102
-
|
SSHB
|
Akt
PI3K
Endogenous Metabolite
|
Metabolic Disease
|
|
(22S,23S)-Homobrassinolide is one of the most active brassinosteroids in inducing plant growth in various plant bioassay systems. (22S,23S)-Homobrassinolide shows Akt-dependent anabolic activity in rat skeletal muscle cells. Orally active .
|
-
- HY-N1500S1
-
|
|
TRP Channel
Endogenous Metabolite
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Pulegone-d8 is deuterated labeled Tetracycline (HY-A0107). Tetracycline is a broad-spectrum antibiotic with oral activity. Tetracycline exhibits activity against a wide range of bacteria including gram-positive, gram-negative bacteria, chlamydiae, mycoplasmas and rickettsiae. Tetracycline can be used for the research of infections .
|
-
- HY-B0592S
-
-
- HY-145598
-
|
HMPL-523
|
Syk
|
Cancer
|
|
Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC50 of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP) .
|
-
- HY-169127
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Seganserin is an orally active 5-HT receptor antagonist with a plasma half-life of 26.1 ± 12.9 (S.D.) h. Seganserin can be utilized in neurological research .
|
-
- HY-135655
-
|
SPR720 disodium; pVXc-486 disodium
|
Bacterial
|
Infection
|
|
Fobrepodacin (SPR720) disodium is an orally active and potent phosphate proagent of SPR719 (VXc-486; HY-12930). Fobrepodacin disodium has potent bactericidal activities in vivo .
|
-
- HY-136447
-
ASP4132
1 Publications Verification
|
AMPK
|
Cancer
|
|
ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models .
|
-
- HY-B0698A
-
|
Sch-39720 dihydrate
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
Ceftibuten (Sch-39720) dihydrate, an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens .
|
-
- HY-134661A
-
CVN424
1 Publications Verification
|
GPR6
|
Neurological Disease
|
|
CVN424 is an orally active and selective GPR6 inverse agonist with a Ki of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research .
|
-
- HY-149278
-
-
- HY-B1800R
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Tolonidine (Standard) is the analytical standard of Tolonidine. This product is intended for research and analytical applications. Tolonidine is a derivative of imidazoline. Tolonidine is orally active and has been shown to possess hypotensive and antihypertensive properties .
|
-
- HY-12717
-
|
|
Adrenergic Receptor
|
Endocrinology
Cancer
|
|
Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction .
|
-
- HY-50761
-
-
- HY-168087
-
|
|
Integrin
|
Cardiovascular Disease
|
|
GSK3335103 is an orally active, non-peptide αvβ6 integrin inhibitor (pIC50=8). GSK3335103 can be used in the study of pulmonary fibrosis .
|
-
- HY-139399
-
|
JNJ-67856633
|
MALT1
|
Cancer
|
|
Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis .
|
-
- HY-148617
-
-
- HY-157929
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
Cancer
|
|
Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs .
|
-
- HY-155731
-
|
|
Influenza Virus
|
Infection
|
|
Antiviral agent 35 (compound 4d) is an orally active and potent influenza virus inhibitor, acting function in the early stage of virus replication. Antiviral agent 35 inhibits ROS accumulation, autophagy and apoptosis induced by influenza virus, and also inhibits inflammatory response mediated by RIG-1 pathway in mouse model with pulmonary infection. Antiviral agent 35 shows little cytotoxicity with CC50 >800 μM in MDCK cells, and anti-H1N1 (A/Weiss/43) activity with EC50 of 2.28 μM .
|
-
- HY-16747
-
|
SHP625 chloride; LUM001 chloride; Lopixibat chloride
|
Apical Sodium-Dependent Bile Acid Transporter
|
Metabolic Disease
|
|
Maralixibat (SHP625) chloride is an orally active ileal bile acid transporter (IBAT) inhibitor. Maralixibat chloride can be used for the research of rare cholestatic liver diseases including Alagille syndrome (ALGS), progressive familial intrahepatic cholestasis (PFIC) and biliary atresia .
|
-
- HY-162235
-
|
|
Orexin Receptor (OX Receptor)
|
Cardiovascular Disease
|
|
CVN766 is an orally active inhibitor of orexin 1 receptor antagonist with blood-brain permeability with the IC50 values of 8 nM and >10 μM for OX1R and OX2R, respectively. CVN766 can be used for study schizophrenia .
|
-
- HY-105303
-
|
|
PARP
|
Cancer
|
|
CEP-9722, the proagent of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects .
|
-
- HY-130628
-
|
|
PAK
|
Cancer
|
|
PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions .
|
-
- HY-44132
-
|
RS 42358-197
|
5-HT Receptor
|
Neurological Disease
|
|
Dehydro Palonosetron (RS 42358-197) is a potent, seslective and orally active 5-HT3 receptor antagonist. Dehydro Palonosetron has no effect on the activities of 5-HT1 receptors, 5-HT2 receptors or 5-HT4 receptors .
|
-
- HY-151899
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [ 35S]GTPγS binding Emax .
|
-
- HY-W013378R
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Carbamazepine 10,11-epoxide (Standard) is the analytical standard of Carbamazepine 10,11-epoxide. This product is intended for research and analytical applications. Carbamazepine 10,11-epoxide is an orally active metabolite of Carbamazepine (HY-B0246). Carbamazepine has anticonvulsant effect. Carbamazepine can be used for the research of seizures .
|
-
- HY-12661A
-
|
|
PERK
Autophagy
|
Cancer
|
|
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy .
|
-
- HY-157585S
-
-
- HY-173024
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
|
-
- HY-173032
-
|
|
mGluR
|
Neurological Disease
|
|
VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .
|
-
- HY-170934
-
|
|
FGFR
|
Cancer
|
|
BW710 is an orally active fibroblast growth factor receptor 2 (FGFR2) inhibitor. BW710 inhibits the proliferation of BaF3-FGFR2 cells with an IC50 of 2.8 nM. BW710 abolishes FGFR2 enzymatic activity and is selective against other 75 tyrosine kinases including FGFR1, FGFR3, and FGFR4 at 1 μM. BW710 suppresses the FGFR2 signaling and selectively inhibits FGFR2-driven cancer cell proliferation. BW710 displays reasonable
pharmacokinetic properties with an oral bioavailability of 29 % in mice .
|
-
- HY-108287
-
|
|
Others
|
Endocrinology
|
|
Trithiozine is an orally active antisecretory and antiulcer agent. Trithiozine can be used for the research of peptic ulcer disease and hypersecretory disorders .
|
-
- HY-108308
-
-
- HY-10777
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
EMD 495235 is a potent and orally active coagulation factor Xa inhibitor with an IC50 of 5.5 nM and a Ki of 6.8 nM. EMD 495235 shows anticoagulant activities .
|
-
- HY-19415A
-
|
|
Phospholipase
|
Metabolic Disease
|
|
SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM .
|
-
- HY-109127
-
|
BCX7353
|
Kallikrein
|
Cancer
|
|
Berotralstat (BCX7353) is an orally active plasma kallikrein inhibitor. Berotralstat can reduce brain edema and is being studied for glioblastoma and hereditary angioedema .
|
-
- HY-19415B
-
|
|
Phospholipase
|
Metabolic Disease
|
|
SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM .
|
-
- HY-16158
-
|
Wy-4508; Aminocyclohexylpenicillin; Ciclacillin
|
Bacterial
Antibiotic
|
Infection
|
|
Cyclacillin (Wy-4508) is an orally active aminopenicillin antibiotic, shows antibacterial activity against a wide range of gram-positive and gram-negative pathogens .
|
-
- HY-122164
-
|
|
iGluR
|
Neurological Disease
|
|
LY-503430 is an orally active AMPA receptor positive allosteric modulator (PAM). LY-503430 can be used for the study of Parkinson's disease .
|
-
- HY-N7560
-
|
|
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
|
Safranal is an orally active main component of Saffron (Crocus sativus) and is responsible for the unique aroma of this spice. Safranal has neuroprotective and anti-inflammatory effects and has the potential for Parkinson’s disease research .
|
-
- HY-105124A
-
|
Ro 3-4787 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
|
-
- HY-105040C
-
|
LY2140023 hydrochloride
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research .
|
-
- HY-B1363R
-
|
|
NKCC
|
Cardiovascular Disease
|
|
Bendroflumethiazide (Standard) is the analytical standard of Bendroflumethiazide. This product is intended for research and analytical applications. Bendroflumethiazide is an orally active diuretic. Bendroflumethiazide is an antihypertensive agent. Bendroflumethiazide has the potential for the research of arterial hypertensive disease .
|
-
- HY-137898
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Avilamycin A is an oral active antibiotic. Avilamycin A is active against veterinary isolates of C. perfringens (MICs ≤ 0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml) .
|
-
- HY-153007
-
|
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity .
|
-
- HY-B0249
-
|
2',3'-Dideoxyinosine; ddI
|
HIV
Reverse Transcriptase
|
Infection
|
|
Didanosine (2',3'-Dideoxyinosine; ddI) is a a potent and orally active dideoxynucleoside analogue, and also is a potent nucleoside reverse transcriptase inhibitor. Didanosine shows antiretroviral activity for HIV .
|
-
- HY-139204
-
-
- HY-A0252R
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
Cancer
|
|
Bupranolol (Standard) is the analytical standard of Bupranolol. This product is intended for research and analytical applications. Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity .
|
-
- HY-153007A
-
|
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-5 hydrochloride is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 hydrochloride shows anti-malaria activity .
|
-
- HY-105094
-
|
NC 1300O3
|
Na+/K+ ATPase
|
Inflammation/Immunology
|
|
Leminoprazole (NC 1300O3) is an inhibitor for acid pump, H + K +-ATPase,. Leminoprazole stimulates the secretion and synthesis of gastric mucus, attenuates gastric ulcers. Leminoprazole is orally active .
|
-
- HY-137432D
-
|
BEY1107 sulfate
|
CDK
|
Cancer
|
|
Avotaciclib (BEY1107) sulfate is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib sulfate can be used for the research of locally advanced or metastatic pancreatic cancer .
|
-
- HY-15454
-
|
AT-406; Debio 1143; SM-406
|
IAP
Apoptosis
|
Cancer
|
|
Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.
|
-
- HY-148456
-
-
- HY-110132
-
-
- HY-124240
-
-
- HY-139590
-
|
BOS-172738; DS-5010
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
|
-
- HY-19656
-
|
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
HMR1426 is an orally active, potent gastric emptying inhibitor. HMR1426 reduces food intake and the rate of gastric emptying, decreases body weight and fat mass and shows an anorectic potential in rats. HMR1426 has the potential for obesity research .
|
-
- HY-103706
-
ROC-325
1 Publications Verification
|
Autophagy
Apoptosis
|
Cancer
|
|
ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis .
|
-
- HY-147066
-
|
|
DYRK
|
Cancer
|
|
Dyrk1A-IN-4 (compound 48) is a potent and orally active DYRK1A and DYRK2 inhibitor with IC50s of 2 nM and 6 nM, respectively. Dyrk1A-IN-4 has anticancer effects .
|
-
- HY-151591
-
|
|
Phosphatase
|
Metabolic Disease
|
|
SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase (LMW-PTP) inhibitor (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used in diabete research .
|
-
- HY-W020183
-
|
|
Fungal
Bacterial
|
Neurological Disease
|
|
γ-Terpinene, a monoterpene, is an orally active antioxidant compound which can scavenge radicals directly. γ-Terpinene has potent antinociception activity. γ-Terpinene exhibits antimicrobial efficacy against various bacteria and fungi .
|
-
- HY-141411A
-
|
(S)-MRI-1867
|
Cannabinoid Receptor
NO Synthase
|
Metabolic Disease
|
|
Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS antagonist. Zevaquenabant ameliorates obesity-induced chronic kidney disease (CKD) .
|
-
- HY-137144
-
|
ZB716
|
Estrogen Receptor/ERR
|
Cancer
|
|
Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells .
|
-
- HY-120160
-
|
CP-86325
|
PPAR
|
Neurological Disease
Metabolic Disease
|
|
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
|
-
- HY-B1355
-
|
|
Bacterial
COX
|
Infection
Inflammation/Immunology
|
|
Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis .
|
-
- HY-108432
-
|
|
CCR
|
Inflammation/Immunology
|
|
BMS-741672 is a selective and orally active CCR2 antagonist with an IC50 of 1.1 nM. BMS-741672 shows >700-fold selective for CCR2 than CCR5 .
|
-
- HY-12146
-
|
|
ELOVL
|
Metabolic Disease
|
|
ELOVL6-IN-2 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-2 inhibits mouse ELOVL6 activities, with an IC50 value of 34 nM .
|
-
- HY-107045
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
CHF 4227 free base is an orally active and selective estrogen receptor modulator (SERM) with high affinity to the human estrogen receptor-α and -β (Ki values of 0.017 nM and 0.099 nM, respectively) .
|
-
- HY-110343
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
DBM 1285 dihydrochloride is an orally active TNF-α production inhibitor with anti-inflammatory effects. DBM 1285 dihydrochloride inhibits Lipopolysaccharide (LPS)-induced TNF-α secretion in various cells of macrophage/monocyte lineage .
|
-
- HY-120643
-
|
|
11β-HSD
|
Metabolic Disease
|
|
BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC50 of 2.3 nM against human 11β-HSD1 .
|
-
- HY-121565
-
|
|
Insulin Receptor
|
Metabolic Disease
Endocrinology
|
|
SaRI 59-801 is an orally effective hypoglycemic compound with stimulation activity of insulin secretion. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice .
|
-
- HY-125558
-
|
ORG-34517
|
Glucocorticoid Receptor
|
Neurological Disease
|
|
PT150 (ORG-34517) is a competitive and orally active glucocorticoid receptor antagonist. PT150 shows neuroprotective effects. PT150 has the potential for the research of Parkinson’s disease .
|
-
- HY-14554
-
|
LY2140023
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research .
|
-
- HY-116524
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile .
|
-
- HY-19833
-
|
|
Cytochrome P450
|
Cancer
|
|
CFG920 is an orally active, nonsteroidal, reversible dual CYP17 and CYP11B2 inhibitor. CFG920 has the potential for metastatic castration-resistant prostate cancer research .
|
-
- HY-120049
-
-
- HY-103058
-
-
- HY-103692
-
|
|
STAT
|
Cancer
|
|
STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM .
|
-
- HY-15127
-
|
13-cis-Retinoic acid
|
RAR/RXR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Isotretinoin (13-cis-Retinoic acid) is an orally active vitamin A derivative and is often be used for the research of severe acne. Isotretinoin also shows anticancer activity .
|
-
- HY-116453
-
-
- HY-106084
-
|
T-2525; RO 19-5247; Cefterame
|
Bacterial
|
Infection
|
|
Cefteram (T-2525) is the free acid of Cefteram pivoxil (HY-106571), which is an orally active cephalosporin ester. Cefteram potently targets to the enteropathogenic Enterobacteriaceae and Vibrionaceae .
|
-
- HY-123863
-
|
|
FAAH
|
Neurological Disease
|
|
SSR411298 is an orally active, selective and reversible fatty acid amide hydrolase (FAAH) inhibitor. SSR411298 has the potential for post-traumatic stress disorder research .
|
-
- HY-B1271
-
|
G-28315
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Sulfinpyrazone (G-28315) is an orally active and potent uricosuric agent for chronic and intermittent gouty arthritis. Sulfinpyrazone has antithrombotic and platelet inhibitory effects .
|
-
- HY-106917
-
|
Ro 41-3696
|
GABA Receptor
|
Neurological Disease
|
|
Lirequinil (Ro 41-3696) is an orally active partial agonist of the benzodiazepine (BDZ) receptor. Lirequinil has the effect of promoting sleep .
|
-
- HY-155130
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 31 (compound 7k) is an orally active Plasmodium falciparum aspartic protease plasmepsin X (PMX) inhibitor .
|
-
- HY-116154
-
|
|
Reverse Transcriptase
HBV
|
Infection
|
|
Metacavir is an orally active, potent and specific nucleoside reverse transcriptase inhibitor against hepatitis B virus (HBV) with antiviral activity .
|
-
- HY-13728A
-
|
(R)-ZD 9331; (R)-BGC9331
|
Biochemical Assay Reagents
|
Cancer
|
|
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B0317R
-
|
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Amlodipine (Standard) is the analytical standard of Amlodipine. This product is intended for research and analytical applications. Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
|
-
- HY-168329
-
|
|
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
TGR5 agonist 7 (Compound 22-Na) is a gut-restricted, orally active agonist for G protein-coupled bile acid receptor TGR5 (GPBAR1 or GPR131) with an EC50 < 1 μM. TGR5 agonist 7 exhibits blood glucose lowering effect in mouse model, and can be used in diabete research .
|
-
- HY-B0010B
-
|
(±)Formoterol
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Formoterol ((±)Formoterol) is an orally active β2-selective agonist. Formoterol potently relaxes the peripheral airways through stimulating the beta 2-adrenoceptors selectively as is the case in the central airways and that it significantly inhibits IgE-mediated slow reactive substance of anaphylaxis (SRS-A) release through beta-adrenoceptor stimulation .
|
-
- HY-109189
-
|
BPI-7711
|
EGFR
|
Cancer
|
|
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
|
-
- HY-10439
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX .
|
-
- HY-137978
-
|
GNS561
|
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Ezurpimtrostat (compound 2-2) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases (extracted from patent WO2020048694 A1) .
|
-
- HY-144064
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity .
|
-
- HY-106584
-
|
Clospipramine
|
Dopamine Receptor
|
Neurological Disease
|
|
Mosapramine (Clospipramine) is an orally active and potent dopamine receptor antagonist with high affinity to dopamine receptor subtypes 2, 3 and 4, and with moderate affinity for the 5-HT 2 receptor. Mosapramine shows antipsychotic activity and can be used in schizophrenia research .
|
-
- HY-130126
-
|
SCO-792
|
Enteropeptidase
|
Others
|
|
Sucunamostat hydrate (SCO-792) is an orally active and reversible enteropeptidase inhibitor with IC50s of 4.6 nM and 5.4 nM for rat enteropeptidase and human enteropeptidase, respectively. Sucunamostat hydrate can slowly dissociate from enteropeptidase in vitro and inhibit protein digestion in vivo .
|
-
- HY-14789
-
-
- HY-144606
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC) .
|
-
- HY-173084
-
|
|
Phosphatase
MDM-2/p53
|
Cancer
|
|
BRD6257 is an orally active inhibitor for protein phosphatase, Mg2+/Mn2+ dependent 1D PPM1D with an IC50 of 5 nM. BRD6257 activates p53 signaling pathway with an EC50 of 51 nM, increases the p21 expression, inhibits the proliferation of cancer cell MOLM13 (IC50=2.8 μM). BRD6257 exhibits good metabolic stability in human and rat liver microsomes .
|
-
- HY-139590A
-
|
BOS-172738 hemiadipate; DS-5010 hemiadipate
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
|
-
- HY-156078
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α-glucosidase inhibitor with an IC50 value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research .
|
-
- HY-W013989
-
|
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
1,3-Dicyclohexylurea (DCU) is an orally active and potent sEH (soluble epoxide hydrolase) inhibitor. Oral Delivery of 1,3-Dicyclohexylurea nanosuspension enhances exposure and lowers blood pressure in hypertensive Rats .
|
-
- HY-105003
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease .
|
-
- HY-A0287S
-
|
Clomiphene-d5 (hydrochloride)
|
Isotope-Labeled Compounds
|
Others
|
|
Clomifene-d5 (hydrochloride) is a deuterium labeled Clomifene. Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation[1].
|
-
- HY-168915
-
|
|
Akt
PKA
|
Cancer
|
|
ML-B01 is the orally active inhibitor for Akt and PKA with the IC50 of 2 nM and 136 nM. ML-B01 exhibits good ability to penetrate the blood-brain barrier (BBB) in the mouse brain .
|
-
- HY-114853
-
|
|
PPAR
|
Metabolic Disease
|
|
BVT.13 is an orally active and selective PPARγ agonist with a maximal efficacy similar to that of Rosiglitazone (HY-17386). In addition, BVT.13 exhibits antidiabetic activity in ob/ob mice .
|
-
- HY-125824
-
|
PF-06882961
|
GCGR
|
Metabolic Disease
|
|
Danuglipron (PF-06882961) is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist. Danuglipron has the potential for type 2 diabetes research .
|
-
- HY-148570
-
|
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer .
|
-
- HY-16759B
-
|
MK-8931 tosylate
|
Beta-secretase
|
Neurological Disease
|
|
Verubecestat tosylate is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat tosylate effectively reduces Aβ40 and has the potential for Alzheimer's Disease .
|
-
- HY-105124
-
-
- HY-B1751F
-
-
- HY-107703
-
|
|
iGluR
|
Neurological Disease
|
|
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity . CGP 39551 shows measurable inhibitory activity at both L-[ 3H]-glutamate (Ki=8.4 μM) .
|
-
- HY-163700
-
|
|
Bacterial
|
Infection
|
|
Fabl inhibitor 1 (Compound (S)-n31) is an orally active and potent SaFabI inhibitor (IC50 = 94.0 nM, MIC = 0.25-1 μg/mL). Fabl inhibitor 1 can be used for the research of methicillin-resistant S. aureus (MRSA) infection .
|
-
- HY-129683
-
|
|
PPAR
|
Metabolic Disease
|
|
AM3102 is an oleoylethanolamide (OEA) analog. AM3102 is an endogenous high-affinity PPAR-alpha agonist. AM3102 resists enzymatic hydrolysis, activates PPAR-alpha with high potency in vitro, and persistently reduces feeding when administered in vivo either parenterally or orally .
|
-
- HY-106158
-
|
|
SGLT
|
Metabolic Disease
|
|
T-1095 is a selective and orally active Na +-glucose cotransporter (SGLT) inhibitor with IC50s of 22.8 µM and 2.3 µM for human SGLT1 and SGLT2, respectively. T-1095 can be used for diabetes research .
|
-
- HY-10011B
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
(Rac)-SCH 563705 is a racemic mixture of SCH 563705 (HY-10011). SCH 563705 (compound 16) is a potent and orally active CXCR2 and CXCR1 antagonist with IC50 values of 1.3 nM and 7.3 nM and Ki values of 1 nM and 3 nM, respectively .
|
-
- HY-16748
-
|
ABT-126
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease .
|
-
- HY-118134
-
|
|
Ser/Thr Protease
|
Cancer
|
|
Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 μM. Hepln-13 can be used for the research of metastatic prostate cancer .
|
-
- HY-147367
-
-
- HY-17383A
-
|
|
Antifolate
|
Neurological Disease
|
|
Levomefolate disodium is an orally active, BBB-penatrable and active form of folic acid. Levomefolate disodium can be used as a food supplement for folic acid and in the research of neural tube defect diseases .
|
-
- HY-144706
-
|
|
TAM Receptor
|
Cancer
|
|
Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases .
|
-
- HY-131065
-
|
|
c-Met/HGFR
|
Cancer
|
|
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity .
|
-
- HY-B0216
-
-
- HY-156290
-
-
- HY-109027
-
|
N91115
|
GSNOR
CFTR
|
Inflammation/Immunology
|
|
Cavosonstat (N91115) is an orally active S-nitrosoglutathione reductase (GSNOR) inhibitor. Cavosonstat is a CFTR stabilizer, and can be used for cystic fibrosis research .
|
-
- HY-117833
-
|
|
VAP-1
|
Inflammation/Immunology
|
|
PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects .
|
-
- HY-108492
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC50 = 0.042 μM) with minimal activity at S1P3 (EC50 = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge .
|
-
- HY-164462
-
|
|
PKC
NF-κB
Apoptosis
|
Cancer
|
|
BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice .
|
-
- HY-W587957
-
|
|
Bacterial
Parasite
|
Infection
|
|
Gypsogenic acid is a triterpenoid acid that can be isolated from Miconia stenostachya and has antibacterial and trypanoidal activities. The MICs values of Gypsogenic acid for the oral bacterial pathogens Enterococcus faecalis, Streptococcus salivarius, Streptococcus haematococcus, Streptococcus mutans and sobrinus were 50-200 μg/mL. Gypsogenic acid can induce blood cortensite cleavage in isolated mice with IC50 56.6 μM .
|
-
- HY-B0317S1
-
|
|
Isotope-Labeled Compounds
Calcium Channel
|
Cancer
|
|
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
|
-
- HY-19672
-
|
BAY 19-8004
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties .
|
-
- HY-12222R
-
|
|
FXR
Autophagy
|
Others
|
|
Obeticholic acid (Standard) is the analytical standard of Obeticholic acid. This product is intended for research and analytical applications. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
|
-
- HY-118706
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PD 118440 is an orally active dopamine (DA) agonist. PD 118440 has significant central nervous system effects, including inhibition of striatal DA synthesis, suppression of DA neuron firing, and reversal of Reserpine (HY-N0480)-induced depression in rats .
|
-
- HY-147250A
-
|
RLY-4008 hydrochloride
|
FGFR
|
Cancer
|
|
Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
|
-
- HY-162284
-
|
|
ADAMTS
|
Cardiovascular Disease
|
|
BAY-9835 is a potent and orally active ADAMTS7 and ADAMTS12 antagonist with IC50s of 6 nM and 30 nM, respectively. BAY-9835 is very selective against a range of off-targets and metalloproteases. BAY-9835 can be used for the atherogenesis research .
|
-
- HY-147250
-
|
RLY-4008
|
FGFR
|
Cancer
|
|
Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
|
-
- HY-144870
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-7, an aryl sulfonamido azetidine compound, is an orally active STAT3 inhibitor. STAT3-IN-7 has anticancer activities (WO2021016333A1, H182) .
|
-
- HY-107002A
-
|
|
Dopamine Receptor
|
Neurological Disease
Endocrinology
|
|
Lergotrile mesylate is a potent and orally active dopamine agonist and a prolactin secretion inhibitor. Lergotrile mesylate inhibits prolactin release from pituitaries by activating an adenohypophyseal dopamine receptor. Lergotrile mesylate has the potential for the research of Parkinson's disease .
|
-
- HY-162692
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-14 (compound 78) is a potent, selective DNA-PK inhibitor with an IC50 value of 7.95 nM. DNA-PK-IN-14 has oral activity and has the potential to be a radiosensitizer for cancer treatment .
|
-
- HY-13768C
-
|
SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
|
Topoisomerase
Apoptosis
Autophagy
|
Cancer
|
|
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity .
|
-
- HY-162555
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
BMS-986308 is a selective and orally active renal outer medullary potassium (ROMK) channel inhibitor. BMS-986308 is selective for ROMK over hERG. BMS-986308 can be used for heart failure research .
|
-
- HY-118189
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers . Misoprostol is an oral agent used to induce labor .
|
-
- HY-143430
-
|
|
CDK
|
Cancer
|
|
(S)-LY3177833 ((S)-Example 2) is an orally active CDC7 kinase inhibitor. (S)-LY3177833 shows broad in vitro anticancer activity .
|
-
- HY-162961
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-16 is potent and orally active xanthine oxidase (XO) inhibitor with an IC50 of 102 nM. Xanthine oxidase-IN-16 shows significant efficacy in hyperuricemia rats .
|
-
- HY-109144
-
|
DWP-16001
|
SGLT
|
Metabolic Disease
|
|
Enavogliflozin (DWP-16001), an antidiabetic agent, is an orally active, best-in-class and selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor .
|
-
- HY-113655
-
|
|
PPAR
|
Metabolic Disease
|
|
AD-5075 is an orally active insulin sensitizer. AD-5075 mediates its antidiabetic activity by binding to PPARγ and thereby generating an active conformation of the receptor .
|
-
- HY-143430A
-
|
|
CDK
|
Cancer
|
|
(S)-LY3177833 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. (S)-LY3177833 hydrate shows broad in vitro anticancer activity .
|
-
- HY-11059
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
KH064, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). KH064 has anti-inflammatory activity .
|
-
- HY-123891
-
|
|
EGFR
|
Cancer
|
|
NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC50 of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .
|
-
- HY-B0089R
-
|
|
Glycosidase
|
Metabolic Disease
Cancer
|
|
Acarbose (Standard) is the analytical standard of Acarbose. This product is intended for research and analytical applications. Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
|
-
- HY-B1751
-
-
- HY-19284
-
|
FK 687; TF 505
|
5 alpha Reductase
|
Endocrinology
|
|
FR-146687 (FK 687) is a selective and orally active 5α-reductase inhibitor with IC50s of 1.7 nM and 4.6 nM for rat and human 5α-reductases, respectively. FR-146687 shows no inhibitory effects on other steroid oxidoreductases .
|
-
- HY-19985
-
|
|
EGFR
|
Cancer
|
|
PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer .
|
-
- HY-16748A
-
|
ABT-126 citrate
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease .
|
-
- HY-B0024
-
|
NM441
|
Bacterial
Antibiotic
|
Infection
|
|
Prulifloxacin (NM441) is an orally active fluoroquinolone antibiotic with a broad spectrum of activity against Gram-positive and -negative bacteria. Prulifloxacin is a proagent of a thiazeto-quinoline carboxylic acid derivative Ulifloxacin (NM394). Prulifloxacin has the potential for lower urinary tract infections and exacerbations of chronic bronchitis .
|
-
- HY-161862
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-44 is a potent and orally active COX-2 inhibitor with IC50 values of 0.18,1.14 µM for COX-2, COX-1, respectively. COX-2-IN-44 shows anti-inflammatory activity .
|
-
- HY-10449
-
|
TS 071
|
SGLT
|
Metabolic Disease
|
|
Luseogliflozin (TS 071) is a potent, selective, orally active sodium-dependent glucose cotransporter (SGLT) 2 inhibitor, with an IC50 of 2.26 nM, about 1765-fold selectivity over SGLT1 (IC50, 3990 nM). Luseogliflozin has the protential for researching type 2 diabetes .
|
-
- HY-115936
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-9 (compound 7a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 10.17 uM. COX-2-IN-9 has higher COX-2 selectivity than Celecoxib. COX-2-IN-9 shows good in vivo anti-inflammatory and low ulcerogenic activity .
|
-
- HY-115934
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-7 (compound 4a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 6.585 uM. COX-2-IN-7 has higher COX-2 selectivity than Celecoxib. COX-2-IN-7 shows good in vivo anti-inflammatory and low ulcerogenic activity .
|
-
- HY-115935
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-8 (compound 6a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 6.585 uM. COX-2-IN-8 has higher COX-2 selectivity than Celecoxib. COX-2-IN-8 shows good in vivo anti-inflammatory and low ulcerogenic activity .
|
-
- HY-114379
-
|
|
LPL Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
AS2717638 is a highly selective, brain-penetrant and orally active lysophosphatidic acid receptor 5 (LPA5) antagonist with an IC50 value of 38 nM. AS2717638 is highly selective and shows no significant antagonistic activity against other LPA receptors (LPA1, LPA2, and LPA3). AS2717638 can be used in the research of pain and neuroinflammation-related diseases .
|
-
- HY-32219
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
T863 is an orally active, selective and potent DGAT1 (acyl-CoA:diacylglycerol acyltransferase 1) inhibitor with an IC50 of 15 nM. T863 has no inhibitory activity against human MGAT3, human DGAT2, or human MGAT2. T863 interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells .
|
-
- HY-W027951
-
|
DMTU
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
N,N'-Dimethylthiourea (DMTU), isolated from Allium sativum, is an orally active scavenger of hydroxyl radical (•OH) and blocks •OH production by activated neutrophils in vitro. N,N'-Dimethylthiourea protects against water-immersion restraint stress (WIRS)-induced gastric mucosal lesions in rats by exerting its antioxidant action including •OH scavenging and anti-inflammatory action .
|
-
- HY-155463
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
|
Inflammation/Immunology
|
|
NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM .
|
-
- HY-B2085
-
|
Arsthinol; Balarsen
|
Others
|
Cancer
|
|
Arsthinenol is an orally active antitumor agent, that exhibits cytotoxicity in U87MG cells with an IC50 of 31.6 μM. Arsthinenol forms complex with cyclodextrin, inhibits the tumor growth and improves the survival rates of U87MG xenograft mice .
|
-
- HY-138564
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
NOS-IN-1 is a potent and orally active NO synthase (NOS) isoforms inhibitor with IC50s of 0.1 μM, 1.1 μM, and 0.2 μM for human iNOS (hiNOS), heNOS and hnNOS, respectively .
|
-
- HY-A0213
-
|
Tiludronic acid
|
Proton Pump
|
Inflammation/Immunology
|
|
Tiludronate (Tiludronic Acid), an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties .
|
-
- HY-B1196
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Tiapride hydrochloride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride hydrochloride shows anti-dyskinetic activity and anxiolytic activity. Tiapride hydrochloride is a neuroleptic agent .
|
-
- HY-168110
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-52 is a potent and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 value of 10.4 nM. HPK1-IN-52 exhibits anti-tumor activities .
|
-
- HY-108194
-
|
|
Biochemical Assay Reagents
|
Others
|
|
CGP 46700 (Compound 49) is an orally active iron chelator, that exhibits high affinity for iron, removes iron from ferritin and human serum transferrin. CGP 46700 promotes iron excretion in a mouse iron overload model .
|
-
- HY-135891
-
|
|
CCR
|
Neurological Disease
|
|
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
|
-
- HY-N0420A
-
|
Wormwood acid tromethamine
|
Endogenous Metabolite
|
Neurological Disease
|
|
Succinic acid tromethamine is a potent and orally active anxiolytic agent. Succinic acid tromethamine is an intermediate product of the tricarboxylic acid cycle. Succinic acid tromethamine can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries .
|
-
- HY-125824A
-
|
PF-06882961 tromethamine
|
GCGR
|
Metabolic Disease
|
|
Danuglipron (PF-06882961) tromethamine is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist. Danuglipron tromethamine has the potential for type 2 diabetes research .
|
-
- HY-B0452A
-
|
DU21220
|
Adrenergic Receptor
|
Endocrinology
|
|
Ritodrine (DU21220) is a potent and orally active β-adrenergic agonist. Ritodrine decreases preterm delivery and uterine contraction. Ritodrine has the potential for the research of preterm labor .
|
-
- HY-117805
-
-
- HY-B0452
-
|
DU21220 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
|
|
Ritodrine (DU21220) hydrochloride is a potent and orally active β-adrenergic agonist. Ritodrine hydrochloride decreases preterm delivery and uterine contraction. Ritodrine hydrochloride has the potential for the research of preterm labor .
|
-
- HY-34439S1
-
-
- HY-137978A
-
|
GNS561 hydrochloride
|
Others
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Ezurpimtrostat hydrochloride (compound 2-3) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat hydrochloride reduces significantly the liver fibrosis in DEN (diethyl nitrosamine) cirrhotic rat model. Ezurpimtrostat hydrochloride can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases .
|
-
- HY-169821
-
|
|
SGLT
|
Metabolic Disease
|
|
SGLT1/2-IN-8 (compound 8) is a potent and orally active SGLT1/2 dual inhibitor with IC50 values of 4 nM and 1 nM, respectively. SGLT1/2-IN-8 exhibits anti-hyperglycemic effects and can be utilized in relevant research .
|
-
- HY-17643
-
|
VT-1161
|
Fungal
Cytochrome P450
|
Infection
|
|
Oteseconazole (VT-1161) is a potent and orally active anti-fungal agent. Oteseconazole potently binds to and inhibits Candida albicans cytochrome P45051 (CYP51) activity (Kd ≤39 nM), shows no obvious effect on human CYP51. Oteseconazole also can be used for the research of dermatophytes .
|
-
- HY-171296
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
p38 Kinase inhibitor 8 (Compound CCLXXVIII) is the orally active inhibitor for p38β and JNK2α2 with IC50 of 6.3 nM and 53.6 nM. p38 Kinase inhibitor 8 exhibits anti-inflammatory effect in rats collagen-induced arthritis models .
|
-
- HY-153704
-
|
|
CDK
|
Cancer
|
|
CDK4/6-IN-17 (compound 12) is an orally active CDK4/6 inhibitor with IC50 ranging of 10-100 nM in BE(2) cells. CDK4/6-IN-17 inhibits tumor growth in COLO205 xenograft model .
|
-
- HY-107923
-
|
N1-Acetylsulfisoxazole
|
Bacterial
|
Infection
|
|
Sulfisoxazole acetyl (N1-Acetylsulfisoxazole), a Sulfisoxazole derivative, is an orally active dihydropteroate synthase inhibitor. Sulfisoxazole acetyl has an antibacterial action .
|
-
- HY-115989
-
|
|
HCV
|
Infection
|
|
HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
|
-
- HY-145653
-
-
- HY-113926
-
|
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
BAY 60-2770 is a potent, selective, and orally active soluble guanylyl cyclase (sGC) activator. BAY 60-2770 increases the activity of sGC in a nitric oxide-independent manner. BAY 60-2770 shows antifibrotic effect .
|
-
- HY-16759
-
|
MK-8931
|
Beta-secretase
|
Neurological Disease
|
|
Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease .
|
-
- HY-A0213A
-
|
Tiludronic acid disodium
|
Proton Pump
|
Inflammation/Immunology
|
|
Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties .
|
-
- HY-162076
-
|
|
Cathepsin
|
Neurological Disease
|
|
AEP-IN-3 (compound 18) is an orally active, potent and brain penetrant asparagine endopeptidase (AEP) inhibitor, with an IC50 of 7.8 ± 0.9 nM. AEP-IN-3 can be used for Alzheimer’s Disease (AD) research .
|
-
- HY-B0265R
-
|
|
Autophagy
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Nimodipine (Standard) is the analytical standard of Nimodipine. This product is intended for research and analytical applications. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders .
|
-
- HY-N9515
-
|
|
Others
|
Neurological Disease
|
|
Diallyl tetrasulfide is an orally active diallyl polysulfide that can be isolated from garlic. Diallyl tetrasulfide has high activities to inhibit lipid peroxidation. Diallyl tetrasulfide possesses cytoprotective and antioxidant activities against cadmium-induced cytotoxicity .
|
-
- HY-107725
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIBO3304 is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively) .
|
-
- HY-152947
-
|
|
ELOVL
|
Metabolic Disease
|
|
ELOVL6-IN-4 is a potent, selective, and orally active long chain fatty acid elongase 6 (ELOVL6) inhibitor with IC50s of 79 nM and 94 nM for human and mouse ELOVL6, respectively. ELOVL6-IN-4 shows excellent selectivity over the other human ELOVL subtypes (ELOVL1, -2, -3, and -5) and mouse ELOVL3 .
|
-
- HY-116278
-
|
|
STAT
|
Cancer
|
|
HJC0149 is a potent and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3) .
|
-
- HY-16730
-
|
PF-6450567
|
Parasite
|
Infection
|
|
Sarolaner (PF-6450567) is an orally active and broad-spectrum ectoparasiticide. Sarolaner is an isoxazoline compound which shows efficacy against fleas and ticks on dogs, with a LC80 value of 0.3 μg/mL against C. felis and a LC100 value of 0.003 μg/mL against O. turicata .
|
-
- HY-B1751A
-
-
- HY-B1751E
-
-
- HY-131349
-
|
|
CCR
|
Cancer
|
|
CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity .
|
-
- HY-131349A
-
|
|
CCR
|
Metabolic Disease
Cancer
|
|
CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity .
|
-
- HY-139970
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
|
-
- HY-116183
-
|
|
HCV
|
Infection
|
|
ITX 4520 is an orally active and potent hepatitis C virus inhibitor exhibiting an excellent PK profile in both rats and dogs .
|
-
- HY-N0465R
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Olaquindox (Standard) is the analytical standard of Olaquindox. This product is intended for research and analytical applications. Olaquindox, a quinoxalin derivative, is an orally active antibiotic. Olaquindox stimulates growth and decreases intestinal mucosal immunity of piglets .
|
-
- HY-116713
-
-
- HY-B0925R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Oxacillin (sodium salt) (Standard) is the analytical standard of Oxacillin (sodium salt). This product is intended for research and analytical applications. Oxacillin sodium salt is an orally active synthetic penicillin with good bactericidal activity against staphylococci and other gram-positive pathogens .
|
-
- HY-115923
-
-
- HY-B1390BR
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Saccharin (sodium hydrate) (Standard) is the analytical standard of Saccharin (sodium hydrate). This product is intended for research and analytical applications. Saccharin sodium hydrate is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium hydrate has bacteriostatic and microbiome-modulating properties .
|
-
- HY-Y0272R
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Saccharin (Standard) is the analytical standard of Saccharin. This product is intended for research and analytical applications. Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties .
|
-
- HY-144444
-
|
|
EGFR
|
Cancer
|
|
NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases .
|
-
- HY-123473
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
SB-414796 is a selective, orally active and cross the blood-brain barrier dopamine D3 receptor antagonist with Ki values of 4, 400 nM for D3, D2, respectively .
|
-
- HY-144445
-
|
|
EGFR
|
Cancer
|
|
NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases .
|
-
- HY-19926
-
|
RG-7602
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies .
|
-
- HY-B1390AR
-
|
|
Bacterial
|
Infection
|
|
Saccharin (sodium) (Standard) is the analytical standard of Saccharin (sodium). This product is intended for research and analytical applications. Saccharin sodium is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium has bacteriostatic and microbiome-modulating properties .
|
-
- HY-13723R
-
|
|
Phosphatase
|
Inflammation/Immunology
|
|
Pimecrolimus (Standard) is the analytical standard of Pimecrolimus. This product is intended for research and analytical applications. Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrolimus shows anti-inflammatory activity .
|
-
- HY-120438
-
|
|
PI3K
Akt
|
Inflammation/Immunology
|
|
TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research .
|
-
- HY-15991A
-
|
AZD1722 hydrochloride; RDX5791 hydrochloride
|
Na+/H+ Exchanger (NHE)
|
Metabolic Disease
|
|
Tenapanor (AZD1722) hydrochloride is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor hydrochloride reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor hydrochloride has the potential for the research of hyperphosphatemia .
|
-
- HY-15991
-
|
AZD1722; RDX5791
|
Na+/H+ Exchanger (NHE)
|
Metabolic Disease
|
|
Tenapanor (AZD1722) is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor has the potential for the research of hyperphosphatemia .
|
-
- HY-17479B
-
|
AHR 5850 sodium
|
COX
|
Inflammation/Immunology
|
|
Amfenac sodium (AHR 5850 sodium) is an orally active and potent anti-inflammatory compound possessing antipyretic and analgesic properties. Amfenac sodium can be used for the research of acute and chronic inflammation .
|
-
- HY-B0232
-
|
UK 68789
|
Potassium Channel
|
Cardiovascular Disease
|
|
Dofetilide (UK 68789), as a class III antiarrhythmic agent, is an orally active, potent and specific IKr blocker. Dofetilide can be used for the research of cardiovascular disease .
|
-
- HY-17479
-
|
|
COX
|
Inflammation/Immunology
|
|
Amfenac (AHR 5850) is an orally active and potent anti-inflammatory compound possessing antipyretic and analgesic properties. Amfenac can be used for the research of acute and chronic inflammation .
|
-
- HY-A0161A
-
|
Clofedanol hydrochloride; Calmotusin hydrochloride; NSC 113595 hydrochloride
|
Others
|
Infection
|
|
Chlophedianol (Clofedanol) hydrochloride is an orally active and potent antitussive agent. Chlophedianol hydrochloride can be used for the research of acute cough due to upper respiratory tract infections (URIs) .
|
-
- HY-168521
-
|
|
Integrin
|
Inflammation/Immunology
|
|
αvβ6-IN-1 (compound 28) is a potent and orally active αvβ6 integrin inhibitor with a pIC50 value of 8.1. αvβ6-IN-1 has the potential for the research of idiopathic pulmonary fibrosis .
|
-
- HY-15010
-
-
- HY-106098
-
|
BM 14478
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Adibendan (BM 14478), a benzimidazole derivative, is an orally active, selective phosphodiesterase III (PDE III) activity inhibitor (IC50=2.0 μM). Adibendan has IC50 values more than 60-fold higher for the inhibition of PDE I or II. Adibendan is a new cardiotonic agent .
|
-
- HY-16346R
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Netupitant (Standard) is the analytical standard of Netupitant. This product is intended for research and analytical applications. Netupitant (CID-6451149) is a highly potent, selective and orally active neurokinin-1 (NK1) receptor antagonist with a Ki of 0.95 nM for hNK1 in CHO cells. Netupitant has antiemetic affect .
|
-
- HY-107338
-
|
Vratizolin; Wratizolin
|
HSV
Interleukin Related
|
Infection
Inflammation/Immunology
Cancer
|
|
Denotivir (Vratizolin) is an orally active antiviral agent for herpes simplex virus (HSV) and varicella-zoster virus (VZV). Denotivir inhibits the proliferation of various cancer cells, and exhibits anti-leukemic activity. Denotivir inhibits the generation of TNF-α, IL-1 and IL-6, exhibits immunosuppressive efficacy .
|
-
- HY-11091
-
|
BMS 561389 hydrochloride; DPC 906 hydrochloride
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity .
|
-
- HY-173030
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Opioid receptor agonist 1 (Compound 2638-28) is the orally active agonist for opioid receptor that exhibits good affinity to MOR, DOR and KOR with Ki of 5, 24 and 212 nM, respectively. Opioid receptor agonist 1 exhibits analgesic activity in mouse warm water tail flick models and acetic acid writhing models .
|
-
- HY-153702
-
|
|
JAK
|
Cancer
|
|
JAK-IN-27 (compound 1) is an orally active and potent JAKS family kinase inhibitor with IC50s of 3.0 nM (TYK2), 7.7 nM (JAK1), 629.6 nM (JAK3), respectively. JAK-IN-27 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=23.7 nM) .
|
-
- HY-19569
-
|
ABT-494
|
JAK
|
Inflammation/Immunology
|
|
Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research .
|
-
- HY-100888
-
|
TAK-931
|
CDK
|
Cancer
|
|
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity .
|
-
- HY-147402
-
|
D-0502
|
Estrogen Receptor/ERR
|
Cancer
|
|
Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models .
|
-
- HY-B0758
-
|
|
Others
|
Inflammation/Immunology
|
|
Troxipide is an orally active defensive factor-enhancing therapeutic agent for gastritis and gastric ulcer (GU). Troxipide is a non-antisecretory gastro protective agent with antiulcer, anti-inflammatory and mucus-secreting properties .
|
-
- HY-164040
-
|
|
Somatostatin Receptor
|
Metabolic Disease
|
|
Zavolosotine (Compound 1) is an orally active agonist for somatostatin receptor type 5 (SST5) with EC50 <1 nM. Zavolosotine inhibits insulin and glucagon secretion, increases levels of glucagon in blood in rat model .
|
-
- HY-132293
-
|
|
DNA-PK
|
Cancer
|
|
BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (IC50=81 nM). BAY-8400 can be used for the research of cancer .
|
-
- HY-116386
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
GSK334429 is a selective and orally active non-imidazole histamine H3 receptor antagonist with a pKi of 9.49 against human H3 receptor. GSK334429 can be utilized in neurological research .
|
-
- HY-133127
-
|
|
Glucokinase
|
Metabolic Disease
|
|
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity .
|
-
- HY-133127A
-
|
|
Glucokinase
|
Metabolic Disease
|
|
AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity .
|
-
- HY-N0661
-
-
- HY-A0213B
-
|
Tiludronic acid disodium hemihydrate
|
Proton Pump
|
Metabolic Disease
|
|
Tiludronate (Tiludronic Acid) disodium hemihydrate, an orally active bisphosphonate, can act an osteoregulator. Tiludronate disodium hemihydrate is used for the research of the metabolic bone disorders. Tiludronate disodium hemihydrate is a potent inhibitor of the osteoclast vacuolar H +-ATPase. Antiresorptive and anti-inflammatory properties .
|
-
- HY-B0281A
-
-
- HY-A0276
-
|
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Gentamicin sulfate, an orally active aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. Gentamicin sulfate inhibits DNase I with an IC50 of 0.57 mM .
|
-
- HY-12410
-
|
|
Itk
|
Inflammation/Immunology
|
|
GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma .
|
-
- HY-123058
-
|
|
PI3K
Autophagy
|
Cancer
|
|
Vps34-IN-4 (compound 19) is a potent, selective, and orally active inhibitor of VPS34. Vps34-IN-4 inhibits the autophagy in vivo. Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components .
|
-
- HY-103226
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
SC-57461A is a potent, orally active, nonpeptide, and selective inhibitor of Leukotriene A4 (LTA4) hydrolase with IC50s of 2.5 nM, 3 nM, and 23 nM for recombinant human, mouse, and rat LTA4 hydrolase, respectively .
|
-
- HY-161937
-
|
|
Topoisomerase
Bacterial
|
Infection
|
|
Antibacterial agent 236 (Compound 4l) is an orally active inhibitor for DNA gyrase and topoisomerase IV (IC50 is 3.2 and 300 nM in Staphylococcus aureus), and exhibits board-spectrum antibacterial activity. Antibacterial agent 236 exhibits good pharmacokinetic properties in mice .
|
-
- HY-16759A
-
|
MK-8931 TFA
|
Beta-secretase
|
Neurological Disease
|
|
Verubecestat (MK-8931) TFA is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat TFA effectively reduces Aβ40 and has the potential for Alzheimer's Disease .
|
-
- HY-121341R
-
|
|
Bacterial
|
Infection
|
|
Brodimoprim (Standard) is the analytical standard of Brodimoprim. This product is intended for research and analytical applications. Brodimoprim (Ro 10-5970), a trimethoprim analogue, is an orally active dihydrofolate reductase inhibitor. Brodimoprim is highly active against a broad spectrum of gram-negative and gram-positive bacteria .
|
-
- HY-169946
-
|
|
Wee1
|
Cancer
|
|
WEE1/PKMYT1-IN-1 (compound 75) is a potent and orally active WEE1 and PKMYT1 inhibitor. WEE1/PKMYT1-IN-1 shows antiproliferation activity .
|
-
- HY-115922
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 10 (compound 30) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 10 expresses activity on COX-2 enzyme more than COX-1. Anti-inflammatory agent 10 is orally active .
|
-
- HY-19562A
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
PF-06260933 hydrochloride is the hydrochloride form of PF-06260933 (HY-19562). PF-06260933 hydrochloride is an orally active and highly selective inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively .
|
-
- HY-147987
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
FFA1 agonist-1 (Compound 17a) is an orally active fatty acid receptor 1 (FFA1) agonist with an EC50 of 0.75 μM. FFA1 agonist-1 can be used for type 2 diabetes mellitus research .
|
-
- HY-13768
-
|
SKF 104864A; NSC 609669
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity .
|
-
- HY-115921
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 9 (compound 28) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 9 expresses activity on COX-2 enzyme more than COX-1. Anti-inflammatory agent 9 is orally active .
|
-
- HY-B0693
-
-
- HY-B0255R
-
|
|
HBV
Reverse Transcriptase
Orthopoxvirus
Endogenous Metabolite
|
Infection
Cancer
|
|
Adefovir dipivoxil (Standard) is the analytical standard of Adefovir dipivoxil. This product is intended for research and analytical applications. Adefovir dipivoxil, an adenosine analogue, is an oral proagent of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains . Adefovir dipivoxil shows anti-orthopoxvirus activity.
|
-
- HY-121778
-
|
Melitracene; N 7001; Trausabun
|
5-HT Receptor
|
Neurological Disease
|
|
Melitracen (Melitracene) is an orally active tricyclic antidepressant and it is also a bipolar thymoleptic with activating properties. Melitracen inhibits 3H-5-HT and 14H-5-HT with IC50s of 670 nM and 5500 nM, respectively. Melitracen can be used for the research of depression and anxiety .
|
-
- HY-170434
-
|
|
Bcl-2 Family
Caspase
|
Cancer
|
|
Bfl-1-IN-6 (Compound 20) is an orally active inhibitor for Bcl-2 related protein A1 (BFL1) with an IC50 of 19 nM. Bfl-1-IN-6 stabilizes BFL1 protein, activates cleaved caspase 3, and exhibits antitumor efficacy in mouse models .
|
-
- HY-159106
-
-
- HY-163994
-
|
KWD 2058 hydrochloride
|
Others
|
Others
|
|
Ibuterol (KWD 2058) hydrochloride, a diester of Terbutaline (HY-B0802A), is an orally active, selective and effective β-stimulating agent with lipophilic activities. Ibuterol hydrochloride is also an orally active ocular hypotensive agent. Ibuterol hydrochloride relieves bronchial obstruction in asthma without causing circulatory effects. Ibuterol hydrochloride is proming for rasearch of intraocular hypertension, asthma and bronchitis .
|
-
- HY-109149
-
|
KP 106
|
Others
|
Neurological Disease
|
|
Lomardexamfetamine (KP 106) is an orally active central nervous system stimulant composed of d-amphetamine and a ligand. Lomardexamfetamine can be used for the research of attention-deficit hyperactivity disorder .
|
-
- HY-107722
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC50 of 12 nM and Ki of 0.3 nM. SCH 221510 shows an anxiolytic-like effect .
|
-
- HY-14771A
-
-
- HY-118410
-
|
|
Integrin
|
Cardiovascular Disease
|
|
L-738167 is an orally active fibrogen receptor antagonist that prevents the binding of fibrinogen to GP IIb/IIIa. L-738167 can be utilized in thrombus research .
|
-
- HY-106968
-
|
|
iGluR
|
Neurological Disease
|
|
ZD-9379 is a potent, orally active, and brain penetrant full antagonist at the glycine site of the NMDA receptor. ZD-9379 has neuroprotective effect .
|
-
- HY-B1526
-
|
Thioacetazone; Amithiozone
|
Bacterial
Antibiotic
|
Infection
|
|
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL .
|
-
- HY-14691
-
|
BAY 869766; RDEA119
|
MEK
|
Cancer
|
|
Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
|
-
- HY-106832A
-
|
Watanidipine hydrochloride; AE0047
|
Calcium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Vatanidipine (Watanidipine) hydrochloride is an orally active dihydropyridine (DHP)-type calcium channel blocker and a useful antihypertensive agent. Vatanidipine hydrochloride shows vasodilatory effects and also suppresses noradrenaline release from sympathetic nerve endings .
|
-
- HY-146615
-
|
|
TAM Receptor
|
Cancer
|
|
Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
|
-
- HY-B1660
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Guanadrel sulfate is an orally active, potent and postganglionic sympathetic inhibitor. Guanadrel sulfate lowers blood pressure by reducing systemic vascular resistance with little effect on cardiac output. Guanadrel sulfate is promising for research of hypertension .
|
-
- HY-133141
-
|
TRE-515
|
DNA/RNA Synthesis
|
Cancer
|
|
DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK .
|
-
- HY-136977
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity .
|
-
- HY-102057
-
|
TD-8954
|
5-HT Receptor
|
Others
|
|
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
|
-
- HY-145924
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
BAY 2666605 is an orally active PDE3A and PDE3B inhibitor with IC50s of 87 nM and 50 nM, respectively. BAY 2666605 is a PDE3A-SLFN12 complex inducer (WO2019025562A1; example 135) .
|
-
- HY-16983
-
|
|
ROR
|
Inflammation/Immunology
|
|
GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC50 of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-172131
-
|
|
Parasite
|
Infection
|
|
Emoquine-1 is an orally active and potent antimalarial drug. Emoquine-1 is efficient against multidrug-resistant Plasmodium parasites, including the Artemisinin-resistant quiescent stage. Emoquine-1 is active against proliferative P. falciparum with IC50 values of 20-55 nM. Emoquine-1 is a candidate to fight Plasmodium parasites resistant to artemisinin-based combination therapies (ACTs) with a capacity to eliminate persistent parasites .
|
-
- HY-138684
-
-
- HY-138684A
-
-
- HY-P5971
-
|
Mifomelatide
|
Melanocortin Receptor
|
Metabolic Disease
|
|
TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia .
|
-
- HY-161903
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
Progranulin modulator-3 (compd C40) is a brain-penetrant and orally active progranulin (PGRN) inducer. Progranulin modulator-3 can be used for neurological research .
|
-
- HY-126248
-
|
|
PARP
|
Cancer
|
|
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model .
|
-
- HY-160984
-
|
TEI 5103; TG 51
|
Others
|
Endocrinology
|
|
Rotraxate (TEI 5103) is an orally active anti-ulcer compound. Rotraxate can increase blood flow to the gastric mucosa and promote the integrity of the gastric mucosa. Rotraxate can be used to study the protective effects of drugs on the gastric mucosa, especially in investigating how drugs can prevent or treat gastric ulcers by acting directly on the gastric mucosa .
|
-
- HY-162622
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
BET-IN-26 (compound 13a) is a potent, selective and orally active BD1 inhibitor with IC50 values of 0.0055, 9.0 µM for BD1, BD2, respectively. BET-IN-26 decreases LPS (HY-D1056) induced serum levels of IL-6 and MCP-1 .
|
-
- HY-B1751D
-
-
- HY-107355
-
|
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Letosteine is an orally active, potent and safe expectorant. Letosteine has the effect of scavenging reactive oxygen species (ROS). Letosteine dissolves bronchial mucus and reduces respiratory inflammation symptoms, and restores gas exchanges and natural defense mechanisms in the lung. Letosteine can be used for acute or chronic respiratory diseases (such as bronchopneumopathies) research .
|
-
- HY-170523
-
|
|
SARS-CoV
DNA Methyltransferase
|
Infection
|
|
RU-0415529 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 of 356 nM. RU-0415529 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and the viral replication. RU-0415529 exhibits anti-infectious activity in mouse models .
|
-
- HY-123812
-
|
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research .
|
-
- HY-159886
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
MG-C-30 is an orally active agonist for CD27 with an EC50 of 0.84 μM. MG-C-30 activates NK cells and T cell co-stimulatory signals, and enhances immune response. MG-C-30 exhibits antitumor efficacy in mouse EG7-OVA model .
|
-
- HY-14904A
-
|
|
Influenza Virus
SARS-CoV
|
Infection
|
|
Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells . Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity .
|
-
- HY-N7225
-
|
Gnidilatidin
|
DNA/RNA Synthesis
|
Cancer
|
|
Yuanhuacine (Gnidilatidin), a diterpene from Daphne genkwa, is an effective and highly selective inhibitor of the basal-like 2 (BL2) subtype of TNBC. Yuanhuacine can induce G2/M cell cycle arrest and has broad anti-tumor activity. Yuanhuacine is an orally active DNA damaging agent .
|
-
- HY-123840
-
|
|
GABA Receptor
|
Neurological Disease
|
|
MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect .
|
-
- HY-122058A
-
|
|
CXCR
HIV
|
Infection
Inflammation/Immunology
|
|
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM .
|
-
- HY-12995
-
|
|
FLAP
|
Cardiovascular Disease
Inflammation/Immunology
|
|
BI 665915 is an orally active and potent 5-lipoxygenase-activating protein (FLAP) inhibitor. BI 665915 inhibits FLAP production that blocks LTB4 biosynthesis in mice. BI 665915 is promising for research of various inflammatory diseases, including respiratory and cardiovascular diseases .
|
-
- HY-151484
-
|
|
Parasite
|
Infection
|
|
Anti-infective agent 4 (compound 73) is an orally active inhibitor of Trypanosoma cruzi with an IC50 value of 0.016 μM. Anti-infective agent 4 effectively reduces parasite burden in vivo. Anti-infective agent 4 can be used for the research of infection .
|
-
- HY-14900
-
|
GRC-10693
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment .
|
-
- HY-103266
-
|
|
Aurora Kinase
|
Cancer
|
|
TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
|
-
- HY-14853
-
|
YM150
|
Factor Xa
Ser/Thr Protease
|
Cardiovascular Disease
|
|
Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects .
|
-
- HY-162461
-
|
|
Reverse Transcriptase
HIV
|
Infection
|
|
HIV-1 inhibitor-66 is an orally active non-nucleoside reverse transcription inhibitor (NNRTI). HIV-1 inhibitor-66 shows inhibitory activity against wild-type HIV-1 reverse transcriptase with an IC50 of 40 nM .
|
-
- HY-12717R
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Phentolamine (Standard) is the analytical standard of Phentolamine. This product is intended for research and analytical applications. Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction .
|
-
- HY-106316
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 can be used for the research of pentylenetetrazol-induced seizures .
|
-
- HY-114977
-
|
|
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Avenanthramide A is a phytoalexin, which can be found in oats (Avena sativa L.). Avenanthramide A targets the RNA helicase DDX3, leads to mitochondrial swelling and increased ROS production, and induces apoptosis in CRC cells. Avenanthramide A exhibits antitumor efficacy in mouse model. Avenanthramide A orally active .
|
-
- HY-168952
-
|
|
STING
IFNAR
Interleukin Related
|
Inflammation/Immunology
|
|
GHN105 is an orally active inhibitor for STING that inhibits STING-dependent IFN-β secretion in THP-1 human monocytes with an IC50 of 4.4 μM. GHN105 reduces the IFN-β, IL-6 and CXCL10 levels in serum, and alleviates colitis in DSS (HY-116282)-induced acute colitis mouse model. GHN105 exhibits good pharmacokinetic parameters in mice with an oral bioavailability of 43% and a half-life of 1.1 hours .
|
-
- HY-147402A
-
|
D-0502 meglumine
|
Estrogen Receptor/ERR
|
Cancer
|
|
Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models .
|
-
- HY-132297
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer .
|
-
- HY-106582
-
|
MST 16
|
Topoisomerase
|
Cancer
|
|
Sobuzoxane (MST-16) is an orally active topoisomerase II inhibitor. Sobuzoxane causes irreversible inhibition of cell division. Sobuzoxane can be used in the study of non-Hodgkin's lymphoma that is resistant to conventional chemotherapy or has recurred .
|
-
- HY-132297A
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer .
|
-
- HY-129288
-
|
NEU-391
|
EGFR
Paraptosis
|
Infection
|
|
GW837016X (NEU-391) is an orally active ErbB-2 kinase covalent inhibitor. GW837016X also is a potent antitrypanosome agent. GW837016X inhibits mitosis and cytokinesis .
|
-
- HY-10716A
-
|
|
GlyT
|
Neurological Disease
|
|
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
|
-
- HY-P10397
-
|
rALP-2, Rubisco anxiolytic-like peptide 2
|
iGluR
|
Neurological Disease
Metabolic Disease
|
|
YHIEPV (rALP-2, Rubisco anxiolytic-like peptide 2) is a potent and orally active peptide. YHIEPV shows anxiolytic effects. YHIEPV increases leptin sensitivity to exert its anti-obesity effects .
|
-
- HY-100641
-
|
Hydroxytolbutamide
|
Potassium Channel
Autophagy
|
Metabolic Disease
Cancer
|
|
4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic .
|
-
- HY-13611
-
|
BN 80915
|
Topoisomerase
|
Cancer
|
|
Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds .
|
-
- HY-106608
-
|
LitOralon
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
Glutaurine containing glutamine and taurine residues is an orally active hormone of the parathyroid. Glutaurine, as a hormone, is isolated from parathyroid gland oxyphil cells. Glutaurine can be used for the research of antiepileptic and anti-amnesia .
|
-
- HY-117609
-
|
|
11β-HSD
|
Neurological Disease
|
|
UE2343 is an orally available, brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. UE2343 is being investigated for the treatment of Alzheimer's disease .
|
-
- HY-141638
-
|
Methyl-IQ
|
Biochemical Assay Reagents
|
Cancer
|
|
Me-IQ (Methyl-IQ), an orally active heterocyclic amine, is carcinogenic and mutagenic. Me-IQ is several hundred-fold more mutagenic in liver than in lung microsomal preparations from uninduced mice and rabbits .
|
-
- HY-119816
-
|
|
NKCC
|
Cardiovascular Disease
|
|
Piretanide is an oral active, relatively safe and effective diuretic. Piretanide has the potential for the research of congestive heart failure with a potential advantage of having potassium-sparing properties. Piretanide can also be used for the research of hypertension [1] [2].
|
-
- HY-10792
-
|
SR-46349
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
|
-
- HY-147642
-
-
- HY-130247
-
|
JAK2/FLT3-IN-1
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
Flonoltinib is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib has anti-cancer activity .
|
-
- HY-120755
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
LY290324 is a potent and orally active leukotriene D4 (LTD4) antagonist. LY290324 reduces LTC4, LTD4 and LTE4 (HY-113465)-induced bronchospasm. LY290324 has the potential for the research of antigen-induced bronchospasm .
|
-
- HY-A0171
-
|
Ba-30803 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Benzoctamine is an orally active and potent psychoactive agent which possesses tranquillizing properties. Benzoctamine increases the turnover rate of catecholamines. Benzoctamine enhances the [3H]noradrenaline uptake in the rat heart. Benzoctamine also accelerated the disappearance of intracisternally injected [3H]noradrenaline .
|
-
- HY-108024A
-
|
KAF156 hydrochloride; GNF156 hydrochloride
|
Parasite
|
Infection
|
|
Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite .
|
-
- HY-19631B
-
|
NS-018 hydrochloride
|
JAK
|
Cancer
|
|
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-113603
-
|
SPR001; LY2371712
|
CRFR
|
Cancer
|
|
Tildacerfont is a potent and orally active corticotrophin-releasing factor type 1 (CRF1) receptort antagonis. Tildacerfont effectively reduces adrenocorticotropic hormone (ACTH) and adrenal androgen levels. Tildacerfont has favourable safety profile. Tildacerfont can be used for researching congenital adrenal hyperplasia .
|
-
- HY-19631A
-
|
NS-018
|
JAK
|
Cancer
|
|
Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-122856
-
|
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-115920
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 8 (compound 13) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 8 expresses activity on COX-2 enzyme more than COX-1 with an IC50 of 0.09 nM. Anti-inflammatory agent 8 is orally active .
|
-
- HY-19631
-
|
NS-018 maleate
|
JAK
|
Cancer
|
|
Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-139485
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
BMS-986224 is a potent, selective and orally active APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr 1) apelin-13. BMS-986224 has the potential for the research of heart failure .
|
-
- HY-135825
-
|
|
Autophagy
|
Neurological Disease
|
|
TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment .
|
-
- HY-106268A
-
|
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Larazotide acetate is a peptide which is an orally active zonulin antagonist. Larazotide acetate shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide acetate can be used for the research of celiac disease and infection.
|
-
- HY-130247C
-
|
JAK2/FLT3-IN-1 sulfate
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib maleate has anti-cancer activity .
|
-
- HY-B0249R
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
Didanosine (Standard) is the analytical standard of Didanosine. This product is intended for research and analytical applications. Didanosine (2',3'-Dideoxyinosine; ddI) is a a potent and orally active dideoxynucleoside analogue, and also is a potent nucleoside reverse transcriptase inhibitor. Didanosine shows antiretroviral activity for HIV .
|
-
- HY-123449
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
MK-761 free base is a potent and orally active β2-adrenergic blocker. MK-761 free base shows antihypertensive and positive inotropic effects. MK-761 free base shows vasodilating properties .
|
-
- HY-146267
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo .
|
-
- HY-106050
-
|
Wy 18251
|
COX
|
Inflammation/Immunology
Cancer
|
|
Tilomisole (Wy 18251) is a benzimidazothiazole experimental agent with anti-inflammatory activity. Tilomisole causes less agranulocytosis than levamisole, but retains immunomodulating capabilities. Tilomisole is orally active. Tilomisole has the potential for the research of cancer and inflammation .
|
-
- HY-169344
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-31 (compound 13) is a potent and orally active cyclin-dependent kinase 7 (CDK7) inhibitor with a Kd value of 0.18 nM. CDK7-IN-31 shows anticancer activity .
|
-
- HY-112094S
-
|
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
WNK-IN-11-d3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11-d3 is effective at regulating cardiovascular homeostasis[1].
|
-
- HY-111145
-
|
|
Androgen Receptor
|
Cancer
|
|
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .
|
-
- HY-W010144
-
|
|
COX
Lipoxygenase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat . Phenidone is used as a photographic developer .
|
-
- HY-136704
-
|
|
Glutaminase
|
Cancer
|
|
GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC50 of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC50 of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI50 of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics .
|
-
- HY-146662
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity .
|
-
- HY-157838
-
|
|
MAP4K
|
Cancer
|
|
HMC-B17 is a selective, orally bioavailable HPK1 inhibitor (IC50 = 1.39 nM) that potentiates anti-PD-L1 efficacy. HMC-B17 potently enhances the IL-2 secretion in Jurkat cells (EC50 = 11.56 nM). HMC-B17 can be used for the research of cancer .
|
-
- HY-170369
-
|
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
SHO1122147 (Compound 7m) affects the mitochondrial electron transport chain, exhibits mitochondrial uncoupling activity (EC50=3.6 μM), and increases the oxygen consumption rate (OCR=69%) and promotes cellular respiration. SHO1122147 is orally active, and can be used in reaearch of obesity and metabolic dysfunction-associated steatohepatitis (MASH) .
|
-
- HY-124403
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10 -7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer .
|
-
- HY-141496
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity .
|
-
- HY-105286
-
|
|
11β-HSD
|
Metabolic Disease
|
|
BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research .
|
-
- HY-110129
-
|
SR-46349 hemifumarate; SR 46349B
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
|
-
- HY-152074
-
|
|
CD73
|
Cancer
|
|
D73-IN-14 is a potent, selective and orally active CD73 inhibitor with an IC50 value of 0.17 nM. CD73-IN-14 increases the number of tumor-infiltrating CD8 + cells and shows anti-tumor activity . CD73-IN-14 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-169986S
-
|
|
JAK
|
Inflammation/Immunology
|
|
TyK2-IN-21-d3 (Compound 3c) is the orally active prodrug of the tyrosine kinase 2. TyK2-IN-21-d3 exhibits good chemical stability in aqueous system under different pHs. TyK2-IN-21-d3 alleviates the effect of gastric acid changes on drug absorption and improve the drug bioavailability in rat model .
|
-
- HY-18039
-
|
SEN15924
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
WAY-361789 (SEN15924) is an orally active agonist for α7 nicotinic acetylcholine receptor (α7 nAChR) with an EC50 of 0.18 μM. WAY-361789 improves the cognitive function, exhibits potential in ameliorating Alzheimer’s Disease and schizophrenia .
|
-
- HY-147567
-
|
|
ATM/ATR
DNA-PK
PI3K
|
Cancer
|
|
ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively .
|
-
- HY-B1355R
-
|
|
Bacterial
COX
|
Infection
Inflammation/Immunology
|
|
Oxyphenbutazone (monohydrate) (Standard) is the analytical standard of Oxyphenbutazone (monohydrate). This product is intended for research and analytical applications. Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis .
|
-
- HY-12933
-
|
|
HSP
|
Cancer
|
|
BIIB-028 is an orally active inhibitor for heat shock protein 90 (Hsp90). BIIB-028 targets the ATP-binding site of Hsp90, disrupts the function of Hsp90, leads to the degradation of client proteins, that are crucial for cancer cell survival and proliferation .
|
-
- HY-103595
-
|
Mepirizole; DA-398
|
Others
|
Inflammation/Immunology
|
|
Epirizole (Mepirizole) is an orally active NSAID (nonsteroidal anti-inflammatory agent). Epirizole shows anti-inflammatory activity, and can be used in chronic rheumatoid arthritis research .
|
-
- HY-19263
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor .
|
-
- HY-10527C
-
|
Bay 57-9352 mesylate
|
VEGFR
PDGFR
c-Kit
|
Cancer
|
|
Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively .
|
-
- HY-113841
-
|
|
Others
|
Cardiovascular Disease
|
|
RS-87337 is an orally active antiarrhythmic agent that increases the duration and the maximum rate of rise of cardiac muscle action potentials. RS-87337 is promising for research of antiarrhythmic and cardioprotective agents .
|
-
- HY-10309
-
|
RO 48-3657
|
Integrin
|
Cardiovascular Disease
|
|
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-proagent of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation .
|
-
- HY-P5971A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
TCMCB07 TFA, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia .
|
-
- HY-112939
-
|
MCI-196; Colestimide
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Colestilan (MCI-196) is a non-absorbed, non-calcium-based phosphate binder and is also a non-metallic, anion exchange resin. Colestilan is orally active and can be used for hypercholesterolaemia research .
|
-
- HY-W326094
-
|
GOE 1734; PD 104 208; NSC 328786
|
DNA/RNA Synthesis
|
Cancer
|
|
Dinaline (GOE 1734; PD 104 208; NSC 328786) is a potent and orally activity anticancer agent. Dinaline shows cytotoxicity and antitumor activity. Dinaline has the potential for the research of colorectal cancer .
|
-
- HY-156628
-
|
MK-5684; ODM-208
|
Cytochrome P450
|
Cancer
|
|
Opevesostat (MK-5684; ODM-208) is an orally active and selective CYP11A1 inhibitor. Opevesostat has the potential for the research of metastatic castration-resistant prostate cancer (mCRPC) .
|
-
- HY-148676
-
|
Menin-MLL inhibitor 26
|
Epigenetic Reader Domain
|
Cancer
|
|
Emilumenib (Menin-MLL inhibitor 26) is an orally active Menin-MLL inhibitor. Emilumenib also is an active reference. Emilumenib can inhibits cell growth. Emilumenib can be used for the research of leukemia .
|
-
- HY-161983
-
|
|
Influenza Virus
|
Infection
|
|
Neuraminidase-IN-22 (compound 3e) is a potent, selective and orally active neuraminidase inhibitor with an IC50 value of 0.03 µM. Neuraminidase shows cytotoxicity and anti-influenza A virus activity .
|
-
- HY-150545
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC50 of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro .
|
-
- HY-107798
-
|
|
Bacterial
|
Infection
|
|
Potassium guaiacolsulfonate hemihydrate is an orally active expectorant used for acute respiratory tract infections. Potassium guaiacolsulfonate hemihydrate helps loosen mucus and used for a cough caused by the common cold, infections or allergies in combination with other agents .
|
-
- HY-125415
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA) .
|
-
- HY-134885
-
|
RM-023
|
SHP2
Ras
|
Cancer
|
|
RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction .
|
-
- HY-101116
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM .
|
-
- HY-W011787
-
|
N,N′-Diphenyl-p-phenylenediamine
|
Reactive Oxygen Species
|
Metabolic Disease
|
|
DPPD (N,N′-Diphenyl-p-phenylenediamine) is an orally active polymerization inhibitor and antioxidant with antioxidative activity. DPPD causes reproductive/developmental toxicity in rats. DPPD is widely used in rubber, oils, and feedstuffs, especially for tires in the rubber industry .
|
-
- HY-119057
-
|
|
Parasite
|
Infection
|
|
DSM74 (compound 21) is an orally active and potent antimalarial inhibitor of PfDHODH (IC50=0.28 μM) and PbDHODH (IC50=0.38 μM). DSM74 inhibits the growth of Plasmodium in animals .
|
-
- HY-106818A
-
|
AJ-2615
|
Acyltransferase
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
Monatepil maleate (AJ-2615) is a potent and orally active Ca 2+-channel antagonist and a noncompetitive ACAT inhibitor. Monatepil maleate decreases blood pressure and improves plasma lipid metabolism. Monatepil maleate has the potential for the research of hyperlipidemia .
|
-
- HY-128442
-
|
Phenyl hydrogen sulfate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phenyl sulfate is an orally active gut microbiota-derived metabolite. Phenyl sulfate induces albuminuria and podocyte damage in experimental models of diabetes. Phenyl sulfate can be used as a disease marker and future therapeutic target in diabetic kidney disease .
|
-
- HY-147263
-
|
CC-11050
|
Phosphodiesterase (PDE)
|
Infection
Inflammation/Immunology
|
|
Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast, as an adjunct, is used for the research of tuberculosis (TB) .
|
-
- HY-103250
-
|
|
Antibiotic
|
Infection
|
|
PF-945863 is an orally active macrolide antibiotic that can be used for the research of multidrug resistant respiratory tract bacterial strains .
|
-
- HY-121097
-
-
- HY-170544
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1-IN-28 (compound 13) is an orally active RIPK1 inhibitor. RIPK1-IN-28 inhibits human I2.1 and Hepa1‐6 cells with IC50s of 0.4 and 1.2 nM, respectively .
|
-
- HY-10262
-
|
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity .
|
-
- HY-162561
-
|
|
Galectin
|
Cancer
|
|
GB1908 is a selective and orally active galectin-1 inhibitor with Ki values of 57 nM and 72 nM for human and mouse galectin-1, respectively. GB1908 displays >50-fold selectivity over galectin-3. GB1908 can be used for the study of lung cancer .
|
-
- HY-130247A
-
|
JAK2/FLT3-IN-1 TFA
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
Flonoltinib TFA is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib TFA has anti-cancer activity .
|
-
- HY-106268
-
|
|
Gap Junction Protein
|
Infection
Inflammation/Immunology
|
|
Larazotideis a peptide which is an orally active zonulin antagonist. Larazotide shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide can be used for the research of celiac disease and infection .
|
-
- HY-100413
-
|
|
Proton Pump
|
Inflammation/Immunology
|
|
CS-526 is a potent, selective, reversible and orally active acid pump antagonist. CS-526 inhibits H +,K +-ATPase activity. CS-526 inhibits gastric acid secretion and prevents esophageal lesions. CS-526 has the potential for the research of gastroesophageal reflux disease .
|
-
- HY-B0024R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Prulifloxacin (Standard) is the analytical standard of Prulifloxacin. This product is intended for research and analytical applications. Prulifloxacin (NM441) is an orally active fluoroquinolone antibiotic with a broad spectrum of activity against Gram-positive and -negative bacteria. Prulifloxacin is a proagent of a thiazeto-quinoline carboxylic acid derivative Ulifloxacin (NM394). Prulifloxacin has the potential for lower urinary tract infections and exacerbations of chronic bronchitis .
|
-
- HY-W020183R
-
|
|
Fungal
Bacterial
|
Neurological Disease
|
|
γ-Terpinene (Standard) is the analytical standard of γ-Terpinene. This product is intended for research and analytical applications. γ-Terpinene, a monoterpene, is an orally active antioxidant compound which can scavenge radicals directly. γ-Terpinene has potent antinociception activity. γ-Terpinene exhibits antimicrobial efficacy against various bacteria and fungi .
|
-
- HY-132981
-
|
|
P2X Receptor
|
Neurological Disease
|
|
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases .
|
-
- HY-122028
-
|
|
11β-HSD
|
Metabolic Disease
|
|
HSD-016 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50 values of 11, 1 and 8 nM against human, mouse and rat 11β-HSD1, respectively. HSD-016 can be used for type 2 diabetes research .
|
-
- HY-A0279
-
|
Pristinamycine
|
Bacterial
Antibiotic
|
Infection
|
|
Pristinamycin, produced by Streptomyces pristinaespiralis, is an orally active streptogramin-like antibiotic consisting of two chemically unrelated components: Pristinamycin I (PI) and Pristinamycin II (PII). Pristinamycin is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus (MRSA), Vancomycin-resistant S. aureus (VRSA) and Enterococcus faecium (VREF) .
|
-
- HY-17643R
-
|
|
Fungal
Cytochrome P450
|
Infection
|
|
Oteseconazole (Standard) is the analytical standard of Oteseconazole. This product is intended for research and analytical applications. Oteseconazole (VT-1161) is a potent and orally active anti-fungal agent. Oteseconazole potently binds to and inhibits Candida albicans cytochrome P45051 (CYP51) activity (Kd ≤39 nM), shows no obvious effect on human CYP51. Oteseconazole also can be used for the research of dermatophytes .
|
-
- HY-14904
-
|
|
SARS-CoV
Influenza Virus
|
Infection
|
|
Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against a number of enveloped and non-enveloped viruses. Umifenovir is used as an anti-influenza virus agent. Umifenovir could effectively inhibit the fusion of virus with host cells . Umifenovir is an efficient inhibitor of SARS-CoV-2 in vitro . Umifenovir shows anti-inflammatory activity .
|
-
- HY-110117
-
|
|
Integrin
Interleukin Related
|
Inflammation/Immunology
|
|
BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1), with a Ki of 25.8 nM. BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders .
|
-
- HY-162661
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
P2Y14R antagonist 2 (compound 39) is a potent, selective and orally active P2Y14R antagonist with an IC50 value of 0.40 nM. P2Y14R antagonist 2 shows anti-inflammatory activity. P2Y14R antagonist 2 has the potential for the research of colitis .
|
-
- HY-146223A
-
|
|
Ras
|
Cancer
|
|
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
- HY-125677
-
|
|
Caspase
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
SHetA2 is a derivative of heteroarotinoid, that exhibits cytotoxicity in cancer cells with IC50 of 0.37–4.6 μM. SHetA2 regulates cancer cells differentiation, induces apoptosis through the intrinsic mitochondrial pathway, and arrest cell cycle at G2 phase. SHetA2 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice. SHetA2 is orally active .
|
-
- HY-B1271R
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Sulfinpyrazone (Standard) is the analytical standard of Sulfinpyrazone. This product is intended for research and analytical applications. Sulfinpyrazone (G-28315) is an orally active and potent uricosuric agent for chronic and intermittent gouty arthritis. Sulfinpyrazone has antithrombotic and platelet inhibitory effects .
|
-
- HY-101918
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases .
|
-
- HY-15127R
-
|
|
RAR/RXR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Isotretinoin (Standard) is the analytical standard of Isotretinoin. This product is intended for research and analytical applications. Isotretinoin (13-cis-Retinoic acid) is an orally active vitamin A derivative and is often be used for the research of severe acne. Isotretinoin also shows anticancer activity .
|
-
- HY-108060A
-
|
NM283 dihydrochloride
|
HCV
HCV Protease
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable proagent of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination .
|
-
- HY-145721A
-
|
GED-0301 sodium
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Mongersen sodium is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen sodium restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen sodium can attenuate Crohn's disease-like experimental colitis in mice .
|
-
- HY-108060
-
-
- HY-15155
-
MLN0905
4 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC50 value of 2 nM. MLN0905 can be used for the research of cancer .
|
-
- HY-164307
-
|
BLU 451; LNG-451
|
EGFR
|
Cancer
|
|
Pebezertinib (BLU 451) is an orally active inhibitor for EGFR. Pebezertinib exhibits the ability to penetrate the central nervous system (CNS). Pebezertinib can be used for research about non-small cell lung cancer carrying EGFR exon 20 insertion .
|
-
- HY-135615A
-
|
N-Desmethylsibutramine hydrochloride
|
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
|
Desmethyl Sibutramine hydrochloride, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine hydrochloride can be used in the research of obesity and appetite suppressant .
|
-
- HY-17479BS
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Amfenac-d5 sodium is deuterated-labeled Amfenac sodium. Amfenac Sodium is an orally active and potent anti-inflammatory compound possessing antipyretic and analgesic properties. Amfenac Sodium can be used for the research of acute and chronic inflammation .
|
-
- HY-145919
-
-
- HY-106083
-
|
RHC 3988
|
Others
|
Inflammation/Immunology
|
|
Quazolast (RHC 3988) is a orally active mast cell stabilizer. Quazolast also is a potent mediator release inhibitor. Quazolast reduces the gastric damage. Quazolast has the potential for the research of gastric ulcers .
|
-
- HY-105033
-
|
Pirfloxacin
|
Bacterial
|
Infection
|
|
Irloxacin (Pirfloxacin) is a quinolone antibacterial agent. Irloxacin shows greater activity with an acid pH. Irloxacin has a good in vitro antimicrobial spectrum against both gram-positive and gram-negative bacteria. Orally active .
|
-
- HY-17479S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Amfenac-d5 is the deuterium labeled Amfenac. Amfenac is an orally active and potent anti-inflammatory compound possessing antipyretic and analgesic properties. Amfenac can be used for the research of acute and chronic inflammation .
|
-
- HY-14771
-
-
- HY-135615
-
|
N-Desmethylsibutramine
|
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
|
Desmethyl Sibutramine, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine can be used in the research of obesity and appetite suppressant .
|
-
- HY-151196
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki of 0.17 nM. FXIa-IN-10 has good oral bioavailability .
|
-
- HY-117610
-
|
Ro 32-0432 free base; Bisindolylmaleimide XI
|
PKC
|
Inflammation/Immunology
|
|
Ro 31-8830 is an orally active, potent and selective inhibitor of protein kinase C with anti-inflammatory activity. Ro 31-8830 is promising for research of inflammatory disorders .
|
-
- HY-100087
-
-
- HY-152104
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4 WT, FGFR3, FGFR4 V550L, FGFR2 and FGFR1, respectively .
|
-
- HY-19490A
-
|
(S)-AQW-051
|
nAChR
|
Neurological Disease
|
|
(S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia .
|
-
- HY-172147
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
|
-
- HY-14240
-
|
PG 530742; PGE 530742; PGE 7113313
|
MMP
|
Inflammation/Immunology
|
|
PG 116800 (PG 530742) is an orally avtive MMP inhibitor. PG 116800 has high affinity for MMP-2, -3, -8, -9, -13, and -14, while having substantially lower affinity for MMP-1 and -7. PG 116800 can be used for knee osteoarthritis research .
|
-
- HY-15658
-
GSK2801
2 Publications Verification
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4 .
|
-
- HY-19569R
-
|
ABT-494 (Standard)
|
JAK
|
Inflammation/Immunology
|
|
Upadacitinib (Standard) is the analytical standard of Upadacitinib. This product is intended for research and analytical applications. Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research .
|
-
- HY-14687
-
|
(rac)-BMN-673; (rac)-LT-673
|
PARP
|
Cancer
|
|
(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is the orally active inhibitor for PARP1/2 with Ki of 1.2 nM and 0.87 nM. (rac)-Talazoparib inhibits cellular PARylation with an EC50 of 2.51 nM. (rac)-Talazoparib causes the accumulation of DNA damage, inhibits proliferation of BRCA1/2-mutated MX-1 cell and Capan-1 cell with IC50 of 0.3 nM and 5 nM. (rac)-Talazoparib exhibits antitumor efficacy in mouse models .
|
-
- HY-149695
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
|
-
- HY-111669
-
CT1812
1 Publications Verification
Sigma-2 receptor antagonist 1
|
Sigma Receptor
|
Neurological Disease
|
|
CT1812 (Sigma-2 receptor antagonist 1) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. CT1812 can be used for the research of Alzheimer’s disease .
|
-
- HY-101699A
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice .
|
-
- HY-109083
-
|
GS-9674
|
FXR
Autophagy
|
Inflammation/Immunology
|
|
Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research .
|
-
- HY-117610A
-
|
Ro 32-0432; Ro 31-8830 hydrochloride
|
PKC
|
Inflammation/Immunology
|
|
Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively .
|
-
- HY-B0298
-
|
HS-592; Meclastine
|
Histamine Receptor
|
Neurological Disease
|
|
Clemastine (HS-592) is a potent and orally active histamine receptor H1 antagonist. Clemastine is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
|
-
- HY-117623
-
|
PF-249
|
AMPK
|
Metabolic Disease
|
|
PF-06685249 (PF-249) is a potent and orally active allosteric AMPK activator with an EC50 of 12 nM for recombinant AMPK α1β1γ1. PF-06685249 can be used for diabetic nephropathy research .
|
-
- HY-106735
-
|
Ro 13-6298; Arotinoid ethyl ester
|
RAR/RXR
|
Inflammation/Immunology
Cancer
|
|
Arotinoid (RO 13-6298) is a retinoid, and acts as an orally active and highly potent agonist of retinoic acid receptors (RARs) with antipsoriatic effects. Arotinoid has antipapiltoma activity with an ED50 of 0.05 mg/kg. Arotinoid can be used for the research of skin carcinomas .
|
-
- HY-170647
-
|
|
Ras
|
Cancer
|
|
SEPT9-IN-1 (compound 8b) is a SEPT9 inhibitor with an IC50 value of 94.83 μM. SEPT9-IN-1 shows cytotoxicity to human oral squamous carcinomas with an IC50 value of 21 µM .
|
-
- HY-19688A
-
|
WR 6026 hydrochloride
|
Parasite
Mitochondrial Metabolism
|
Infection
|
|
Sitamaquine (WR6026) hydrochloride, an orally active 8-aminoquinoline analog, is an antileishmanial agent. Sitamaquine hydrochloride inhibits mitochondrial complex II (succinate dehydrogenase). Sitamaquine hydrochloride is a lipophilic weak base that rapidly accumulates in acidic compartments of Leishmania spp., mainly in acidocalcisomes .
|
-
- HY-161107
-
|
|
GPR84
|
Inflammation/Immunology
|
|
OX04529 (compound 69) is a potent, selective and orally active agonist of GPR84. OX04529 inhibits FSK-induced cAMP production with an EC50 of 0.0185 nM. OX04529 displayed excellent potency, high G-protein signaling bias .
|
-
- HY-W013172
-
|
|
Progesterone Receptor
|
Endocrinology
|
|
Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive . Norgestimate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-151881
-
|
|
Ras
|
Cancer
|
|
SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer .
|
-
- HY-106993B
-
|
GT-2331 (enantiomer)
|
Histamine Receptor
|
Neurological Disease
|
|
Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant (HY-106993), Cipralisant is an orally active, potent, selective, and high affinity histamine H3 receptor antagonist (rat Ki=0.47 nM) . Cipralisant (enantiomer) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-168927
-
|
|
Apoptosis
Pyroptosis
|
Cancer
|
|
Apoptosis inducer 36 (Compound 42) exhibits anti-leukemic activity through reduction of leukemia stem cells (LSCs) and induction of differentiation. Apoptosis inducer 36 inhibits the proliferation of AML cells, arrests cell cycle at G1 phase, and induces PANoptosis including apoptosis, pyroptosis and necrosis. Prodrug of apoptosis inducer 36 exhibits orally active antitumor efficacy in mouse model .
|
-
- HY-10322
-
|
BIBX 1382
|
EGFR
|
Cancer
|
|
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity .
|
-
- HY-18010
-
|
|
Btk
BCRP
|
Inflammation/Immunology
|
|
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .
|
-
- HY-B0464A
-
|
|
Reactive Oxygen Species
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Hydralazine is a orally active antihypertensive agent, reduces peripheral resistance directly by relaxing the smooth muscle cell layer in arterial vessel. Hydralazine has antioxidant activity, as well as inhibits reactive oxygen species (ROS) release and O2 ·- generation with an IC50 value of 9.53 mM and 1.19 mM, respectively .
|
-
- HY-12776
-
GSK805
4 Publications Verification
|
ROR
|
Inflammation/Immunology
|
|
GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity .
|
-
- HY-B1196R
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Tiapride (hydrochloride) (Standard) is the analytical standard of Tiapride (hydrochloride). This product is intended for research and analytical applications. Tiapride hydrochloride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride hydrochloride shows anti-dyskinetic activity and anxiolytic activity. Tiapride hydrochloride is a neuroleptic agent .
|
-
- HY-13215
-
|
CI-1011; PD-148515
|
Acyltransferase
|
Cancer
|
|
Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively . Avasimibe can be used for the research of prostate cancer .
|
-
- HY-N7697F
-
|
|
Others
|
Others
|
|
Chitobiose, a chitosan oligosaccharide, is a dimer of β-1,4-linked glucosamine units . Chitobiose has orally activity and high antioxidant activity .
|
-
- HY-145564A
-
|
PF-07265803 hydrochloride
|
p38 MAPK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Emprumapimod (PF-07265803) hydrochloride is an orally active and selective inhibitor of p38α MAPK. Emprumapimod hydrochloride can be used for the research of dilated cardiomyopathy and acute inflammatory pain .
|
-
- HY-121450
-
|
Loxtidine; AH-234844
|
Histamine Receptor
|
Cancer
|
|
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia .
|
-
- HY-14578
-
-
- HY-107354
-
|
|
Drug Derivative
|
Cardiovascular Disease
|
|
Gepefrine is an orally active pressor agent and sympathomimetic agent. Gepefrine improves the early orthostatic disregulation of the arterial pressure .
|
-
- HY-115506
-
|
|
TRP Channel
|
Neurological Disease
|
|
PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain .
|
-
- HY-103345
-
-
- HY-106645
-
-
- HY-15879
-
-
- HY-141700
-
|
|
FATP
|
Metabolic Disease
|
|
FATP1-IN-2 (compound 12a), an arylpiperazine derivative, is an orally active fatty acid transport protein 1 (FATP1) inhibitor (human IC50=0.43 μM, mouse IC50=0.39 μM) .
|
-
- HY-109177
-
|
QBW251
|
CFTR
|
Inflammation/Immunology
|
|
Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research .
|
-
- HY-162118
-
|
|
Vasopressin Receptor
|
Neurological Disease
|
|
RGH-122 (compound 43) is an orally active, potent, selective, and hV1a receptor antagonist with Ki value of 0.3 nM and IC50 of 0.9 nM. RGH-122 showes microsomal stability with CLint value of 13/28/25 μL/min/mg .
|
-
- HY-19141
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
L-691121 exhibits antiarrhythmic efficacy through block of potassium channel and a followed prolonged cardiac potential. L-691121 exhibits embryotoxicity with fetal mortality at the dose of 0.8 mg/kg/day (p.o.). L-691121 is orally active .
|
-
- HY-13512
-
|
Camostat mesilate; FOY305; FOY-S980
|
Ser/Thr Protease
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase .
|
-
- HY-109075
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Tasipimidine is an orally active and selective α2A-adrenoceptor agonist with a pEC50 of 7.57 for human α2A-adrenoceptors. Tasipimidine can be utilized in research related to situational anxiety and fear .
|
-
- HY-17491
-
|
RU 43-715; Sandoz-43-715
|
Others
|
Inflammation/Immunology
|
|
Proquazone (RU 43-715) is a chemically distinctive non-steroidal anti-inflammatory agent (NSAID). unlike most other NSAIDs, Proquazone does not have a free acid group in its structure. Proquazone may inhibit or arrest progression of bone erosions. Proquazone is an orally active anti-inflammatory, analgesic and anti-pyretic agent .
|
-
- HY-102051
-
|
|
IAP
|
Cancer
|
|
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo .
|
-
- HY-19838
-
|
|
GPR139
|
Neurological Disease
|
|
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB) .
|
-
- HY-18204A
-
|
LCZ696
|
Angiotensin Receptor
Neprilysin
Apoptosis
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Sacubitril/Valsartan (LCZ696), comprised Valsartan and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure . Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis .
|
-
- HY-132292
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .
|
-
- HY-151111
-
|
|
Renin
|
Cardiovascular Disease
|
|
SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research .
|
-
- HY-150963
-
|
|
Renin
|
Cardiovascular Disease
|
|
Renin inhibitor-1 (compound 26) is a potent and orally active renin inhibitor with IC50s of 0.9, 1.8 nM for rh-renin and hPRA, respectively. Renin inhibitor-1 shows antihypertensive efficacy. Renin inhibitor-1 has the potential for the research of hypertension and cardiovascular/renal diseases .
|
-
- HY-118189S
-
|
|
Isotope-Labeled Compounds
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Misoprostol acid-d5 is deuterium labeled Misoprostol acid. Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers[1]. Misoprostol is an oral agent used to induce labor[2].
|
-
- HY-106647
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
Abacavir hydroxyacetate is an orally active inhibitor of IL-20 and PRINS. Abacavir hydroxyacetate reduces proliferation rate of skin in psoriasis as an immune modulator. Abacavir hydroxyacetate can be used for the research of inflammatory skin problems .
|
-
- HY-163590
-
-
- HY-122083
-
|
|
PPAR
|
Metabolic Disease
|
|
T2384 is a peroxisome proliferator-activated receptor γ (PPARγ) ligand. T2384 also is an orally active antidiabetic agent. T2384 reduces the fasting plasma glucose levels and plasma insulin levels .
|
-
- HY-153168
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Bemoradan (compound 10a) is an orally active and selective canine Phosphodiesterase (PDE) fraction III inhibitor. Bemoradan is a long-acting, potent, inotropic vasodilator and a novel cardiotonic agent, and can be used in congestive heart
failure research .
|
-
- HY-B1461
-
|
|
Tyrosinase
Apoptosis
|
Cancer
|
|
Deoxyarbutin is an orally active tyrosinase inhibitor that can promote apoptosis of melanoma cells, enhance the vitality of mouse acinar cells, and has skin whitening and anti-tumor activity [1][2][3].
|
-
- HY-152156
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis .
|
-
- HY-144676
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC50 values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities .
|
-
- HY-144677
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities .
|
-
- HY-B1751R
-
|
|
Potassium Channel
Cytochrome P450
Apoptosis
Parasite
|
Infection
Cardiovascular Disease
Cancer
|
|
Quinidine (15% dihydroquinidine) (Standard) is the analytical standard of Quinidine (15% dihydroquinidine). This product is intended for research and analytical applications. Quinidine (15% dihydroquinidine) is an antiarrhythmic agent. Quinidine is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine can be used for malaria research .
|
-
- HY-B0452R
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Ritodrine (hydrochloride) (Standard) is the analytical standard of Ritodrine (hydrochloride). This product is intended for research and analytical applications. Ritodrine (DU21220) hydrochloride is a potent and orally active β-adrenergic agonist. Ritodrine hydrochloride decreases preterm delivery and uterine contraction. Ritodrine hydrochloride has the potential for the research of preterm labor .
|
-
- HY-15546
-
|
|
CCR
|
Inflammation/Immunology
|
|
BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis .
|
-
- HY-N2059
-
|
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Santalol is a mixture of α and β-isomer santalol. α-Santalol is found in sandalwood oil. α-Santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer. Santalol has sedative activity .
|
-
- HY-151485
-
|
|
Parasite
|
Infection
|
|
Anti-infective agent 5 (compound 74) is an orally active inhibitor of Trypanosoma cruzi with an IC50 value of 0.10 μM. Anti-infective agent 5 effectively reduces parasite burden in vivo. Anti-infective agent 5 can be used for the research of infection .
|
-
- HY-100606
-
|
(-)-Pindolol; (S)-(-)-Pindolol; S-Pindolol
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
l-Pindolol ((-)-pindolol) is a reversible, competitive and orally active 5-HT1A/1B antagonist. l-Pindolol is a partial β-adrenoceptor agonist. l-Pindolol can be used for the research of neurological disease .
|
-
- HY-145721
-
|
GED-0301
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice .
|
-
- HY-15043
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
|
-
- HY-106608A
-
|
LitOralon TFA
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
Glutaurine (Litoralon) TFA containing glutamine and taurine residues is an orally active hormone of the parathyroid. Glutaurine (Litoralon) TFA, as a hormone, is isolated from parathyroid gland oxyphil cells. Glutaurine (Litoralon) TFA can be used for the research of antiepileptic and anti-amnesia .
|
-
- HY-109176
-
|
GDC-9545; RG6171
|
Estrogen Receptor/ERR
|
Cancer
|
|
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity .
|
-
- HY-121132
-
-
- HY-N8435
-
-
- HY-10563
-
|
MCI-9042 free acid
|
5-HT Receptor
|
Infection
|
|
Sarpogrelate (MCI-9042) is a new, specific orally active 5-HT2 receptor antagonist, Sarpogrelate increases platelet aggregation and has hemostasis effect, and can be used for the research of Buerger’s disease .
|
-
- HY-115494
-
|
Neladenoson bialanate hydrochloride; BAY-1067197 hydrochloride
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases .
|
-
- HY-148074
-
|
RPT193
|
CCR
|
Inflammation/Immunology
|
|
Zelnecirnon (RPT193) is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. Zelnecirnon can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research .
|
-
- HY-123353
-
|
Neladenoson bialanate; BAY-1067197
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases .
|
-
- HY-170573
-
|
|
Monoamine Oxidase
|
Cancer
|
|
LOX-IN-5 (compound 22) is a selective and orally active lysyl oxidase-like 2 (LOXL2) inhibitor with an IC50 of <300 nM. LOX-IN-5 possess anti-fibrosis properties .
|
-
- HY-N0586A
-
|
(+)-Laurelliptine hydrochloride
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis .
|
-
- HY-169857
-
|
|
RANKL/RANK
|
Others
|
|
AS2690168 freebase is an orally active RANKL signal transduction inhibitor which suppresses RANKL-induced osteoclastogenesis of RAW264 cells. AS2690168 can be utilized in research related to pathological osteolysis .
|
-
- HY-170573A
-
|
|
Monoamine Oxidase
|
Cancer
|
|
LOX-IN-5 tosylate (compound 22) is a selective and orally active lysyl oxidase-like 2 (LOXL2) inhibitor with an IC50 of <300 nM. LOX-IN-5 tosylate possess anti-fibrosis properties .
|
-
- HY-117630
-
|
|
Drug Intermediate
|
Cancer
|
|
RB-6145 is an orally active pro-drug of the hypoxic cell radiosensitizer RSU 1069. RB-6145 acts a hypoxic cell radiosensitizer and cytotoxin but reduces systemic toxicity in mice .
|
-
- HY-169857A
-
|
|
RANKL/RANK
|
Others
|
|
AS2690168 hydrochloride is an orally active RANKL signal transduction inhibitor which suppresses RANKL-induced osteoclastogenesis of RAW264 cells. AS2690168 can be utilized in research related to pathological osteolysis .
|
-
- HY-121203
-
|
|
Serotonin Transporter
|
Neurological Disease
Cancer
|
|
Citalopram is a racemate mixture of the active S(+)-enantiomer (Escitalopram; HY-14258) and R(-)-enantiomer. Citalopram is an orally active selective serotonin reuptake inhibitor (SSRI). Citalopram is an antidepressant and enhances serotoninergic neurotransmission .
|
-
- HY-168887
-
|
|
STING
|
Cancer
|
|
ZSA-51 is a potent and orally active STING agonist. ZSA-51 shows anticancer activity. ZSA-51 remodeles immune microenvironment both in tumor and lymph node .
|
-
- HY-113745
-
|
|
Amino acid Transporter
|
Neurological Disease
|
|
LX-6171 is an orally active SLC6A7 inhibitor. LX-6171 can be used to study diseases characterized by cognitive impairment, such as Alzheimer's disease, schizophrenia or vascular dementia .
|
-
- HY-B0326
-
|
|
Others
|
Endocrinology
|
|
Alibendol can be taken orally. It has anti-spasmodic properties and promotes bile secretion, making it useful for research on digestive system issues like indigestion, nausea, vomiting, and constipation .
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-
- HY-N0586
-
|
(+)-Laurelliptine
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
Norisoboldine is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis .
|
-
- HY-19934
-
|
TAS-117
|
Akt
Apoptosis
Autophagy
|
Cancer
|
|
Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy .
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-
- HY-19934A
-
|
TAS-117 hydrochloride
|
Akt
Apoptosis
Autophagy
|
Cancer
|
|
Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy .
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-
- HY-18662
-
|
|
TRP Channel
|
Neurological Disease
Cancer
|
|
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels .
|
-
- HY-14336
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity .
|
-
- HY-141523
-
|
RMC-4630; SHP2-IN-7
|
SHP2
Phosphatase
|
Cancer
|
|
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .
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-
- HY-163736
-
|
|
Lipoxygenase
PGE synthase
|
Inflammation/Immunology
|
|
mPGES-1/5-LOX-IN-1 (compound 3j) is a potent and orally active mPGES-1 and 5-LOX dual inhibitor with IC50 values of 0.92, 1.89 µM, respectively. mPGES-1/5-LOX-IN-1 shows anti-inflammatory impact .
|
-
- HY-112666
-
|
FTS amide; Salirasib amide
|
Ras
|
Cancer
|
|
Farnesyl thiosalicylic acid amide (FTS-A) is an orally active derivative of farnesyl thiosalicylic acid (HY-14754). Farnesyl thiosalicylic acid amide reduces Ras-GTP levels and inhibits cell growth with IC50s of 20 and 10 μM for Panc-1 and U87 cells, respectively. Farnesyl thiosalicylic acid amide can be used for the research of cancer .
|
-
- HY-130247B
-
|
JAK2/FLT3-IN-1 monomaleate
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity .
|
-
- HY-160514
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LXQ46 is an orally active inhibitor for protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 0.190 μM. LXQ46 enhances insulin and leptin signaling pathways in insulin-resistant C2C12. LXQ46 ameliorates type 2 diabetes and increases insulin tolerance in mouse models .
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-
- HY-B0281AR
-
|
|
Histamine Receptor
Cytochrome P450
Bacterial
|
Infection
Metabolic Disease
Endocrinology
Cancer
|
|
Ranitidine (hydrochloride) (Standard) is the analytical standard of Ranitidine (hydrochloride). This product is intended for research and analytical applications. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9 .
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-
- HY-153701
-
|
|
JAK
|
Cancer
|
|
JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=17.2 nM) .
|
-
- HY-119402
-
|
BCL6-IN-8c
|
Bcl-2 Family
|
Cancer
|
|
TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay .
|
-
- HY-103416
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pKi=7.40; Ki=39.8 nM) with antiparkinsonian activity. A-77636 hydrochloride is functionally inactive at dopamine D2 receptor .
|
-
- HY-12413A
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC50 of 0.07 µM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models .
|
-
- HY-134772
-
|
|
STAT
Cytochrome P450
|
Inflammation/Immunology
|
|
AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research .
|
-
- HY-151140
-
|
|
Cytochrome P450
|
Others
|
|
CYP11B1-IN-2 (compound 7aa) is an orally active, potent and selective CYP11B1 inhibitor, with IC50 values of 9 nM and 25 nM for human CYP11B1 and rat CYP11B1, respectively. CYP11B1-IN-2 can be used for the research of diseases caused by excessive cortisol .
|
-
- HY-14904AR
-
|
|
Influenza Virus
SARS-CoV
|
Infection
|
|
Umifenovir (hydrochloride) (Standard) is the analytical standard of Umifenovir (hydrochloride). This product is intended for research and analytical applications. Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells . Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity .
|
-
- HY-133829
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Zofenoprilat is an orally active inhibitor for angiotensin converting enzyme (ACE) with an IC50 of 1.7 nM. Zofenoprilat inhibits the expression of angiotensin II, reduces the blood pressure, exhibits thus cardioprotective and renalprotective activity. Zofenoprilat promotes the NO production, decreases endothelin-1 (ET-1) expression, exhibits protective effect on vascular endothelial function. Zofenoprilat regulates oxidative stress-related molecules, exhibits antioxidant activity .
|
-
- HY-W931056
-
|
|
TRP Channel
|
Neurological Disease
|
|
AMG-628 is an orally active inhibitor for TRPV1, that inhibits Capsaicin (HY-10448) or acid (pH 5)-induced Ca 2+ influx into TRPV1- expressing CHO cell with IC50 of 4.9 and 3.1 nM. AMG-628 exhibits analgesic activity in Capsaicin (HY-10448)-induced rat model, and exhibits a half-life of 2.4 h in rats .
|
-
- HY-162754
-
|
|
Proteasome
|
Inflammation/Immunology
|
|
LMP7/LMP2-IN-1 (Compound 19) is the orally active inhibitor for immunoproteasome subunits LMP7 and LMP2 with IC50 of 257 and 10 nM. LMP7/LMP2-IN-1 reduces the generation of antibody, downregulates the cells in spleen germinal center B and in plasma in NP-OVA-immunized mice, and can be used in research about autoimmune diseases .
|
-
- HY-129716
-
|
|
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
L-693989 is an orally active water-soluble lipopeptide with anticandidal and antipneumocystis activity. L-693989 is effective in preventing the development of both P. carinii cysts. L-693989 is promising for research of P. carinii pneumonia .
|
-
- HY-163149
-
|
|
HBV
|
Infection
|
|
AB-452, a Dihydroquinolizinone (DHQ) analogue, is a potent and orally active HBV RNA destabilizer. AB-452 inhibits PAPD5/7 proteins in vitro with good in vivo efficacy in a chronic HBV mouse model .
|
-
- HY-119658
-
|
INCB10820
|
CCR
|
Inflammation/Immunology
|
|
PF-4178903 (INCB10820) is an orally active, potent dual CCR2 and CCR5 antagonist with IC50 values of 3 nM and 5.3 nM, respectively. PF-4178903 is promising for research of chronic inflammatory and autoimmune diseases .
|
-
- HY-17610
-
|
TS-091
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
|
-
- HY-P5558
-
|
|
VEGFR
|
Inflammation/Immunology
|
|
KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF. KLTWQELYQLKYKGI is active in gastric ulcer healing in rodents when administered either orally or systemically. KLTWQELYQLKYKGI shows the ability to induce capillary formation and organization in vitro .
|
-
- HY-132295
-
|
ZN-c3
|
Wee1
|
Cancer
|
|
Azenosertib (ZN-c3) is a selective, orally active inhibitor for Wee1 inhibitor (IC50=3.9 nM). Azenosertib exhibits antitumor activity .
|
-
- HY-113864
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
Diisobutyl carbinol (DIBC) is an orally active organic solvent widely used as industrial intermediates and fragrance ingredient. Diisobutyl carbinol and Diisobutyl ketone are well interconverted metabolically in rats .
|
-
- HY-100919
-
|
WIN 8077 chloride
|
Cholinesterase (ChE)
|
Others
|
|
Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium chloride inhibits human AChE with an IC50 value of 0.7 nM (hAChE) .
|
-
- HY-120669
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
PF-06761281 (Compound 4a) is a potent, orally active, partial selective sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor with IC50 values of 0.51, 13.2 and 14.1 μM against HEKNaCT, HEKNaDC1 and HEKNaDC3, respectively .
|
-
- HY-141535A
-
|
|
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
IL-17 modulator 1 (disodium) is an orally active, highly efficacious IL-17 modulator extracted from patent WO 2020127685. IL-17 modulator 1 (disodium) can be used for the research of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis .
|
-
- HY-168842
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-47 (compound 20) is a potent, selectively and orally active, MTA cooperative PRMT5 inhibitor with an IC50 value of 15 nM. PRMT5-IN-47 shows antiproliferative activity. PRMT5-IN-47 shows anticancer activity .
|
-
- HY-141514
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide .
|
-
- HY-149989
-
|
|
Ack1
Akt
|
Cancer
|
|
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity .
|
-
- HY-B0758R
-
|
|
Calcium Channel
|
Inflammation/Immunology
|
|
Troxipide (Standard) is the analytical standard of Troxipide. This product is intended for research and analytical applications. Troxipide is an orally active defensive factor-enhancing therapeutic agent for gastritis and gastric ulcer (GU). Troxipide is a non-antisecretory gastro protective agent with antiulcer, anti-inflammatory and mucus-secreting properties .
|
-
- HY-19464
-
|
|
GnRH Receptor
Estrogen Receptor/ERR
|
Endocrinology
|
|
Org 43553 is an orally active and low molecular weight (LMW) luteinizing hormone receptor (LH-R) agonist. Org 43553 shows agonistic activity to human LH and FSH receptors with EC50 values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine .
|
-
- HY-103689
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Cucurbit[8]uril is a potent, low toxicity and orally active supramolecular inducer of protein heterodimerization. Cucurbit[8]uril induces heterodimerization of methylviologen and naphthalene functionalized proteins. Cucurbit[8]uril can induce energy transfer .
|
-
![Cucurbit[8]uril](//file.medchemexpress.com/product_pic/hy-103689.gif)
- HY-101699
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
AMG-076 free base is an orally bioavailable and selective MCHR1 antagonist. AMG-076 free base results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice .
|
-
- HY-134217
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
KYN-101 is a potent, selective and orally active AHR inhibitor. KYN-101 decreases the CYP1A1 mRNA expression. KYN-101 shows anti-cancer activity .
|
-
- HY-113847
-
|
UK-61260-27
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Nanterinone mesylate (UK-61260-27) is an orally active and positive inotropic and balanced-type vasodilating agent, partially based on phosphodiesterase III inhibition with venodilating properties. Nanterinone mesylate is promising for research of cardiovascular diseases .
|
-
- HY-19394
-
|
|
PPAR
|
Metabolic Disease
|
|
CLX-0921 is an orally active PPARγ agonist with an IC50 of 1.54 μM. CLX-0921 has a potent antihyperglycemic activity, and can be used for the study of type 2 diabetes .
|
-
- HY-19674
-
|
SSR182289A free base
|
Thrombin
|
Cardiovascular Disease
|
|
SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (Ki=0.031 μM). SSR182289 demonstrates anticoagulant activity in vitro (thrombin time EC100=96 nM) and inhibits tissue factor-induced thrombin generation (IC50=0.15 μM) in human plasma. SSR182289 inhibits thrombin-induced aggregation of human platelets (IC50=32 nM), but has no effect on aggregation induced by other platelet agonists .
|
-
- HY-N10612
-
|
|
AMPK
PPAR
TRP Channel
Mitochondrial Metabolism
|
Metabolic Disease
Cancer
|
|
Petasin inhibits adipogenesis in cell 3T3-F442A with an IC50 of 0.95 μM. Petasin inhibits the expression of lipid synthesis factors ACC1, FAS and SCD1 by inhibiting transcription factors PPARγ and C/EBPα, as well as targeting TRPA1 and TRPV1 channels . Petasin inhibits mitochondrial complex I, thereby inhibiting tumor growth and metastasis. Petasin activates AMPK signaling pathway, participating in regulation of glucose and lipid metabolism. Petasin is orally active .
|
-
- HY-145695
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC50=550 nM) and MAO B (IC50=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability .
|
-
- HY-B2145
-
|
IY-81149 sodium
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-170575
-
|
|
Bacterial
|
Infection
|
|
Pks13-IN-1 (Compound 44) is an orally active inhibitor for Mycobacterium tuberculosis Polyketide synthase 13 (Pks13). Pks13-IN-1 inhibits M. tuberculosis strain H37Rv with a MIC of 0.07 μM. Pks13-IN-1 exhibits antibacterial efficacy in mouse model .
|
-
- HY-142686
-
|
|
SGK
|
Inflammation/Immunology
|
|
SGK1-IN-3 (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 has the potential for the research of osteoarthritis .
|
-
- HY-114977R
-
|
|
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Avenanthramide A (Standard) is the analytical standard of Avenanthramide A. This product is intended for research and analytical applications. Avenanthramide A is a phytoalexin, which can be found in oats (Avena sativa L.). Avenanthramide A targets the RNA helicase DDX3, leads to mitochondrial swelling and increased ROS production, and induces apoptosis in CRC cells. Avenanthramide A exhibits antitumor efficacy in mouse model. Avenanthramide A orally active .
|
-
- HY-142686A
-
|
|
SGK
|
Inflammation/Immunology
|
|
SGK1-IN-3 hydrochloride (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 hydrochloride has the potential for the research of osteoarthritis .
|
-
- HY-123689A
-
|
ALKS-33 hydrochloride; RDC-0313 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo .
|
-
- HY-A0276R
-
|
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Gentamicin (sulfate) (Standard) is the analytical standard of Gentamicin (sulfate). This product is intended for research and analytical applications. Gentamicin sulfate, an orally active aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. Gentamicin sulfate inhibits DNase I with an IC50 of 0.57 mM .
|
-
- HY-162702
-
|
|
Androgen Receptor
PROTACs
|
Cancer
|
|
AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker) .
|
-
- HY-N0807R
-
|
|
MMP
NF-κB
JAK
Keap1-Nrf2
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Swertiamarin (Standard) is the analytical standard of Swertiamarin. This product is intended for research and analytical applications. Swertiamarin is an orally active iridoid compound with hypoglycemic, hypolipidemic, anti rheumatic and antioxidant activities, which can be used in the research of diabetes and arthritis .
|
-
- HY-108288
-
|
CP 47904
|
Beta-lactamase
Antibiotic
Bacterial
|
Infection
|
|
Sulbactam pivoxil is a proagent of sulbactam. Sulbactam is a β-lactamase inhibitor which poorly adsorbed from gastrointestinal tract. Sulbactam pivoxil has a better absorption than the parent agent and provides high serum levels after oral administration .
|
-
- HY-147088
-
|
|
YAP
|
Cancer
|
|
TEAD-IN-2 is a novel, orally active inhibitor of transcriptional enhancer associate domain (TEAD) and modulates TEAD by ubiquitination and/or degradation by compounds. TEAD-IN-2 can be used for the research of a variety of diseases, disorders or conditions associated with TEAD .
|
-
- HY-119087
-
-
- HY-108411
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-N0304
-
|
Levodopa; 3,4-Dihydroxyphenylalanine
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease .
|
-
- HY-122011
-
|
|
ROCK
SGK
PKA
PKC
|
Inflammation/Immunology
|
|
PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration .
|
-
- HY-116565
-
|
SUVN-D4010
|
5-HT Receptor
|
Neurological Disease
|
|
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .
|
-
- HY-100748
-
|
CXD101
|
HDAC
|
Cancer
|
|
Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity .
|
-
- HY-146268
-
|
|
CaMK
|
Neurological Disease
|
|
CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability .
|
-
- HY-103433
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
K579 is a potent and orally active dipeptidyl peptidase IV inhibitor. K579 inhibits the blood glucose elevation. K579 increases the plasma insulin and active forms of glucagon-like peptide-1 (GLP-1). K579 has the potential for the research of diabetic .
|
-
- HY-151941
-
|
|
Bacterial
|
Infection
|
|
MtInhA-IN-1 is a selective and orally active Mycobacterium tuberculosis NADH-dependent enoyl-acyl carrier protein reductase (MtInhA) inhibitor with an IC50 of 0.23 μM. MtInhA-IN-1 potently against M. tuberculosis H37Rv strain with a MIC value of 0.4 μM .
|
-
- HY-123625
-
|
R-932348 choline
|
Interleukin Related
JAK
Syk
|
Inflammation/Immunology
|
|
R-348 (R-932348) choline is a potent and orally active JAK3 and Syk inhibitor. R-348 reduces IFN-γ, IL-6, and IL-10 expression. R-348 effectively diminishes acute cardiac allograft rejection .
|
-
- HY-114245B
-
|
Methylselenocysteine hydrochloride; Se-Methylseleno-L-cysteine hydrochloride
|
Endogenous Metabolite
Apoptosis
Beta-secretase
|
Cancer
|
|
Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine hydrochloride is orally bioavailable, and induces apoptosis .
|
-
- HY-114245
-
|
Methylselenocysteine; Se-Methylseleno-L-cysteine
|
Apoptosis
Endogenous Metabolite
Beta-secretase
|
Cancer
|
|
Se-Methylselenocysteine, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine is orally bioavailable, and induces apoptosis .
|
-
- HY-167669
-
|
|
Bacterial
|
Infection
|
|
Tioxacin is an orally active bactericide agent. Tioxacin combined with aliphatic amines has activities against G(+) and G (-) bacteria, including Escherichia coli resistant to Nalidixic acid (HY-B0398) and Pseudomonas aeruginosa .
|
-
- HY-10999
-
|
GSK1120212; JTP-74057
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
|
-
- HY-114191B
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM) .
|
-
- HY-10515
-
|
|
PDK-1
|
Cancer
|
|
BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect .
|
-
- HY-136185
-
|
|
Drug Metabolite
|
Others
|
|
Atorvastatin Epoxy Tetrahydrofuran Impurity is an impurity isolated oxidative degradation products of Atorvastatin (HY-B0589) . Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
|
-
- HY-151460
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo .
|
-
- HY-163739
-
|
|
α-synuclein
|
Neurological Disease
|
|
LETC is an orally active α-synuclein (α-Syn) aggregation inhibitor with an EC50 of 66 nM in transfected DH60.21 neuroblastoma cells. LETC can cross the blood-brain barrier. LETC can be used for the study of synucleinopathies .
|
-
- HY-145272
-
|
|
ELOVL
|
Neurological Disease
|
|
ELOVL1-IN-3 (Compound 22) is a potent and orally active inhibitor of elongation of very long chain fatty acid 1 (ELOVL1) enzyme. ELOVL1-IN-3 serves as a useful tool for researching adrenoleukodystrophy (ALD) [1].
|
-
- HY-B1617A
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
Endocrinology
|
|
Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent .
|
-
- HY-15550
-
-
- HY-126383
-
|
|
Bacterial
|
Infection
Others
Inflammation/Immunology
Cancer
|
|
Spilanthol is an orally active analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial and insecticidal compound.pilanthol can induce cAMP to inhibit negative regulation of urinary concentration mechanism. Spilanthol can be use as diuretic research .
|
-
- HY-121006
-
|
|
Mitochondrial Metabolism
AMPK
|
Metabolic Disease
Cancer
|
|
Biguanide is an orally active antihyperglycemic agent. Biguanide inhibits mitochondrial ATP production, activates the LKB1-AMPK signaling pathway, and damages the energy homeostasis. Biguanide exhibits potential in ameliorating the type 2 diabetes and the insulin-associated cancers .
|
-
- HY-158776
-
|
|
Parasite
|
Infection
|
|
SLU-10482 is an orally active anti-parasitic agent, that inhibits Cryptosporidium parvum with an IC50 of 0.0687 μM. SLU-10482 exhibits anti-infective efficacy in C. parvum infected mice with an AC50 of 0.0686 μM .
|
-
- HY-120763
-
|
|
Farnesyl Transferase
|
Cancer
|
|
LB42908 is a potent, selective and orally active farnesyltransferase inhibitor. LB42908 inhibits farnesylation of H-Ras, K-Ras with IC50 values of 0.9 nM, 2.4 nM for H-Ras, K-Ras, respectively. LB42908 shows antiproliferative activity. LB42908 shows antitumor activity .
|
-
- HY-B0162
-
|
|
HCN Channel
|
Cardiovascular Disease
Cancer
|
|
Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- HY-10594
-
|
TAK-442
|
Factor Xa
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Letaxaban (TAK-442) is an orally active and selective direct FXa inhibitor. Letaxaban is a drug with dual anticoagulant and anti-inflammatory activity that works by directly inhibiting FXa and by intervening in the PAR1 signaling pathway. Letaxaban can be used in the study of thrombotic diseases, cardiovascular diseases and inflammation-related diseases .
|
-
- HY-14670
-
|
ML 1785713
|
COX
|
Inflammation/Immunology
|
|
Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects .
|
-
- HY-149960
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-17 (compound 5u) is an orally active antiparasitic agent. Antiparasitic agent-17 inhibits Chloroquine sensitive (Pf3D7) and Chloroquine resistant (PfK1) strain with IC50s of 0.96 μM and 1.67 μM, respectively .
|
-
- HY-119816R
-
|
|
NKCC
|
Cardiovascular Disease
|
|
Piretanide (Standard) is the analytical standard of Piretanide. This product is intended for research and analytical applications. Piretanide is an oral active, relatively safe and effective diuretic. Piretanide has the potential for the research of congestive heart failure with a potential advantage of having potassium-sparing properties. Piretanide can also be used for the research of hypertension .
|
-
- HY-12282
-
|
|
LRRK2
|
Neurological Disease
|
|
GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .
|
-
- HY-135401
-
|
|
Discoidin Domain Receptor
|
Inflammation/Immunology
|
|
VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production .
|
-
- HY-B0162A
-
|
|
HCN Channel
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- HY-100516
-
|
UR-8880
|
COX
|
Inflammation/Immunology
|
|
Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar .
|
-
- HY-16247
-
|
HE3235
|
Biochemical Assay Reagents
|
Cancer
|
|
Apoptone, synthetic analogue of 3β-androstanediol, is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer . Apoptone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-147297
-
|
BCX9930
|
Complement System
|
Inflammation/Immunology
|
|
Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D with an IC50 value of 14.3 nM. Pelecopan can target factor D to prevent both intravascular and extravascular hemolysis in PNH. Pelecopan also be used for other alternative pathway (AP) mediated diseases .
|
-
- HY-12697
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .
|
-
- HY-101663
-
|
MK-8408
|
HCV
|
Infection
|
|
Ruzasvir (MK-8408) is an orally active inhibitor for genotypic HCV nonstructural protein 5A (NS5A), which inhibits the replication of NS5A mutants GT1a, GT1a L31V, GT1a Y93H, GT2b, GT3a and GT4a with EC90 ranging from 0.003 to 0.067 nM. Ruzasvir exhibits good pharmacokinetic characters in rhesus monkey model .
|
-
- HY-170527
-
|
|
Reactive Oxygen Species
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Anticancer agent 260 (Compound 3g/4d) is an orally active anticancer agent, that inhibits the proliferation of cancer cell HCT-116, MIA-PaCa2 and MDA-MB231 with IC50s of 98.7, 81.0, and 77.2 µg/mL, respectively. Anticancer agent 260 exhibits promotes ulcer formation and lipid peroxidation, anti-inflammatory and analgesic efficacy .
|
-
- HY-14904R
-
|
|
SARS-CoV
Influenza Virus
|
Infection
|
|
Umifenovir (Standard) is the analytical standard of Umifenovir. This product is intended for research and analytical applications. Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against a number of enveloped and non-enveloped viruses. Umifenovir is used as an anti-influenza virus agent. Umifenovir could effectively inhibit the fusion of virus with host cells . Umifenovir is an efficient inhibitor of SARS-CoV-2 in vitro . Umifenovir shows anti-inflammatory activity .
|
-
- HY-A0231
-
|
Gondafon; Glycodiazine
|
Insulin Receptor
|
Metabolic Disease
|
|
Glymidine sodium is an oral active antidiabetic. Glymidine sodium is the inhibitor of hepatic lipolysis. Glymidine sodium inhibits the glucose formation and supresses the elevated pyruvate oxidation which results from the inhibition of endogenous lipid mobilization .
|
-
- HY-14325A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
|
-
- HY-124290A
-
|
AJM300 hydrochloride
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) hydrochloride is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl hydrochloride, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl hydrochloride prevents the development of colitis in mice .
|
-
- HY-124754
-
|
BTRX-335140; CYM-53093
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .
|
-
- HY-122643
-
|
|
Bacterial
|
Infection
|
|
NITD-916, a 4-hydroxy-2-pyridone derivative, is an orally active and highly lipophilic mycobacterial enoyl reductase InhA inhibitor with an IC50 of 570 nM. NITD-916 forms a ternary complex with InhA and NADH to block access to the fatty acyl substrate binding pocket. NITD-916 has potent anti-tuberculosis effects .
|
-
- HY-123689
-
|
ALKS-33; RDC-0313
|
Opioid Receptor
|
Neurological Disease
|
|
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
|
-
- HY-160019
-
|
|
Deubiquitinase
Mitophagy
|
Neurological Disease
|
|
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
|
-
- HY-124290
-
|
AJM300
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice .
|
-
- HY-156280
-
|
|
RAR/RXR
|
Endocrinology
|
|
RARα antagonist 1 (compound 21) is an orally active and selective retinoic acid receptor α(RARα) antagonist, with the IC50 of 4.6nM .
|
-
- HY-N0661R
-
-
- HY-10315
-
|
RWJ-53308
|
Integrin
|
Cardiovascular Disease
|
|
Elarofiban (RWJ-53308) is a nonpeptide, orally active antagonist for fibrinogen receptor αIIbβ3 (GPIIb/IIIa), with an IC50 of 0.15 nM. Elarofiban has the potential for platelet mediated thrombotic disorders research .
|
-
- HY-114913
-
|
EL 222
|
Androgen Receptor
Bacterial
|
Infection
Endocrinology
|
|
Fenarimol (EL 222) is a potent and orally active fungicide. Fenarimol also is a androgen receptor inhibitor with an IC50 value of 19 µM. Fenarimol decreases the mRNA expression of PBP C3, ODC, IGF-1 .
|
-
- HY-148246
-
|
|
TGF-β Receptor
|
Cancer
|
|
MU1700 is an orally active and potent ALK1/2 inhibitor with IC50s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability .
|
-
- HY-15197
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1 .
|
-
- HY-17610A
-
|
TS-091 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
|
-
- HY-122592
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
Zifaxaban is an orally active, competitively and selective Factor Xa (FXa) inhibitor with an IC50 of 11.1 nM for human FXa. Zifaxaban shows >10000-fold greater selectivity than other serine proteases. Zifaxaban can be used for the arterial and venous thrombosis research .
|
-
- HY-147570
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC50 of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC50 of 37.34 nM. ATR-IN-18 has anti-tumor activity .
|
-
- HY-B2178
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-144270
-
-
- HY-N0304A
-
|
Levodopa sodium; 3,4-Dihydroxyphenylalanine sodium
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
L-DOPA (Levodopa) sodium is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA sodium can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA sodium has anti-allodynic effects, and can be used for Parkinson's disease research .
|
-
- HY-116420
-
|
|
ROCK
|
Neurological Disease
|
|
ROCK2-IN-8 (Compound 1) is an orally active ROCK2 inhibitor, with an IC50 of 7.2 nM. ROCK2-IN-8 can be used for the research of aqueous humor outflow in porcine eyes and myosin light chain phosphorylation .
|
-
- HY-139077
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
Cancer
|
|
SCD1 inhibitor-3 is a safe, potent and orally active SCD1 inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, type II diabetes and dyslipidemia, as well as skin diseases, acne and cancer .
|
-
- HY-107623
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R . TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively .
|
-
- HY-119086
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
L-651392 is an orally active and specific 5-lipoxygenase inhibitor that inhibits the production of leukotrienes. L-651392 controls the inflammatory process in Escherichia coli pyelonephritis by preventing inflammatory cells from reaching the site of infection and protecting the renal tubules from inflammation-related damage during pyelonephritis .
|
-
- HY-14356
-
-
- HY-B0425
-
|
Albamycin; Cathomycin
|
Antibiotic
DNA/RNA Synthesis
HSP
Apoptosis
Bacterial
Orthopoxvirus
|
Infection
Cancer
|
|
Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity .
|
-
- HY-19522
-
|
MBX-8025; RWJ-800025
|
PPAR
|
Metabolic Disease
|
|
Seladelpar (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM. Seladelpar shows more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively. Seladelpar can be used for the study of primary biliary cholangitis .
|
-
- HY-132298
-
|
|
Adenylate Cyclase
|
Others
|
|
TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound .
|
-
- HY-146334
-
|
|
Chloride Channel
|
Inflammation/Immunology
|
|
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain .
|
-
- HY-W015715
-
|
Orcinol monohydrate
|
Tyrosinase
|
Neurological Disease
|
|
5-Methylresorcinol monohydrate (Orcinol monohydrate) is a tyrosinase inhibitor. 5-Methylresorcinol monohydrate shows cytotoxicity. 5-Methylresorcinol monohydrate also is an oral active and cross the blood-brain barrier anxiolytic agent .
|
-
- HY-147772
-
-
- HY-170510
-
|
|
Galectin
|
Cancer
|
|
GB2095 is a selective, orally active inhibitor for galectin-3 with Kd of 36 nM and 0.35 μM for human galectin-3 and mouse galectin-3. GB2095 exhibits antitumor efficacy in mouse models .
|
-
- HY-109500
-
|
meso-Nordihydroguaiaretic acid; meso-NDGA
|
Lipoxygenase
|
Metabolic Disease
Cancer
|
|
Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenase inhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of type II diabetes .
|
-
- HY-147416
-
|
BI 1029539; GS-248; OX-MPI
|
PGE synthase
|
Infection
Cancer
|
|
Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity .
|
-
- HY-148189
-
|
LXY-05-029
|
AMPK
|
Metabolic Disease
|
|
Aldometanib (LXY-05-029) is an orally active aldolase inhibitor. Aldometanib can activate lysosomal adenosine monophosphate-activated protein kinase (AMPK) and decreases blood glucose. Aldometanib can be used for the research of metabolic homeostasis .
|
-
- HY-109143
-
|
ABBV-105
|
Btk
|
Inflammation/Immunology
|
|
Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease .
|
-
- HY-F0001
-
|
Disodium NADH
|
Endogenous Metabolite
|
Metabolic Disease
|
|
NADH disodium salt (Disodium NADH) is an orally active reduced coenzyme. NADH disodium salt is a donor of ADP-ribose units in ADP-ribosylaton reactions and a precursor of cyclic ADP-ribose. NADH disodium salt plays a role as a regenerative electron donor in cellular energy metabolism, including glycolysis, β-oxidation and the tricarboxylic acid (TCA) cycle .
|
-
- HY-141521
-
|
NX-13
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NX-13 is a first-in-class, orally active and gut-restricted agent that selectively targets and activates the NLRX1 pathway to induce immunometabolic changes. NX-13 results in lower inflammation and responses in inflammatory bowel disease. NX-13 can be used for the research of crohn's disease and ulcerative colitis .
|
-
- HY-124729
-
|
|
ULK
Autophagy
|
Neurological Disease
|
|
BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment .
|
-
- HY-13044
-
-
- HY-10864
-
URB-597
5 Publications Verification
KDS-4103
|
FAAH
Autophagy
Mitophagy
|
Neurological Disease
|
|
URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
|
-
- HY-15908
-
BCA
5 Publications Verification
Disodium bicinchoninate
|
Beta-secretase
|
Neurological Disease
Cancer
|
|
BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
|
-
- HY-151807
-
|
|
15-PGDH
|
Metabolic Disease
|
|
15-PGDH-IN-1 is a potent and orally active 15-PGDH inhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration .
|
-
- HY-150061
-
|
|
PI3K
mTOR
|
Cancer
|
|
NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor . NVP-BBD130 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-170569
-
|
|
Dipeptidyl Peptidase
Cytochrome P450
P-glycoprotein
|
Metabolic Disease
|
|
Cetagliptin is an orally active inhibitor for dipeptidyl peptidase 4 (DPP-4) and CYP2D6 (IC50 of 6 µM). Cetagliptin is a substrate for P-glycoprotein. Cetagliptin reduces the GLP-1 degradation, maintains the level of postprandial blood sugar, and can be used in type 2 diabetes mellitus research .
|
-
- HY-F0001A
-
|
Disodium NADH hydrate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
NADH disodium salt (Disodium NADH) hydrate is an orally active reduced coenzyme. NADH disodium salt hydrate is a donor of ADP-ribose units in ADP-ribosylaton reactions and a precursor of cyclic ADP-ribose. NADH disodium salt hydrate plays a role as a regenerative electron donor in cellular energy metabolism, including glycolysis, β-oxidation and the tricarboxylic acid (TCA) cycle .
|
-
- HY-19888
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases .
|
-
- HY-109127A
-
|
BCX7353 dihydrochloride
|
Kallikrein
|
Others
|
|
Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE .
|
-
- HY-141535
-
|
|
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
IL-17 modulator 1 is an orally active, highly efficacious small molecule IL-17 modulators extracted from patent WO 2020127685. IL-17 modulator 1 can be used for the research of preventing, researching or ameliorating a variety of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis .
|
-
- HY-125625
-
|
|
Renin
|
Cardiovascular Disease
|
|
ES 6864 is an orally active, competitive inhibitor for human renin, with an IC50 of 6.9 nM and a Ki of 7.3 nM. ES 6864 exhibits high species-specific and enzyme-specific properties. ES 6864 exhibits metabolic stability in rat tissue homogenates. ES 6864 reduces blood pressure in rats and sodium-depleted awake marmosets .
|
-
- HY-110198
-
|
|
Prostaglandin Receptor
PERK
|
Inflammation/Immunology
|
|
ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research .
|
-
- HY-167886
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
GA 0113 is a potent and orally active angiotensin II (Ang II) AT1-receptor antagonist. GA 0113 inhibits the Ang II (HY-13948)-induced pressor response with ID50 of 0.032 mg/kg and dose-dependently increases plasma renin activity for 48 h .
|
-
- HY-116565A
-
|
SUVN-D4010 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease .
|
-
- HY-101664
-
|
IY-81149
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-146435
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 22 (compound 14a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 22 inhibits LPS-induced TNF-α production with an IC50 value of 14.6 μM. Anti-inflammatory agent 22 has preventive effects on lymphedematous tissue via suppression of adipogenesis. Anti-inflammatory agent 22 suppresses limb lymphedema volume in mice .
|
-
- HY-163536
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway(IC50=1.07 μM). TGF-β1/Smad3-IN-1 possesses antifibrotic activity and oral potency .
|
-
- HY-12072
-
|
|
Src
|
Inflammation/Immunology
|
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis .
|
-
- HY-138696
-
|
XL092
|
TAM Receptor
c-Met/HGFR
VEGFR
|
Cancer
|
|
Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research .
|
-
- HY-143880
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
|
|
MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
|
-
- HY-14180
-
|
|
IKK
|
Inflammation/Immunology
|
|
PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation .
|
-
- HY-147226
-
|
|
Prostaglandin Receptor
|
Neurological Disease
Endocrinology
|
|
EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pKi of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research .
|
-
- HY-12938
-
|
|
Beta-secretase
|
Neurological Disease
|
|
AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain .
|
-
- HY-113974
-
|
t-AUCB
|
Epoxide Hydrolase
|
Cancer
|
|
trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity .
|
-
- HY-100399
-
|
PD-132301; ATR-101
|
Acyltransferase
Apoptosis
|
Cancer
|
|
Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer .
|
-
- HY-121149
-
|
3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
|
-
- HY-144285
-
|
|
CXCR
HIV
|
Inflammation/Immunology
|
|
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
|
-
- HY-100399A
-
|
PD-132301 hydrochloride; ATR101 hydrochloride
|
Acyltransferase
Apoptosis
|
Cancer
|
|
Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer .
|
-
- HY-19136
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-100289 is an orally active antagonist for 5-HT3 receptor, that exhibits high affinity to the isolated rat vagus nerves with pA2 of 8.9. WAY-100289 inhibits the Bezold-Jarisch reflex in anesthetized and awake rats .
|
-
- HY-137849
-
|
|
PARP
|
Cancer
|
|
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
|
-
- HY-150652
-
|
|
FGFR
Apoptosis
|
Cancer
|
|
FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities .
|
-
- HY-118301
-
|
|
GABA Receptor
|
Neurological Disease
|
|
ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity .
|
-
- HY-114191
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM) .
|
-
- HY-B0411A
-
|
R33812 monomaleate
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
|
-
- HY-114191A
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM) .
|
-
- HY-139486
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease .
|
-
- HY-144117
-
|
|
CDK
|
Metabolic Disease
|
|
GFB-12811 is a high selective and orally active CDK5 inhibitor with an IC50 of 2.3 nM. GFB-12811 is highly selective over the other tested kinases (CDK1/2/6/7/9) .
|
-
- HY-144448
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .
|
-
- HY-107798R
-
|
|
Bacterial
|
Infection
|
|
Potassium guaiacolsulfonate (hemihydrate) (Standard) is the analytical standard of Potassium guaiacolsulfonate (hemihydrate). This product is intended for research and analytical applications. Potassium guaiacolsulfonate hemihydrate is an orally active expectorant used for acute respiratory tract infections. Potassium guaiacolsulfonate hemihydrate helps loosen mucus and used for a cough caused by the common cold, infections or allergies in combination with other agents .
|
-
- HY-100886
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth .
|
-
- HY-122237
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
ATZ-1993 is an orally active, nonpeptide endothelin receptor subtype Aand endothelin receptor subtype B antagonist with pKi values of 8.69, 7.20, respectively. ATZ-1993 has the potential for the research of intimal hyperplasia after balloon denudation of the carotid artery .
|
-
- HY-158417
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
KSI-6666 is an orally active, competitive antagonist for sphingosine 1-phosphate receptor 1 (S1PR1), with an IC50 of 6.4 nM. KSI-6666 exhibits anti-inflammatory efficacy in autoimmune encephalomyelitis model and T cell transfer colitis model .
|
-
- HY-147573
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-23 is a potent and orally active BRD4 inhibitor with IC50s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1) .
|
-
- HY-143872
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2) .
|
-
- HY-116804
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-138967
-
|
|
Nuclear Hormone Receptor 4A/NR4A
RAR/RXR
|
Neurological Disease
|
|
BRF110 is the selective, orally active rexinoid for Nurr1-RXRα, that selectively activates the Nurr1-RXRα heterodimer with an EC50 of 0.9 μM in SH-SY5Y. BRF110 upregulates the expression of BDNF, exhibits neuroprotective activity against MPP+ induced toxicity. BRF110 can cross blood-brain barrier .
|
-
- HY-B0368A
-
|
SQ 14225 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Captopril (SQ 14225) hydrochloride, antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril hydrochloride is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
|
-
- HY-B1156A
-
|
Cefradine sodium; SQ-11436 sodium
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine sodium is a broad-spectrum and orally active cephalosporin. Cephradine sodium is active against both gram-positive and gram-negative pathogens. Cephradine sodium is effective in eradicating most penicillinase-producing organisms. Cephradine sodium has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine sodium blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-B0368
-
|
SQ 14225
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
|
-
- HY-149726
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-17 (compound 28) is a potent and orally active EZH2 inhibitor with an IC50 value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively) .
|
-
- HY-134188
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders .
|
-
- HY-B1156
-
|
Cefradine; SQ-11436
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Cefradine) is a broad-spectrum and orally active cephalosporin. Cephradine is active against both gram-positive and gram-negative pathogens. Cephradine is effective in eradicating most penicillinase-producing organisms. Cephradine has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-130120
-
|
|
Free Fatty Acid Receptor
PPAR
|
Metabolic Disease
|
|
HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects .
|
-
- HY-19522B
-
|
MBX-8025 (lysine)
|
PPAR
|
Metabolic Disease
|
|
Seladelpar (MBX-8025) lysine is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM. Seladelpar lysine shows more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively. Seladelpar lysine can be used for the study of primary biliary cholangitis .
|
-
- HY-156819
-
|
RMC-9805; KRAS G12D inhibitor 18
|
Ras
Apoptosis
|
Cancer
|
|
RMC-9805 (KRAS G12D inhibitor 18) is a potent and orally active KRAS G12D inhibitor. RMC-9805 induces apoptosis in KRAS G12D mutant cancer cells. RMC-9805 has the potential for the research of KRAS G12D mutant cancer .
|
-
- HY-106088
-
|
LY186655 free acid
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Tibenelast (LY186655) free acid is a potent and orally active is a phosphodiesterase inhibitor. Tibenelast free acid is an anti-asthma agent Tibenelast free acid increases the heart rate response to isoproterenol (HY-108353). Tibenelast free acid shows anti-anaphylactic shock activity. Tibenelast free acid has the potential for the research of asthma and other respiratory diseases .
|
-
- HY-13801
-
|
HOE 239
|
Parasite
|
Infection
|
|
Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC50s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei .
|
-
- HY-15011
-
|
|
Oxytocin Receptor
|
Others
|
|
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR .
|
-
- HY-139247
-
|
|
Drug Derivative
|
Inflammation/Immunology
|
|
pNPS-DHA (Compound 19) is an orally active DHA-ethanolamide (DHEA) derivative that has antiallergic activity. pNPS-DHA inhibits IgE-dependent passive cutaneous anaphylaxis (PCA) reaction in mice. pNPS-DHA has anti-degranulating activity in RBL-2H3 mast cells with an IC50 of 15 μM .
|
-
- HY-13512R
-
|
|
Ser/Thr Protease
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Camostat (mesylate) (Standard) is the analytical standard of Camostat (mesylate). This product is intended for research and analytical applications. Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase .
|
-
- HY-114234A
-
|
|
Beta-secretase
|
Neurological Disease
|
|
TAK-070 Free base is a noncompetitive and orally active BACE1 inhibitor (IC50: 3.15 μM). TAK-070 Free base can be used for research of Alzheimer’s disease (AD). TAK-070 Free base inhibits brain levels of soluble Aβ, and improves cognitive impairments in AD model .
|
-
- HY-158762
-
|
|
SHP2
|
Cancer
|
|
TK-642 is a highly active, selective, orally activity SHP2 inhibitor based on pyrazole and pyrazine (IC50=2.7 nmol/L). TK-642 can effectively inhibit the proliferation of esophageal carcinoma cells and induce cell apoptosis. TK-642 can be used in the study of esophageal cancer .
|
-
- HY-132935
-
|
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
BPR1R024 is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology .
|
-
- HY-124758
-
|
|
Mitochondrial Metabolism
|
Metabolic Disease
Cancer
|
|
SH-BC-893 is an orally active anti-neoplastic sphingolipid analog. SH-BC-893 also protects from ceramide-induced mitochondrial dysfunction and corrects diet-induced obesity. SH-BC-893 can be used for the research of cancer and obesity .
|
-
- HY-147268
-
|
RAF/KIN_2787
|
Raf
p38 MAPK
|
Cancer
|
|
Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity .
|
-
- HY-147719
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity .
|
-
- HY-114154
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity .
|
-
- HY-107626
-
|
|
MCHR1 (GPR24)
5-HT Receptor
|
Neurological Disease
|
|
ATC0065 is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 does not exhibits significant activity for MCHR2. ATC0065 has anxiolytic and antidepressant activities .
|
-
- HY-144266
-
|
Glucosylceramide synthase-IN-1
|
Glucosylceramide Synthase (GCS)
|
Neurological Disease
Metabolic Disease
|
|
Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research .
|
-
- HY-111432
-
|
|
Ras
|
Others
|
|
CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma .
|
-
- HY-123502
-
|
AZD-6738 formate
|
ATM/ATR
|
Cancer
|
|
Ceralasertib formate is a potent, selective and orally active ATR inhibitor with an IC50 value of 1 nM. Ceralasertib formate inhibits cell viability and induces DNA damage. Ceralasertib formate induces cell senescence. Ceralasertib formate shows antitumor activity .
|
-
- HY-144656
-
|
|
Steroid Sulfatase
|
Cancer
|
|
Steroid sulfatase-IN-1 is a potent and orally active Steroid sulfatase inhibitor with an IC50 of 1.71 nM. Steroid sulfatase-IN-1 shows antitumor activity in vivo. Steroid sulfatase-IN-1 has the potential for the research of breast cancer .
|
-
- HY-12113
-
|
ONX 0912; PR-047
|
Proteasome
Autophagy
Apoptosis
|
Cancer
|
|
Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells .
|
-
- HY-118837
-
|
|
ROCK
|
Cancer
|
|
WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer .
|
-
- HY-B1945
-
DEHP
2 Publications Verification
Bis(2-ethylhexyl) phthalate; Ergoplast FDO; ESBO-D 82
|
Endogenous Metabolite
|
Metabolic Disease
|
|
DEHP (Bis(2-ethylhexyl) phthalate) is a widely used plasticizer, which has orally active. DEHP can produce a wide spectrum of toxic effects on organisms including neurotoxicity, liver toxicity, immunotoxicity, and reproductive toxicity .
|
-
- HY-168949
-
|
|
VISTA
|
Inflammation/Immunology
Cancer
|
|
VISTA-IN-4 (Compound B3) is the orally active inhibitor for immune checkpoint protein VISTA with a KD of 0.452 μM. VISTA-IN-4 degrades VISTA in HepG2 with a 77% degradation rate at 5 μM. VISTA-IN-4 activates VISTA-mediated immunosuppression, restores T cell activity, and promotes the release of cytokine IL-2. VISTA-IN-4 exhibits antitumor activity in CT26 xenograft mouse models, and exhibits good pharmacokinetic properties with a good oral exposure in serum with an AUC(0-t) of 412.9 mg·h/mL in SD rats .
|
-
- HY-162897
-
|
|
mAChR
|
Cardiovascular Disease
|
|
BAY-2413555 is an orally active muscarinic acetylcholine receptor M2 modulator that protects the heart and improve cardiac function. BAY-2413555 is promising for research of heart failure .
|
-
- HY-145828
-
|
|
Microtubule/Tubulin
Ferroptosis
|
Cancer
|
|
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity .
|
-
- HY-10274
-
|
BIBR 1048
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran etexilate (BIBR 1048) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation .
|
-
- HY-145872
-
|
|
HBV
|
Infection
|
|
HBV-IN-20 is a potent and oral active HBV inhibitor with an EC50 of 0.46 µM. HBV-IN-20 is a typical type II CpAM (core protein assembly modulators) .
|
-
- HY-170309
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
NZ-804 is an orally active inhibitor for SARS-CoV-2 main protease Mpro with an IC50 of 8.9 nM. NZ-804 inhibits the SARS-CoV-2 replication in HeLa-hACE2 cell with an EC50 of 14 nM. NZ-804 exhibits board-spectrum antiviral activity aganst multiple CoVs. NZ-804 diminishes virus replication in mouse and hamster model .
|
-
- HY-144256
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties .
|
-
- HY-14186
-
|
WYE-160020
|
Potassium Channel
|
Cardiovascular Disease
|
|
KVI-020 is an orally active, potent and selective blocker of the atrial potassium channel Kv1.5, with an IC50 of 480 nM. KVI-020 can inhibits hERG, with an IC50 of 15100 nM. KVI-020 is a potent antiarrhythmic agent, and can be used for atrial fibrillation (AF) research .
|
-
- HY-105896
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB399885 is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with pKi values 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. SB399885 has cognitive enhancing properties .
|
-
- HY-114452
-
|
BTRX-246040
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models .
|
-
- HY-W015828
-
|
RGX-202; 3-Guanidinopropionic acid
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Ompenaclid (RGX-202) is an oral small-molecule SLC6A8 transporter inhibitor. Ompenaclid robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. Ompenaclid can be used for the research of cancer and duchenne muscular dystrophy .
|
-
- HY-50905
-
|
CHIR-258; TKI258
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
|
Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity .
|
-
- HY-10443A
-
|
Ro 4588161 hydrochloride; R1626 hydrochloride
|
HCV
DNA/RNA Synthesis
|
Infection
|
|
Balapiravir hydrochloride (Ro 4588161 hydrochloride; R1626 hydrochloride) is an orally active proagent of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir hydrochloride has anti-HCV activity . Balapiravir (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-10443
-
|
Ro 4588161; R1626
|
HCV
DNA/RNA Synthesis
|
Infection
|
|
Balapiravir (Ro 4588161; R1626) is an orally active proagent of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir has anti-HCV activity . Balapiravir is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-136207
-
|
|
nAChR
|
Neurological Disease
|
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect .
|
-
- HY-12501A
-
ITI-214
3 Publications Verification
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions .
|
-
- HY-12047
-
|
AP24534
|
Bcr-Abl
PDGFR
VEGFR
FGFR
Src
Autophagy
|
Cancer
|
|
Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively .
|
-
- HY-116800
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity .
|
-
- HY-D0873
-
|
EPPS
|
Amyloid-β
|
Neurological Disease
|
|
HEPPS (EPPS) is a buffering agent with the useful pH range from 7.3 ~ 8.7. HEPPS reduces Aβ-aggregate-induced memory deficits and rescues cognitive deficits in mice. EPPS is orally active and penetrates the blood-brain barrier .
|
-
- HY-136270
-
|
VX-803; M4344; ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
|
-
- HY-B0250
-
|
BCH-189
|
HIV
Reverse Transcriptase
HBV
|
Infection
Cancer
|
|
Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
|
-
- HY-13027G
-
-
- HY-15381
-
|
FTY720 phosphate
|
LPL Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases .
|
-
- HY-W424839
-
|
DTBP
|
Heme Oxygenase (HO)
|
Cardiovascular Disease
|
|
Probucol dithiobisphenol (DTBP) is the derivative of Probucol (HY-B0388). Probucol dithiobisphenol induces the production of heme oxygenase 1 (HO-1), and exhibits antioxidant activity. Probucol dithiobisphenol inhibits atherosclerotic lesions in Apoe −/− mice aorta, promotes re-endothelialization of aorta and inhibits restenosis in rabbit arterial injury models. Probucol dithiobisphenol is orally active .
|
-
- HY-123797
-
|
|
SGLT
|
Metabolic Disease
|
|
KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 has antidiabetic efficacy .
|
-
- HY-15798
-
|
|
VSV
TAM Receptor
|
Cardiovascular Disease
|
|
UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC50s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research .
|
-
- HY-116182
-
|
|
Influenza Virus
|
Infection
|
|
RO5487624, an analogue of RO5464466 (HY-120690), is an orally active hemagglutinin (HA) inhibitor of influenza H1N1 viruses that abolishes influenza virus fusion by blocking HA conformational changes in low pH environments. RO5487624 displays a protective effect on mice that are lethally challenged with influenza H1N1 virus .
|
-
- HY-107670
-
|
DHβE hydrobromide
|
nAChR
|
Neurological Disease
|
|
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities .
|
-
- HY-142283AS
-
|
|
EGFR
|
Cancer
|
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
|
-
- HY-11051
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
|
-
- HY-121798
-
|
|
PPAR
|
Metabolic Disease
|
|
TZD18 is a potent and orally active PPARα and PPARγ dual agonist with IC50 values of 0.028, 0.057, >10 µM for PPARα, PPARγ, PPARδ, respectively. TZD18 reduces plasma levels of both glucose and triglycerides in diabetic mice. TZD18 has the potential for the research of type 2 diabetes .
|
-
- HY-112090
-
|
|
Epigenetic Reader Domain
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .
|
-
- HY-14674
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities .
|
-
- HY-19644
-
|
GSK 2256294
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH). GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease .
|
-
- HY-10274A
-
|
BIBR 1048MS; Dabigatran etexilate methanesulfonate
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation .
|
-
- HY-145311
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Bis-Pro-5FU (Compound 4) is a 5-FU precursor that confers oral bioavailability and increase the safety profile of 5-Fluorouracil (5-FU) chemotherapy regimens. 5-FU is an antineoplastic antimetabolite that is widely used for the research of colorectal and pancreatic cancer .
|
-
- HY-13458A
-
|
L-DOPS hydrochloride; DOPS hydrochloride; SM5688 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Droxidopa (L-DOPS) hydrochloride is a potent, orally active norepinephrine precursor. Droxidopa hydrochloride increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa hydrochloride has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder) .
|
-
- HY-161847
-
|
|
Ser/Thr Protease
|
Cancer
|
|
Anticancer agent 241 (HZ1) is an orally active first-in-class cyclin-dependent kinase like 3 (CDKL3)-specific inhibitor. Anticancer agent 241 shows a strong tumor-suppressing effect, and has the potential to overcome the resistance of CDK4/6 inhibitor .
|
-
- HY-135615AR
-
|
|
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
|
Desmethyl Sibutramine (hydrochloride) (Standard) is the analytical standard of Desmethyl Sibutramine (hydrochloride). This product is intended for research and analytical applications. Desmethyl Sibutramine hydrochloride, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine hydrochloride can be used in the research of obesity and appetite suppressant .
|
-
- HY-152857
-
|
LY3473329
|
LDLR
|
Cardiovascular Disease
|
|
Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a)
formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys .
|
-
- HY-122891
-
|
|
PI3K
CXCR
STAT
|
Cancer
|
|
SB02024 is a potent and orally active VPS34 inhibitor. SB02024 inhibits Vps34 kinase activity. SB02024 induces CCL5 and CXCL10 via STAT1/IRF7. SB02024 shows anticancer activity .
|
-
- HY-10977
-
|
AV-951; KRN951
|
VEGFR
|
Cancer
|
|
Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy .
|
-
- HY-101634
-
|
|
HCV
|
Infection
|
|
ABT-072 is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM) .
|
-
- HY-142772
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity .
|
-
- HY-132193
-
|
|
RET
|
Cancer
|
|
RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects .
|
-
- HY-14336A
-
|
SB 271046A
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM) .
|
-
- HY-144770
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-13 (compound 5) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.057 μM. SARS-CoV-2-IN-13 is a niclosamide analogue. SARS-CoV-2-IN-13 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
|
-
- HY-144771
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-14 (compound 6) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.39 μM. SARS-CoV-2-IN-14 is a niclosamide analogue. SARS-CoV-2-IN-14 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
|
-
- HY-144772
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
|
-
- HY-141513
-
NH-3
3 Publications Verification
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC50 of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment . NH-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-161936
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Z21115 is an orally active inhibitor for phosphodiesterase 4 (PDE4), that inhibits PDE4D7 with IC50 of 10.5 nM. Z21115 inhibits Lipopolysaccharide (HY-D1056)-induced expression of IL-6, TNF-α and iNOS. Z21115 exhibits anti-inflammatory activity in DSS (HY-116282)-induced mouse colitis models without significant toxicity (1 g/kg) .
|
-
- HY-13540
-
|
GPI 21016
|
PARP
|
Cancer
|
|
E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent .
|
-
- HY-119524
-
|
|
Glutathione S-transferase
|
Metabolic Disease
|
|
Clofibride is an orally active hypolipaemic agent of pchlorophenoxyisobutyric type. Clofibride has weak toxicity and marked hypocholesterolaemic and hypotriglyceridaemic activity. Clofibride is converted into 4-chlorophenoxyisobutyric acid (CPIB) and 4-hydroxy-N-dimethylbutyramide (HMB) in vivo .
|
-
- HY-100555
-
|
|
HSP
|
Infection
Cancer
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
|
-
- HY-149120
-
|
|
Phospholipase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ASM-IN-1 is a potent and orally active acid sphingomyelinase (ASM) inhibitor with an IC50 value of 1.5 µM. ASM-IN-1 reduces lipid plaques in the aortic arch and aorta and reduces plasma ceramide concentration and Ox-LDL levels. ASM-IN-1 shows antiatherosclerotic and anti-inflammatory activity .
|
-
- HY-148740
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Werner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity .
|
-
- HY-145427
-
|
|
DNA-PK
|
Cancer
|
|
NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect .
|
-
- HY-19544
-
|
|
JAK
|
Cancer
|
|
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM) .
|
-
- HY-12580
-
|
|
MDM-2/p53
|
Cancer
|
|
RO5353 is an orally active inhibitor for p53-MDM2 with an IC50 of 7 nM for MDM2. RO5353 inhibits the proliferation of wild-type p53 cancer cells with an average IC50 of 7 nM. RO5353 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
|
-
- HY-148741
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity .
|
-
- HY-14803
-
|
BMS-214778; VEC-162
|
Melatonin Receptor
|
Neurological Disease
Endocrinology
|
|
Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24) .
|
-
- HY-14653
-
|
TAC-101; Am 555S
|
RAR/RXR
Apoptosis
|
Cancer
|
|
Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer .
|
-
- HY-167855
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
MRS4833 (compound 15) is an orally active, potent, competitive P2Y14R antagonist with an of IC50 of 5.92 nM for hP2Y14R and an IC50 of 4.8 nM for mP2Y14R. MRS4833 reduces airway eosinophilia in a protease-mediated asthma model and reverses chronic neuropathic pain in a mouse CCI model .
|
-
- HY-161663
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
|
-
- HY-137742
-
|
|
ULK
Autophagy
|
Cancer
|
|
SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-139094
-
|
|
LPL Receptor
|
Metabolic Disease
|
|
A6770 is an orally active, potent sphingosine 1-phosphate (S1P) lyase (S1PL) inhibitor. A6770 is phosphorylated and the phosphorylated form directly inhibits S1P lyased.A6770, a potential key metabolite of THI, induces a [ 3H]dhS1P increase .
|
-
- HY-144863
-
|
|
GnRH Receptor
|
Cancer
|
|
BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids .
|
-
- HY-115553
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor .
|
-
- HY-17421
-
|
TU-199
|
Proton Pump
|
Infection
Inflammation/Immunology
|
|
Tenatoprazole (TU-199) is an orally active imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life. Tenatoprazole inhibits hog gastric H +/K +-ATPase activity with an IC50 of 6.2 μM. Tenatoprazole blocks the interaction of ubiquitin with the ESCRT-1 factor Tsg101, inhibits production of several enveloped viruses, including EBV .
|
-
- HY-106420
-
|
16,16-dimethyl PGE2
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
16,16-Dimethyl prostaglandin E2 (16,16-dimethyl PGE2) is an orally active vertebrate Hematopoietic stem cells (HSCs) homeostasis critical regulator. 16,16-Dimethyl prostaglandin E2 can act through EP2/EP4 and has an interaction with the Wnt pathway .
|
-
- HY-145153
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism .
|
-
- HY-19742A
-
|
SRA-333 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Lecozotan (SRA-333) hydrochloride is an orally active and selective antagonist of 5-HT1A with a Ki of 4.5 nM for cloned human 5-HT1A receptor. Lecozotan hydrochloride enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties. Lecozotan hydrochloride has the potential for mild-to-moderate Alzheimer's disease (AD) research .
|
-
- HY-161892
-
|
|
FABP
|
Metabolic Disease
Inflammation/Immunology
|
|
FABP4-IN-4 (Compound 30) is an orally active inhibitor for FABP, with IC50 of 1.18 μM for FABP 1. FABP4-IN-4 improves the glucose tolerance, reduces the level of blood glucose, plasma lipids and hepatic inflammatory factors, attenuates hepatic steatosis, and exhibits anti-inflammatory effects in mouse diet-induced obesity models .
|
-
- HY-14806S
-
|
MP-513 d8
|
Dipeptidyl Peptidase
|
Cardiovascular Disease
|
|
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor[1].
|
-
- HY-13731
-
|
|
MetAP
|
Inflammation/Immunology
Cancer
|
|
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research .
|
-
- HY-N2109
-
|
|
Others
|
Metabolic Disease
|
|
Macranthoidin A is an orally active saponin from Flos Lonicerae. Macranthoidin A possess protection effects on hepatic injury caused by Acetaminophen, Cd, and CCl4, and conspicuous depressant effects on swelling of ear croton oil .
|
-
- HY-14184
-
-
- HY-139801
-
|
CI-907
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Metabolic Disease
|
|
Indolapril hydrochloride (CI-907) is an orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor. Indolapril hydrochloride is highly specific in suppressing the contractile or pressor responses to Angiotensin I. Indolapril hydrochloride is a potent antihypertensive agent .
|
-
- HY-10977A
-
|
AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate
|
VEGFR
|
Cancer
|
|
Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy .
|
-
- HY-101634A
-
|
|
HCV
|
Infection
|
|
ABT-072 (potassium trihydrate) is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM) .
|
-
- HY-19447
-
|
LB80331
|
HBV
|
Infection
|
|
Besifovir (LB80331), a parent agent converted by LB80380 (HY-19447A), further metabolizes to its active form, LB80317 (HY-106235). Besifovir is an orally active, novel antiviral agent against hepatitis B virus (HBV) .
|
-
- HY-10358
-
|
MK-2206 (2HCl)
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy .
|
-
- HY-131034
-
|
|
Wnt
|
Others
|
|
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats .
|
-
- HY-19374
-
|
|
GCGR
|
Metabolic Disease
|
|
BAY-27-9955 is an orally active non-peptide glucagon receptor antagonist. Bay 27-9955 competitively blocks the interaction of glucagon with the human glucagonreceptor at an IC50 value of 110 nM. BAY-27-9955 can be used for the study of type 2 diabetes .
|
-
- HY-13556
-
|
LY353381; SERM III
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile .
|
-
- HY-136657
-
SC-43
4 Publications Verification
|
Phosphatase
STAT
Apoptosis
|
Cancer
|
|
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects .
|
-
- HY-108766
-
|
AP24534 hydrochloride
|
Bcr-Abl
FGFR
PDGFR
VEGFR
Src
Autophagy
|
Infection
Cancer
|
|
Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively .
|
-
- HY-16743C
-
|
Venglustat hydrochloride; SAR402671 hydrochloride; GZ402671 hydrochloride
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Ibiglustat hydrochloride is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat hydrochloride can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease .
|
-
- HY-10619B
-
|
MK-4827 tosylate
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-168214
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC50 of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED50 of 12.02 and 9.63 mg/kg .
|
-
- HY-12501
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions .
|
-
- HY-10715
-
|
|
GlyT
|
Neurological Disease
|
|
SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities .
|
-
- HY-12947
-
|
|
MAP3K
|
Neurological Disease
|
|
GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases .
|
-
- HY-124007
-
|
ISAHA
|
HDAC
|
Cancer
|
|
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer .
|
-
- HY-123689S
-
|
ALKS-33-d4; RDC-0313-d4
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
|
-
- HY-108327
-
|
|
Potassium Channel
|
Neurological Disease
|
|
PF-05020182 is an orally active opener for Kv7 channel, that activates human Kv7.2/7.3, Kv7.4 and Kv7.3/7.5 with EC50 of 334, 625 and 588 nM, respectively. PF-05020182 exhibits anticonvulsant activity in rats corneal electric shock-induced tonic seizure (MES) models. PF-05020182 is blood-brain barrier (BBB) penetrable .
|
-
- HY-100560
-
|
(S)-(+)-Abscisic acid; ABA
|
Endogenous Metabolite
Proton Pump
|
Metabolic Disease
|
|
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome .
|
-
- HY-101664R
-
|
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (Standard) is the analytical standard of Ilaprazole. This product is intended for research and analytical applications. Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-120667
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC50 of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC50=0.17 μM) and DLD-1 (mutant p53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice .
|
-
- HY-160998
-
|
|
CCR
|
Inflammation/Immunology
|
|
YM-344031 is an orally active antagonist for CCR3. YM-344031 inhibits binding of Eotaxin-1 and RANTES to CCR3, with IC50 of 3.0 and 16.3 nM. YM-344031 inhibits ligand-induced rise in intracellular Ca [2+] and the ligand-induced chemotaxis. YM-344031 inhibits eotaxin-1-induced changes in eosinophil morphology in macaques blood, and prevents allergic skin reactions in a mouse allergy model .
|
-
- HY-128449
-
|
Cefradine monohydrate
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Cefradine) monohydrate is a broad-spectrum and orally active cephalosporin. Cephradine monohydrate is active against both grampositive and gram-negative pathogens and effective in eradicating most penicillinase-producing organisms known to be resistant to penicillin G, penicillin V, and ampicillin. Cephradine monohydrate has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine monohydrate blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-162703
-
|
|
AMPK
|
Metabolic Disease
|
|
Lipid-lowering agent-2 (Compound 14d) is an orally active lipid-lowering agent with an EC50 of 0.06 μM. Lipid-lowering agent-2 inhibits the lipid synthesis, activates the AMPK signaling pathway, and exhibits anti-obesity effect. Lipid-lowering agent-2 inhibits food intake, improves the glucose metabolism, and reduces the body weight and adipose tissue in high-fat diet (HFD)-induced obese mice .
|
-
- HY-146789
-
|
|
PI3K
|
Cancer
|
|
PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies .
|
-
- HY-161735
-
|
|
CXCR
|
Inflammation/Immunology
|
|
CXCR4-IN-3 (compound XVI) is an orally active and potent inhibitor targeting the inflammation-related receptor CXCR4, with an IC50 of 3.2 nM. CXCR4-IN-3 exhibits potent antichemotactic activity, at 79.19±2.33% inhibition. CXCR4-IN-3 shows anti-inflammatory activity. CXCR4-IN-3 can be used for IBD (inflammatory bowel disease) research .
|
-
- HY-133018
-
|
|
HCV
|
Infection
|
|
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity .
|
-
- HY-13458
-
|
L-DOPS; DOPS; SM5688
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Droxidopa (L-DOPS; SM5688) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder) .
|
-
- HY-146684
-
|
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research .
|
-
- HY-15228
-
RX-3117
1 Publications Verification
TV-1360; Fluorocyclopentenylcytosine
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis .
|
-
- HY-135747
-
|
GR-7
|
Bacterial
|
Infection
|
|
Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice .
|
-
- HY-149252
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity .
|
-
- HY-131417
-
|
|
MMP
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases .
|
-
- HY-130208
-
|
TDG
|
Galectin
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with Kd values of 24 μM, 49 μM for GAL1 and GAL3, respectively . Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats .
|
-
- HY-133018A
-
|
|
HCV
|
Cancer
|
|
HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity .
|
-
- HY-108411R
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine (Standard) is the analytical standard of Emedastine. This product is intended for research and analytical applications. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-W436428
-
|
|
Na+/K+ ATPase
Bacterial
|
Infection
|
|
V-161 is the orally active inhibitor for Na +-V-ATPase with an IC50 of 144 nM. V-161 inhibits Enterococcus hirae and Vancomycin-resistant Enterococcus faecium (VRE) under alkaline condition with MIC of 4 µg/mL and 4 µg/mL. V-161 inhibits colonization of VRE in mouse small intestine .
|
-
- HY-114319
-
|
|
Others
|
Cancer
|
|
β-Cembrenediol is a potent and orally active anticancer agent. β-Cembrenediol shows phytotoxic activities. β-Cembrenediol reduces the migration and colony formation. β-Cembrenediol decreases the protein expression of TDO2, IDO1. β-Cembrenediol has the potential for the research of prostate cancer .
|
-
- HY-19151A
-
|
IS-741 sodium
|
Integrin
Phospholipase
|
Inflammation/Immunology
|
|
Fuzapladib (IS-741) sodium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib sodium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib sodium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
|
-
- HY-116664
-
|
|
Apoptosis
Ras
Raf
Caspase
|
Cancer
|
|
DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer .
|
-
- HY-103493
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment .
|
-
- HY-100851A
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats .
|
-
- HY-19151B
-
|
IS-741 potassium
|
Integrin
Phospholipase
|
Inflammation/Immunology
|
|
Fuzapladib (IS-741) potassium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib potassium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib potassium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
|
-
- HY-103258
-
|
|
MAP3K
Apoptosis
|
Cancer
|
|
TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM) .
|
-
- HY-100851
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
LY-272015 is an orally active, specific 5-HT2B receptor antagonist. LY-272015 completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats .
|
-
- HY-144309
-
|
|
Cytochrome P450
|
Neurological Disease
|
|
Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective cholesterol 24-hydroxylase (CH24H or CYP46A1) inhibitor (IC50=8.5 nM). Cholesterol 24-hydroxylase-IN-1 can cross blood-brain barrier .
|
-
- HY-139915
-
|
|
Glutathione Peroxidase
|
Inflammation/Immunology
|
|
MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC50s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation .
|
-
- HY-W727879
-
|
ABT-494-15N,d2
|
Isotope-Labeled Compounds
|
Others
|
|
Upadacitinib- 15N,d2 (ABT-494- 15N,d2) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- 15N,d2 (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib- 15N,d2 (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- 15N,d2 (ABT-494) can be used for several autoimmune disorders research .
|
-
- HY-N6858
-
|
4-Hydroxy-L-isoleucine
|
Others
|
Metabolic Disease
|
|
4-Hydroxyisoleucine is an orally active amino acid that can be isolated from fenugreek seeds. 4-Hydroxyisoleucine displays insulinotropic and antidiabetic properties .
|
-
- HY-147015
-
|
|
Orthopoxvirus
|
Infection
|
|
HOE961, the diacetate ester proagent of S2242, is active against respiratory cowpox virus infections, is orally active in infection models. Anti-orthopoxvirus activity .
|
-
- HY-16743
-
|
Venglustat; SAR402671; GZ402671
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Ibiglustat (Venglustat) is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease .
|
-
- HY-15701B
-
ADH-503
1 Publications Verification
(Z)-Leukadherin-1 choline
|
Complement System
|
Cancer
|
|
ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses .
|
-
- HY-155785
-
|
|
Apoptosis
Autophagy
Reactive Oxygen Species
JAK
|
Cancer
|
|
MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma .
|
-
- HY-N0586R
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
Norisoboldine (Standard) is the analytical standard of Norisoboldine. This product is intended for research and analytical applications. Norisoboldine is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis .
|
-
- HY-121203R
-
|
|
Serotonin Transporter
|
Neurological Disease
Cancer
|
|
Citalopram (Standard) is the analytical standard of Citalopram. This product is intended for research and analytical applications. Citalopram is a racemate mixture of the active S(+)-enantiomer (Escitalopram; HY-14258) and R(-)-enantiomer. Citalopram is an orally active selective serotonin reuptake inhibitor (SSRI). Citalopram is an antidepressant and enhances serotoninergic neurotransmission .
|
-
- HY-121203S4
-
|
|
Serotonin Transporter
Isotope-Labeled Compounds
|
Neurological Disease
Cancer
|
|
Citalopram-d3 hydrochloride is deuterated labeled Citalopram (HY-121203). Citalopram is a racemate mixture of the active S(+)-enantiomer (Escitalopram; HY-14258) and R(-)-enantiomer. Citalopram is an orally active selective serotonin reuptake inhibitor (SSRI). Citalopram is an antidepressant and enhances serotoninergic neurotransmission .
|
-
- HY-152149
-
|
|
DNA/RNA Synthesis
|
Inflammation/Immunology
|
|
CTP Synthetase-IN-1 is a potent, orally active cytidine 5'-triphosphate synthetase (CTPS) inhibitor with IC50s of 32 nM and 18 nM for human CTPS1 and human CTPS2, respectively. CTP Synthetase-IN-1 has anti-inflammatory effects .
|
-
- HY-135903
-
|
GDC-9545 tartrate; RG6171 tartrate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity .
|
-
- HY-120350
-
BI-1347
1 Publications Verification
|
CDK
|
Cancer
|
|
BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity .
|
-
- HY-136527
-
|
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis) .
|
-
- HY-P10318
-
|
|
GLP Receptor
|
Endocrinology
|
|
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
|
-
- HY-144619
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases .
|
-
- HY-134463
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
|
-
- HY-A0027
-
|
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
Endocrinology
|
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
|
-
- HY-B0425R
-
|
|
Antibiotic
DNA/RNA Synthesis
HSP
Apoptosis
Bacterial
Orthopoxvirus
|
Infection
Cancer
|
|
Novobiocin (Standard) is the analytical standard of Novobiocin. This product is intended for research and analytical applications. Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity [4] .
|
-
- HY-15670
-
|
|
γ-secretase
Notch
|
Cancer
|
|
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity .
|
-
- HY-B0093
-
|
CGS14824A free base
|
Angiotensin-converting Enzyme (ACE)
Apoptosis
Reactive Oxygen Species
|
Cardiovascular Disease
Cancer
|
|
Benazepril (CGS14824A free base) is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. Benazepril improves diabetic nephropathy and decreases proteinuria. Benazepril can be used in the study of hypertension, heart failure and diabetic nephropathy .
|
-
- HY-B0162AR
-
|
|
HCN Channel
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Ivabradine (hydrochloride) (Standard) is the analytical standard of Ivabradine (hydrochloride). This product is intended for research and analytical applications. Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- HY-145953
-
|
|
Acetyl-CoA Carboxylase
|
Cancer
|
|
VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer .
|
-
- HY-A0027A
-
|
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
|
-
- HY-149099
-
|
|
RET
|
Cancer
|
|
RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
|
-
- HY-B0093A
-
-
- HY-16768
-
|
QAW039; NVP-QAW039
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Fevipiprant (QAW039, NVP-QAW039) is s an orally active, selective, reversible prostaglandin D2 (DP2) receptor antagonist with an Kd value of 1.14 nM. Fevipiprant has the potential for the research of bronchial asthma .
|
-
- HY-10619E
-
|
MK-4827 tosylate hydrate
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-10619
-
|
MK-4827
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-15981
-
|
MK-3102
|
Dipeptidyl Peptidase
|
Neurological Disease
Metabolic Disease
|
|
Omarigliptin (MK-3102) is a potent, selective, orally active and cross the blood-brain barrier dipeptidyl peptidase 4 (DPP-4) inhibitor. Omarigliptin shows anti-parkinsonian activity. Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction .
|
-
- HY-10619A
-
|
MK-4827 hydrochloride
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-120536
-
|
|
Bacterial
|
Infection
|
|
HPi1 is a potent, selective and orally active antimicrobial against Helicobacter pylori with an IC50 of 0.24 μM and an MIC of 0.08-0.16 μg/mL. HPi1 is inactive against other bacteria, including the gut commensals Lactobacillus casei, Lactobacillus reuteri, and Bifidobacterium longum .
|
-
- HY-111232
-
|
|
GHSR
|
Metabolic Disease
|
|
GSK894281 is an orally active and highly potent ghrelin receptor full agonist with a pEC50 of <4.9 at the human motilin receptor. GSK894281 effectively enters the CNS. GSK894281 has the potential for constipation or to assist in emptying the colon prior to colonoscopy or colon surgery research .
|
-
- HY-13956C
-
|
(R)-U 72107
|
PPAR
|
Neurological Disease
|
|
(R)-Pioglitazone ((+)-pioglitazone) is the R enantiomer of Pioglitazone (HY-13956). (R)-Pioglitazone is an orally active and selective peroxisome proliferator-activated receptor (PPARγ) agonist with high affinity binding to the PPARγ ligand-binding domain. (R)-Pioglitazone can be used for the research of Alzheimer's disease .
|
-
- HY-10999A
-
|
GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)
|
MEK
Apoptosis
|
Cancer
|
|
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis .
|
-
- HY-169294
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
SLC6A8 corrector 1 is an orally active and brain-penetrant mutant SLC6A8 variant corrector. SLC6A8 corrector 1 can be used for the study of creatine transporter deficiency (CTD) .
|
-
- HY-B0411
-
|
R33812
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
|
-
- HY-131343
-
|
|
HBV
DNA/RNA Synthesis
|
Infection
|
|
HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies .
|
-
- HY-12085
-
-
- HY-145685
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer .
|
-
- HY-138563
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) .
|
-
- HY-144260
-
|
|
SARS-CoV
|
Infection
|
|
3CPLro-IN-1 (compound A17) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 of 5.65 μM. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19 .
|
-
- HY-122844
-
|
BI-853520; IN-10018
|
FAK
|
Cancer
|
|
Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1?nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900?nM and 1040?nM, respectively .
|
-
- HY-151066
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMS-1233 is an orally active inhibitor for programmed cell death-ligand 1 (PD-L1), with IC50 of 14.5 nM. BMS-1233 promotes cell death of HepG2 in a Jurkat T cell and HepG2 cell co-culture model, exhibits antitumor activity against melanoma in mouse model .
|
-
- HY-107626A
-
|
|
MCHR1 (GPR24)
5-HT Receptor
|
Neurological Disease
|
|
ATC0065 free base is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 free base does not exhibits significant activity for MCHR2. ATC0065 free base has anxiolytic and antidepressant activities .
|
-
- HY-151248
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM . HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively .
|
-
- HY-164799
-
|
|
FXR
|
Inflammation/Immunology
|
|
FXR agonist 12 (Compound C7) is the orally active agonist for FXR. FXR agonist 12 down-regulates bile acid synthesis-related genes, and up-regulates bile acid transport-related genes in HepG2 cells. FXR agonist 12 improves ANIT-induced cholestasis, ameliorates the liver damage and fibrosis in mouse NASH models .
|
-
- HY-139300
-
|
HMPL-813
|
EGFR
|
Cancer
|
|
Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer . Epitinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-130187
-
|
|
Bacterial
|
Infection
|
|
Sapienic acid is a fatty acid commonly found on the skin and in mucosa. Sapienic acid has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively .
|
-
- HY-112852A
-
|
|
Src
Apoptosis
|
Cancer
|
|
TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth .
|
-
- HY-129755
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
CK-17 is an orally active and potent anti-inflammatory agent. CK-17 shows potent inhibition of ocular inflammation induced by lens protein, endotoxin, and IL-1. The effects on IL-1-induced inflammation are about 2 fold more potent than Prednisolone (HY-17463) .
|
-
- HY-146886
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia .
|
-
- HY-116830
-
BRD0705
1 Publications Verification
|
GSK-3
|
Cancer
|
|
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research .
|
-
- HY-145280A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 hydrochloride (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 hydrochloride exhibits antitumor activies. Orally active .
|
-
- HY-124344
-
|
|
Interleukin Related
|
Neurological Disease
|
|
Avenanthramide C is an orally active avenanthramide that can be isolated from oat seeds. Avenanthramide C decreases the protein expression of cleaved caspase-3 and increases the expression of p-GSK3β(Ser9) and IL-10 levels. Avenanthramide C has the potential for the research of Alzheimer’s disease .
|
-
- HY-145280
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active .
|
-
- HY-112852
-
TL02-59
5 Publications Verification
|
Src
Apoptosis
|
Cancer
|
|
TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth .
|
-
- HY-A0060
-
|
NKK 105
|
Lipoxygenase
|
Cancer
|
|
Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-lipoxygenase (5-LOX) (IC50=4.7 μM). Malotilate prevents the development of hepatocytic injury in alcohol-pyrazole hepatitis by decreasing hepatic acetaldehyde levels and preventing the retention of transferrin in the hepatocytes .
|
-
- HY-152075
-
|
|
TAM Receptor
|
Cancer
|
|
AXL-IN-14 is a potent and orally active AXL inhibitor with an IC50 value of 0.8 nM. AXL-IN-14 inhibits Gas6/AXL-mediated cell migration and invasion. AXL-IN-14 decreases the expression of p-AXL and p-AKT proteins. AXL-IN-14 shows anti-tumor activity .
|
-
- HY-N9587
-
|
|
Apoptosis
|
Neurological Disease
|
|
Tricin 7-O-β-D-glucopyranoside is a potent and orally active neuroprotective agent. Tricin 7-O-β-D-glucopyranoside induces Apoptosis. Tricin 7-O-β-D-glucopyranoside decreases the expression of TNF-α induced phosphor-κB-α, phosphor-NF-κB, HMGB1 .
|
-
- HY-137371
-
|
|
Bacterial
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Lactonic sophorolipid is a natural antimicrobial surfactant for oral hygiene . Lactonic sophorolipid, a potential anticancer agent, induces apoptosis in human HepG2 cells through the caspase-3 pathway .
|
-
- HY-N10225
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Thielavin A is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin A specifically inhibits the conversion of arachidonic acid into prostaglandin H2. Thielavin A has no anti-inflammatory activity on intravenous injection or on oral administration .
|
-
- HY-144318
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth .
|
-
- HY-N2549
-
|
(±)-ABA
|
Calcium Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
(±)-Abscisic acid ((±)-ABA) is an orally active phytohormone. (±)-Abscisic acid induces Ca 2+ channel opening to facilitate the influx of calcium ions and modulates stomatal movement. (±)-Abscisic acid shows anti-inflammatory activity and has the potential for the research of inflammatory bowel disease (IBD) .
|
-
- HY-162517
-
|
|
Orthopoxvirus
|
Infection
|
|
UMM-766 is an orally available nucleoside analog. UMM-766 has potent, broad-spectrum antiviral activity against multiple members of the pox virus family. UMM-766 provides protection in a murine model of orthopox disease .
|
-
- HY-168734
-
|
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
CB2 receptor agonist 9 (Compound 33) is an orally active agonist for cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. CB2 receptor agonist 9 inhibits the expression of TNF-α, IL-1β and IL-6, exhibits anti-inflammatory efficacy in DDS (HY-116282)-induced mouse acute colitis model .
|
-
- HY-117658
-
|
|
MAP3K
|
Cardiovascular Disease
|
|
GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 μM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue .
|
-
- HY-139609
-
|
RP-3500; ATR inhibitor 4
|
ATM/ATR
mTOR
|
Cancer
|
|
Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity .
|
-
- HY-117569
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
KF24345 free base is an orally active adenosine uptake inhibitor. KF24345 free base inhibits adenosine uptake by human, mouse, rabbit and hamster erythrocytes with IC50 values ??of 59.5, 130.1, 104.2 and 30.9 nM, respectively. KF24345 free base has anti-inflammatory activity and can inhibit LPS-induced TNF-α production and leukopenia in mice .
|
-
- HY-132817
-
|
ICP-192
|
FGFR
|
Cancer
|
|
Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer . Gunagratinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
|
-
- HY-147841
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .
|
-
- HY-111158
-
|
|
c-Met/HGFR
|
Cancer
|
|
BMS-748730 is an oral tyrosine kinase inhibitor. BMS-748730 inhibits tyrosine kinase activity by competing with the ATP binding site of the tyrosine kinase, which prevents the kinase from phosphorylating the substrate protein, thereby inhibiting signaling pathways associated with cell proliferation and tumor growth. BMS-748730 can be used in the study of certain types of cancer, including chronic myeloid leukemia (CML) .
|
-
- HY-157646
-
|
GYS1-IN-2
|
Others
|
Metabolic Disease
|
|
MZ-101 (GYS1-IN-2) is an orally active, potent and selective small-molecule glycogen synthase 1 (GYS1) inhibitor with with an IC50 value of 0.041 µM. MZ-101 reduces glycogen concentrations in cells and in mice. MZ-101 can used to study GYS1 -mediated Pompe disease and other glycogen storage diseases .
|
-
- HY-A0115
-
-
- HY-B1327A
-
|
7-Chlorotetracycline
|
Bacterial
Antibiotic
Parasite
|
Infection
Inflammation/Immunology
|
|
Chlortetracycline (7-Chlorotetracycline) is an orally active, effective and selectively methanogenic bacteria inhibitor with bactericidal effects. Chlortetracycline is also a antibiotic that acts by inhibiting bacterial protein synthesis. Additionally, Chlortetracycline is a specific and potent calcium ionophore antibiotic, inhibiting binding of aminoacyl-tRNA to ribosomes .
|
-
- HY-10315A
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Elarofiban diTFA is the salt form of Elarofiban (HY-10315) with two TFA. Elarofiban diTFA is a nonpeptide, orally active antagonist for fibrinogen receptor αIIbβ3 (GPIIb/IIIa), with an IC50 of 0.15 nM. Elarofiban diTFA has the potential for platelet mediated thrombotic disorders research .
|
-
- HY-113820
-
|
|
PPAR
|
Metabolic Disease
|
|
AZD4619 is an orally active, selective peroxisome proliferator-activated receptor α (PPARα) agonist. AZD4619 increases alanine aminotransferase 1 (ALT1) protein expression in a dose-dependent manner in human, but not in rat primary hepatocytes. AZD4619 is a lipid-lowering drug .
|
-
- HY-10999R
-
|
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib (Standard) is the analytical standard of Trametinib. This product is intended for research and analytical applications. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
|
-
- HY-15701A
-
|
ADH-503 free base
|
Complement System
|
Cancer
|
|
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses .
|
-
- HY-16743B
-
|
Venglustat succinate; SAR402671 succinate; GZ402671 succinate
|
Glucosylceramide Synthase (GCS)
|
Neurological Disease
|
|
Ibiglustat (Venglustat) succinate is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat succinate can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease .
|
-
- HY-B1327
-
|
7-Chlorotetracycline hydrochloride
|
Bacterial
Antibiotic
Parasite
|
Infection
Inflammation/Immunology
|
|
Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is an orally active, effective and selectively methanogenic bacteria inhibitor with bactericidal effects. Chlortetracycline hydrochloride is also a antibiotic that acts by inhibiting bacterial protein synthesis. Additionally, Chlortetracycline hydrochloride is a specific and potent calcium ionophore antibiotic, inhibiting binding of aminoacyl-tRNA to ribosomes .
|
-
- HY-100459
-
|
|
RET
|
Metabolic Disease
Inflammation/Immunology
|
|
GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity .
|
-
- HY-B1156R
-
|
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Standard) is the analytical standard of Cephradine. This product is intended for research and analytical applications. Cephradine (Cefradine) is a broad-spectrum and orally active cephalosporin. Cephradine is active against both gram-positive and gram-negative pathogens. Cephradine is effective in eradicating most penicillinase-producing organisms. Cephradine has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-101903A
-
|
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-101903
-
|
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-B0368R
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Captopril (Standard) is the analytical standard of Captopril. This product is intended for research and analytical applications. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
|
-
- HY-123857
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain .
|
-
- HY-138742
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .
|
-
- HY-18054A
-
|
|
11β-HSD
|
Inflammation/Immunology
|
|
BVT-2733 hydrochloride is a potent, selective and orally active nonsteroidal 11β-HSD1 inhibitor. BVT-2733 hydrochloride is more potent against mouse 11β-HSD1 enzyme (IC50=96 nM) than against human 11β-HSD1 enzyme (IC50=3341 nM). BVT-2733 hydrochloride has the potential to be used in the study of arthritis and obesity-related diseases .
|
-
- HY-168709
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Nrf2 activator 18 (Compound 11a) is an orally active activator for Keap1/Nrf2/HO-1 signaling pathway, that promotes the Nrf2 nuclear translocation, and enhances the antioxidant efficacy. Nrf2 activator 18 inhibits the release of IL-6 with an IC50 of 4.816 μM. Nrf2 activator 18 exhibits anti-inflammatory efficacy in mouse PM2.5-induced lung injury model .
|
-
- HY-132307
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent .
|
-
- HY-19599
-
|
(+)-Vorozole; R83842
|
Cytochrome P450
|
Cancer
|
|
Vorozole is a potent and selective, orally active non-steroidal aromatase inhibitor . Vorozole shows antitumor activity in vivo. Vorozole has the potential for the research of mammary cancer .
|
-
- HY-147322
-
|
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity .
|
-
- HY-139605
-
|
|
GLUT
|
Inflammation/Immunology
Cancer
|
|
GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases .
|
-
- HY-16957
-
|
|
HCV
HIV
|
Infection
|
|
LJ001 is a broad-spectrum and orally active antiviral agent. LJ001 exerts antiviral activities by binding to viral membranes. LJ001 inhibits TGEV and PDCoV infection. LJ001 decreases TGEV N and PDCoV N-protein expression .
|
-
- HY-B0423
-
|
Eustigmin bromide; Neoserine bromide
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers .
|
-
- HY-144107
-
|
|
HCV
|
Infection
|
|
HCV-IN-34 (compound 3i) is an orally active and potent HCV entry inhibitor. HCV-IN-35 shows excellent antiviral activity, with an EC50 of 0.010 μM and a CC50 (half-maximal cytotoxic concentration) of 8.23 μM .
|
-
- HY-115986
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-5 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.204 µM. MAO-B-IN-5 has the potential for the research of Parkinson's disease (PD) .
|
-
- HY-P3499
-
|
|
Guanylate Cyclase
|
Inflammation/Immunology
|
|
Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research .
|
-
- HY-152506
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Antioxidant agent-8 is an orally active inhibitor of Aβ1-42 deposition. Antioxidant agent-8 inhibits fibril aggregation (IC50=11.15 µM) and promotes fibril disaggregation (IC50=6.87 µM). Antioxidant agent-8 also inhibits Cu 2+-induced Aβ1-42 fibril aggregation (IC50=3.69 µM) and promotes Cu 2+-induced Aβ1-42 fibril disaggregation (IC50=3.35 µM). Antioxidant agent-8 has antioxidant activity, anti-inflammatory activity, biosafety, blood-brain barrier permeability and neuroprotective effect .
|
-
- HY-122700
-
|
|
Complement System
|
Inflammation/Immunology
|
|
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases .
|
-
- HY-142520
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
|
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation .
|
-
- HY-151920
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC50 value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTK Y223 and p-PLCγ2 Y1217. BTK-IN-17 shows anti-inflammatory effects .
|
-
- HY-19394A
-
|
|
PPAR
|
Metabolic Disease
|
|
(E)-CLX-0921 is the E-isomer of CLX-0921 (HY-19394). CLX-0921 is an orally active PPARγ agonist with an IC50 of 1.54 μM. CLX-0921 has a potent antihyperglycemic activity, and can be used for the study of type 2 diabetes .
|
-
- HY-124476
-
|
|
Caspase
Glutaminase
Apoptosis
|
Cancer
|
|
Cystamine is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
|
-
- HY-W020050
-
|
|
Caspase
Glutaminase
Apoptosis
|
Neurological Disease
Cancer
|
|
Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
|
-
- HY-15178
-
|
GRC 3886
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases .
|
-
- HY-148629
-
|
|
JNK
|
Neurological Disease
|
|
GDC-0134 is a potent, selective, orally active, brain-penetrant dual leucine zipper kinase (DLK) inhibitor. GDC-0134 blocks DLK activity in cellular assays and in animal models of neuronal injury. GDC-0134 can be used for the study of amyotrophic lateral sclerosis (ALS) .
|
-
- HY-106697
-
|
ICI 128436
|
Aldose Reductase
|
Metabolic Disease
|
|
Ponalrestat (ICI 128436) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Ponalrestat selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Ponalrestat inhibits the conversion of glucose to sorbitol .
|
-
- HY-12047S
-
|
AP24534-d8
|
Bcr-Abl
PDGFR
VEGFR
FGFR
Src
Autophagy
|
Cancer
|
|
Ponatinib-d8 is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
|
-
- HY-145829
-
|
|
JAK
Apoptosis
|
Inflammation/Immunology
|
|
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
|
-
- HY-12294
-
|
NVP-AAM077
|
Caspase
Apoptosis
iGluR
|
Neurological Disease
|
PEAQX (NVP-AAM077) is an orally active and selective NMDA antagonist, with IC50 values of 270 nM and 29.6 μM for hNMDAR 1A/2A and hNMDAR 1A/2B, respectively. PEAQX can promote the activation of caspase-3 and induce cell apoptosis in cortical striatal slice cultures .
|
-
- HY-114153
-
|
|
c-Fms
|
Neurological Disease
|
|
PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals .
|
-
- HY-108425A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM .
|
-
- HY-114452A
-
|
BTRX-246040 tartrate
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models .
|
-
- HY-149843
-
|
|
FGFR
PROTACs
|
Cancer
|
|
LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity .
|
-
- HY-B2178R
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine (difumarate) (Standard) is the analytical standard of Emedastine (difumarate). This product is intended for research and analytical applications. Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-134521
-
|
|
COX
|
Inflammation/Immunology
|
|
Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
|
-
- HY-12959A
-
|
BAY x 3702
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects .
|
-
- HY-15652
-
|
ONO-6818; ONO-PO-736
|
Elastase
|
Inflammation/Immunology
|
|
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
|
-
- HY-155141
-
|
|
Cytochrome P450
|
Cancer
|
|
hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .
|
-
- HY-173047
-
|
|
Ras
ERK
|
Cancer
|
|
KRASG12C IN-15 (Compound 21) is the orally active inhibitor for KRAS G12C, and inhibits SOS1-mediated GDP/GTP exchange with an IC50 of 19 nM. KRASG12C IN-15 inhibits the phosphorylation of ERK with IC50 of 0.051 μM. KRASG12C IN-15 inhibits the cell viability of KRAS G12C mutated MIA PaCa-2 with IC50 of 0.023 μM. KRASG12C IN-15 exhibits antitumor effect in MIA PaCa-2 xenograft mouse models .
|
-
- HY-B0731A
-
|
SM-9018 free base
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
|
-
- HY-160851
-
|
AK3287; AKEX0011
|
ASK1
p38 MAPK
|
Inflammation/Immunology
|
|
GDC-3280 (AK3287; AKEX0011) is an orally active compound based on Pirfenidone (HY-B0673)'s phenyl pyridone scaffold. GDC-3280 alleviates the inflammatory and fibrotic reaction of silicosis by inhibiting the ASK1-p38 MAPK pathway and regulating macrophage polarization. GDC-3280 exhibits anti-inflammatory and anti-fibrotic effects .
|
-
- HY-146237
-
|
CC-99282
|
Ligands for E3 Ligase
Molecular Glues
|
Cancer
|
|
Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL) .
|
-
- HY-109127R
-
|
|
Ser/Thr Protease
|
Others
|
|
Berotralstat (Standard) is the analytical standard of Berotralstat. This product is intended for research and analytical applications. Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE .
|
-
- HY-111313
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease .
|
-
- HY-115885
-
|
|
HDAC
|
Inflammation/Immunology
Cancer
|
|
XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma .
|
-
- HY-B1028S
-
|
D-Pantethine-15N2; LBF disulfide-15N2
|
Isotope-Labeled Compounds
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Pantethine- 15N2 is the 15N2 labeled Pantethine. Pantethine is an orally active lipid-lowering agent. Pantethine has anti-tumor, anti-inflammatory and anti-SARS-COV virus activities. Pantethine is also a neuroprotective agent. Pantethine can be used in the study of Alzheimer's disease, Parkinson's disease, major depression, systemic sclerosis and pantothenate kinase-related neurodegeneration .
|
-
- HY-13801R
-
|
|
Parasite
|
Infection
|
|
Fexinidazole (Standard) is the analytical standard of Fexinidazole. This product is intended for research and analytical applications. Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC50s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei .
|
-
- HY-F0001R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
NADH (disodium salt) (Standard) is the analytical standard of NADH (disodium salt). This product is intended for research and analytical applications. NADH disodium salt (Disodium NADH) is an orally active reduced coenzyme. NADH disodium salt is a donor of ADP-ribose units in ADP-ribosylaton reactions and a precursor of cyclic ADP-ribose. NADH disodium salt plays a role as a regenerative electron donor in cellular energy metabolism, including glycolysis, β-oxidation and the tricarboxylic acid (TCA) cycle .
|
-
- HY-108260
-
|
GT-56-252
|
Ferroptosis
|
Cardiovascular Disease
|
|
Deferitrin (GT-56-252), a desferrithiocin (DFT) analogue, is an orally active trident iron chelator. Deferitrin is used for chronic iron overload due to transfusional therapy. Deferitrin has the potential for beta-thalassemia major .
|
-
- HY-13580
-
|
|
Glucocorticoid Receptor
ADC Cytotoxin
|
Inflammation/Immunology
Cancer
|
|
Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma .
|
-
- HY-155693
-
|
|
Topoisomerase
Parasite
|
Infection
|
|
Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research .
|
-
- HY-W062109
-
|
|
Endogenous Metabolite
Histamine Receptor
|
Inflammation/Immunology
|
|
Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis .
|
-
- HY-143444
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo .
|
-
- HY-135299
-
|
|
Src
|
Cancer
|
|
CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo .
|
-
- HY-A0115S2
-
-
- HY-16743A
-
|
Venglustat (L-Malic acid); SAR402671 (L-Malic acid); GZ402671 (L-Malic acid)
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Ibiglustat (Venglustat) L-Malic acid is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat L-Malic acid can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease .
|
-
- HY-145655
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7 .
|
-
- HY-14165
-
-
- HY-16950
-
|
(Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen; (Z)-Afimoxifene
|
Estrogen Receptor/ERR
|
Cancer
|
|
4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) induces CRISPR/Cas9 systems based on ER mediated nucleus translocation. 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is also the active metabolic form of Tamoxifen (HY-13757A) in vivo and can be used to induce gene knockout in transgenic mice expressing CreER .
|
-
- HY-15196
-
TAK-285
2 Publications Verification
|
EGFR
|
Cancer
|
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) .
|
-
- HY-13208
-
|
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
|
IAP
Apoptosis
|
Cancer
|
|
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
|
-
- HY-128449R
-
|
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (monohydrate) (Standard) is the analytical standard of Cephradine (monohydrate). This product is intended for research and analytical applications. Cephradine (Cefradine) monohydrate is a broad-spectrum and orally active cephalosporin. Cephradine monohydrate is active against both grampositive and gram-negative pathogens and effective in eradicating most penicillinase-producing organisms known to be resistant to penicillin G, penicillin V, and ampicillin. Cephradine monohydrate has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine monohydrate blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-14184S
-
-
- HY-121383
-
|
AH5158; Sch-15719W free base
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy .
|
-
- HY-N12240
-
|
|
Bacterial
|
Infection
|
|
Oleanolic aldehyde is an antimicrobial compound used to inhibit oral bacteria. Oleanolic aldehyde inhibits Streptococcus mutans and Porphyromonas gingivalis, which are associated with dental caries and periodontal disease, with minimum inhibitory concentrations (MICs) of 488 μg/mL and 250 μg/mL, respectively .
|
-
- HY-147208
-
|
|
YAP
|
Cancer
|
|
MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .
|
-
- HY-107064
-
|
CGP 9000; Oraspor
|
Bacterial
Antibiotic
|
Infection
|
|
Cefroxadine (CGP 9000) is an orally active cephalosporin antibiotic. Cefroxadine is more effective than cephalexin against Escherichia coli and Klebsiella pneumoniae with MIC values of 3.13 and 1.56 μg/mL respectively with a concentration of 10 6 μg/mL. Cefroxadine can be used for the research of infection .
|
-
- HY-P2229
-
|
SDZ CO 611
|
Somatostatin Receptor
|
Cancer
|
|
Ilatreotide (SDZ CO61), glycated somatostatin derivative, is a highly potent glycated analog of somatostatin with improved oral activity. Ilatreotide can suppress the fasting level and postprandial release of several gastrointestinal and pancreatic hormones. Ilatreotide can be used for the research of gastroenteropancreatic tumors .
|
-
- HY-114895
-
|
|
GlyT
|
Neurological Disease
|
|
SSR504734 free base is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38?nM, respectively). SSR504734 free base shows anti-schizophrenia, anti-anxiety and anti-depression activities .
|
-
- HY-14305
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis .
|
-
- HY-148250
-
|
|
iGluR
|
Neurological Disease
|
|
TP-050 is a potent, orally active and selective NMDAR agonist with an EC50 value of 0.51 µM and 9.6 µM for GluN2A and GluN2D, respecticely. TP-050 can cross the blood-brain barrier (BBB). TP-050 induces hippocampal long-term (LPT) potentiation enhancemen and enhances neuronal signal transmission .
|
-
- HY-170492
-
|
|
Epoxide Hydrolase
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
sEH inhibitor-19 (Compound (R)-14i) is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 1.2 nM. sEH inhibitor-19 inhibits the expression of TNF-α and IL-6, exhibits anti-inflammatory activity in mouse acute pancreatitis or Carrageenan (HY-125474)-induced edema models .
|
-
- HY-136895
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM) .
|
-
- HY-144263
-
|
|
SARS-CoV
|
Infection
|
|
3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 and Ki of 1.55 and 6.09 μM, respectively. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19 .
|
-
- HY-114153A
-
|
|
c-Fms
|
Neurological Disease
|
|
PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals .
|
-
- HY-13691
-
|
Ro-31-7453
|
Akt
mTOR
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family .
|
-
- HY-139300A
-
|
HMPL-813 succinate
|
EGFR
|
Cancer
|
|
Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer . Epitinib (succinate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-145697
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). GPR84 antagonist 2 shows improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. GPR84 antagonist 2 has the potential for the research of ulcerative colitis .
|
-
- HY-147927
-
|
|
Enteropeptidase
|
Metabolic Disease
|
|
Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research .
|
-
- HY-144254
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models .
|
-
- HY-14294
-
|
S-1153
|
Reverse Transcriptase
HIV
|
Infection
|
|
Capravirine (S-1153) is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) with potent antiviral activity. Capravirine inhibits replication of HIV-1 strains that are resistant to nucleoside/nucleotide reverse transcriptase inhibitors and other NNRTIs. Capravirine is metabolized by the cytochrome P450 enzyme CYP3A4 .
|
-
- HY-132300
-
|
|
β-catenin
|
Cancer
|
|
ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM .
|
-
- HY-B1945R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
DEHP (Standard) is the analytical standard of DEHP. This product is intended for research and analytical applications. DEHP (Bis(2-ethylhexyl) phthalate) is a widely used plasticizer, which has orally active. DEHP can produce a wide spectrum of toxic effects on organisms including neurotoxicity, liver toxicity, immunotoxicity, and reproductive toxicity .
|
-
- HY-145835
-
|
|
PERK
|
Cancer
|
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
|
-
- HY-N0366
-
|
|
PDGFR
|
Inflammation/Immunology
|
|
Sennoside B is a potent and orally active platelet-derived growth factor (PDGF) inhibitor. Sennoside B inhibits cell proliferation and the expression of phosphorylation of PDGFR-β, STAT-5, AKT and ERK induced by PDGF-BB. Sennoside B shows gastroprotective activities. Sennoside B has the potential for the research of gastritis .
|
-
- HY-14128
-
|
SB-723620
|
CRFR
|
Neurological Disease
|
|
NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC50 of 58.9 nM and a Ki of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.
|
-
- HY-116218C
-
|
JPI-289 hydrochloride
|
PARP
|
Cardiovascular Disease
Neurological Disease
|
|
Amelparib (JPI-289) hydrochloride is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib hydrochloride inhibits PARP-1 activity (IC50 = 18.5 nM) and cellular PAR formation (IC50 = 10.7 nM). Amelparib hydrochloride is a potential neuroprotective agent. Amelparib hydrochloride has the potential for the research of acute ischaemic stroke .
|
-
- HY-B1804
-
|
Trioctanoin; Glyceryl trioctanoate
|
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
|
Tricaprilin (Trioctanoin) is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
|
-
- HY-111817
-
|
|
Parasite
|
Infection
|
|
ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial .
|
-
- HY-132935A
-
|
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor.
BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology .
|
-
- HY-125390
-
|
CL-087
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
Cancer
|
|
SM-360320 (CL-087) is a potent, orally active TLR7 agonist. SM-360320 is a immuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response . SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity .
|
-
- HY-146012
-
|
|
HIV
|
Infection
|
|
HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a proagent of atazanavir. HIV-1 protease-IN-4 as a proagent that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent agent .
|
-
- HY-162423
-
|
|
5-HT Receptor
Androgen Receptor
|
Neurological Disease
|
|
CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration .
|
-
- HY-106874A
-
|
RS-15385-197 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Delequamine (RS-15385-197) hydrochloride is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine hydrochloride shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine hydrochloride can be used for the study of erectile dysfunction .
|
-
- HY-106874
-
|
RS-15385-197
|
Adrenergic Receptor
|
Neurological Disease
|
|
Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine can be used for the study of erectile dysfunction .
|
-
- HY-170918
-
|
|
Potassium Channel
|
Others
|
|
BKCa activator-1 (Compound 51b) is the orally active activator for the calcium-activated potassium channel BKCa with an EC50 of 2.82 μM. BKCa activator-1 increases K+ efflux, leads to cell membrane hyperpolarization, thereby inhibiting smooth muscle contraction. BKCa activator-1 alleviates urinary incontinence in spontaneously hypertensive rat (SHR) model, exhibits antitussive effect in puinea pig cough model .
|
-
- HY-120160A
-
|
CP 86325 Sodium
|
PPAR
|
Neurological Disease
Metabolic Disease
|
|
Darglitazone Sodium, a thiazolidinedione, is an orally active, potent, and selective PPAR-γ (peroxisome proliferator-activated receptor) agonist. Darglitazone Sodium is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
|
-
- HY-161887
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
SMARCA2-IN-8 (Compound 13) is an orally active inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 (also known as Brahma homologue, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1) with IC50 of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC50 of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC50 of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
|
-
- HY-159179
-
|
|
Integrin
|
Inflammation/Immunology
|
|
α4 integrin receptor antagonist 3 (Compound 11) is an orally active α4integrin receptor antagonist. α4 integrin receptor antagonist 3 can inhibit the adhesion of K562 cells mediated by the interaction between α4β1/VCAM-1 and α4β7/MAdCAM-1, with IC50 values of 130 nM and 2 nM, respectively. α4 integrin receptor antagonist 3 has the potential to be used in the study of dextran sulfate sodium (DSS) colitis mouse model .
|
-
- HY-15779
-
|
|
SphK
Apoptosis
|
Cancer
|
|
K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity .
|
-
- HY-15779A
-
|
|
SphK
Apoptosis
|
Cancer
|
|
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity .
|
-
- HY-144109
-
|
|
HCV
|
Infection
|
|
HCV-IN-36 (compound (S)-3h) is an orally active and potent HCV entry inhibitor. HCV-IN-36 shows excellent antiviral activity, with an EC50 of 0.016 μM and a CC50 (half-maximal cytotoxic concentration) of 8.78 μM .
|
-
- HY-106080A
-
|
U-63557A
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent .
|
-
- HY-150076
-
|
|
PKA
|
Metabolic Disease
Cancer
|
|
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research .
|
-
- HY-101528
-
|
|
iGluR
|
Neurological Disease
|
|
IDRA 21 is a positive and orally active modulator of the AMPA receptor. IDRA 21 facilitates excitatory neurotransmission via GluR1/2 receptors. IDRA 21 has the potential for the research of cognitive/memory disorders, including those associated with aging .
|
-
- HY-156963
-
|
FP-025
|
MMP
|
Inflammation/Immunology
|
|
Aderamastat (FP-025) is an orally active matrix metalloproteinase 12 (MMP-12) inhibitor. Aderamastat can be used for the research of asthma, chronic obstructive pulmonary disease (COPD), and pulmonary fibrosis .
|
-
- HY-14743B
-
|
SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride
|
Bacterial
STAT
|
Infection
Inflammation/Immunology
Cancer
|
|
Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2) .
|
-
- HY-145284
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease .
|
-
- HY-18676B
-
|
OSU-T315 analog
|
Integrin
Autophagy
Apoptosis
Caspase
PDHK
|
Cancer
|
|
ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models .
|
-
- HY-13699
-
|
|
GnRH Receptor
PERK
|
Others
|
|
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca 2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases .
|
-
- HY-120181
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC50=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors .
|
-
- HY-159108
-
|
|
c-Fms
|
Cardiovascular Disease
|
|
AZ683 is a potent and selective 3-amido-4-anilinoquinoline CSF1R inhibitor. AZ683 has high affinity for CSF1R (Ki=8 nM; IC50=6 nM). AZ683 has good oral bioavailability. [ 11C]AZ683 can be used as a positron emission tomography (PET) radiotracer for colony stimulating factor 1 receptor (CSF1R) .
|
-
- HY-116594A
-
|
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
|
OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity .
|
-
- HY-170499
-
|
BI02982816
|
mGluR
|
Neurological Disease
|
|
VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable .
|
-
- HY-156419A
-
|
|
PARP
|
Cancer
|
|
PARP7-IN-16 free base is the free base form of PARP7-IN-16 (HY-156419). PARP7-IN-16 free base is a selective and orally active inhibitor of PARP-1/2/7, with IC50s of 0.94, 0.87 and 0.21 nM, respectively. PARP7-IN-16 can be used for the research of breast cancer and prostate cancer .
|
-
- HY-130609
-
|
|
γ-secretase
|
Neurological Disease
|
|
Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
|
-
- HY-14803R
-
|
|
Melatonin Receptor
|
Neurological Disease
Endocrinology
|
|
Tasimelteon (Standard) is the analytical standard of Tasimelteon. This product is intended for research and analytical applications. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24) .
|
-
- HY-120124
-
|
SUVN-G3031
|
Histamine Receptor
|
Neurological Disease
|
|
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
|
-
- HY-125351
-
|
|
Ceramidase
|
Metabolic Disease
|
|
SPT-IN-1 (compound 1) is an orally active and potent SPT (serine palmitoyl transferase) inhibitor, with an IC50 of 5.19 nM for hSPT1. SPT-IN-1 can be used for type 2 diabetes and dyslipidemia research .
|
-
- HY-102074
-
|
|
DNA/RNA Synthesis
|
Infection
|
|
ERDRP-0519, an orally bioavailable small-molecule Measles virus (MeV) polymerase inhibitor, prevents measles disease in squirrel monkeys (Saimiri sciureus). ERDRP-0519 inhibits morbilliviruses with nanomolar potency. .
|
-
- HY-N6967
-
|
(-)-α-Bisabolol
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-161373
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα H1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .
|
-
- HY-129388A
-
|
CC-90011; LSD1-IN-7
|
Histone Demethylase
|
Cancer
|
|
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-15550R
-
|
|
Drug Metabolite
|
Neurological Disease
Inflammation/Immunology
|
|
4'-Hydroxy diclofenac (Standard) is the analytical standard of 4'-Hydroxy diclofenac. This product is intended for research and analytical applications. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties .
|
-
- HY-N0936
-
Coixol
1 Publications Verification
6-Methoxy-2-benzoxazolinone; 6-MBOA
|
Others
|
Inflammation/Immunology
|
|
Coixol (6-Methoxy-2-benzoxazolinone; 6-MBOA) is a potent and orally active anti-inflammatory agent. Coixol decreases the iNOS protein expression. Coixol inhibits the production of TNF-α, IL-6, and IL-1β. Coixol improves glucose tolerance and plasma insulin. Coixol decreases the blood glucose level .
|
-
- HY-139015
-
|
5-Aza-T-dCyd; NTX-301
|
DNA Methyltransferase
|
Cancer
|
|
5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects .
|
-
- HY-168485
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARα/δ agonist 3 (Compound 8) is the orally active agonist for PPAR, that activates PPARα, PPARδ and PPARγ with EC50 of 5.6, 3.4 and 1278 nM, respectively. PPARα/δ agonist 3 exhibits anticholestatic activity in mouse ANIT- or CDCA (HY-76847)-induced cholestatic liver disease models .
|
-
- HY-15652A
-
|
ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
|
Elastase
|
Inflammation/Immunology
|
|
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
|
-
- HY-B1971
-
-
- HY-114785
-
|
|
MMP
|
Cancer
|
|
BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with IC50s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC50s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects .
|
-
- HY-145564
-
|
PF-07265803
|
p38 MAPK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain .
|
-
- HY-130187A
-
|
|
Bacterial
|
Infection
|
|
Sapienic acid sodium is a fatty acid commonly found on the skin and in mucosa. Sapienic acid sodium has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid sodium is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively .
|
-
- HY-112037A
-
|
IACS-10759 hydrochloride
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research .
|
-
- HY-147110
-
|
|
Fungal
|
Infection
Inflammation/Immunology
|
|
APX2039 is an orally active and potent inhibitor of the fungal Gwt1 enzyme. APX2039 has extremely potent anticryptococcal activity against C. neoformans and C. gattii. APX2039 blocks the localization of GPI (glycosylphosphatidyl inositol)-anchored cell wall mannoproteins. APX2039 can be used for Cryptococcal meningitis (CM) research .
|
-
- HY-112037
-
|
IACS-10759
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research .
|
-
- HY-B0411AR
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (monomaleate) (Standard) is the analytical standard of Domperidone (monomaleate). This product is intended for research and analytical applications. Domperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
|
-
- HY-144893
-
|
|
HDAC
|
Cancer
|
|
OKI-006 is a potent and orally active inhibitor of histone deacetylase (HDAC). OKI-006 is a unique congener of the natural product HDAC inhibitor largazole. Histone deacetylases (HDACs) play critical roles in epigenomic regulation, and histone acetylation is dysregulated in many human cancers. OKI-006 has the potential for the research of cancer disease .
|
-
- HY-12047R
-
|
|
Bcr-Abl
PDGFR
VEGFR
FGFR
Src
Autophagy
|
Cancer
|
|
Ponatinib (Standard) is the analytical standard of Ponatinib. This product is intended for research and analytical applications. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively .
|
-
- HY-145702
-
|
|
MEK
ERK
|
Cancer
|
|
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
|
-
- HY-103442
-
|
DAPH
|
EGFR
Amyloid-β
|
Neurological Disease
Cancer
|
|
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease .
|
-
- HY-131543
-
|
RU 42698
|
Endogenous Metabolite
Glucocorticoid Receptor
|
Metabolic Disease
|
|
22-Hydroxy Mifepristone (RU 42698) is an orally active hydroxylated alcoholic metabolite with antiprogestational and antiglucocorticoidal activities, which contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. The relative binding affinity of 22-Hydroxy Mifepristone to the human glucocorticoid receptor is 48% .
|
-
- HY-B0267C
-
|
Aroxybutynin
|
mAChR
|
Neurological Disease
|
|
(R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
|
-
- HY-107385
-
|
ONO-9302; SKF105657
|
5 alpha Reductase
|
Cancer
|
|
Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .
|
-
- HY-101246
-
|
|
RET
|
Cancer
|
|
RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .
|
-
- HY-121852
-
|
SCH-225336
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice .
|
-
- HY-B0396
-
-
- HY-B0396A
-
|
L084 hydrochloride
|
Penicillin-binding protein (PBP)
Bacterial
Antibiotic
|
Infection
|
|
Tebipenem pivoxil (L084) hydrochloride is an orally active antibiotic against a variety of pathogenic bacteria. Tebipenem pivoxil hydrochloride binds penicillin-binding protein (PBP), thereby inhibiting cell wall synthesis .
|
-
- HY-144743
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
ATX inhibitor 12 (compound 20) is an orally active and potent ATX (autotaxin) inhibitor, with an IC50 of 1.72 nM. ATX inhibitor 12 effectively alleviates lung structural damage with fewer fibrotic lesions at an oral dose of 60 mg/kg in C57Bl/6J mice. ATX inhibitor 12 can be uesd for idiopathic pulmonary fibrosis (IPF) research .
|
-
- HY-100560R
-
|
|
Endogenous Metabolite
Proton Pump
|
Metabolic Disease
|
|
Abscisic acid (Standard) is the analytical standard of Abscisic acid. This product is intended for research and analytical applications. Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H+-ATPase) and leads to the plasma membrane depolarization in a Ca2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome .
|
-
- HY-173048
-
|
|
ClpP
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
CLPP-2068 is the orally active activator for human caseinolytic protease P (HsClpP) with an EC50 of 50.4 nM. CLPP-2068 exhibits anti-proliferative efficacy in OCI-LY10 cancer cell with an IC50 of 5.2 nM. CLPP-2068 decreases mitochondrial membrane potential, increases mitochondrial ROS levels, and induces mitochondrial dysfunction. CLPP-2068 arrests the cell cycle at G1 phase, and induces apoptosis in cell OCI-LY10. CLPP-2068 exhibits antitumor activity in mouse xenograft models .
|
-
- HY-106080
-
|
U-63557A free acid
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Furegrelate (U-63557A free acid) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate is being developed as an antiplatelet agent .
|
-
- HY-B0714
-
|
Dexketoprofen tromethamine salt
|
COX
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective COX inhibitor. Dexketoprofen trometamol has a pain-relieving effect, anti-inflammatory effect and anti-cancer effect .
|
-
- HY-108482
-
-
- HY-111143
-
|
|
nAChR
|
Metabolic Disease
|
|
SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA). SCH-900271 has an improved therapeutic window to flushing .
|
-
- HY-143264
-
|
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to research neuropathic pain without causing locomotion impairment .
|
-
- HY-14973
-
|
AMG 853
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC50s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment .
|
-
- HY-16635
-
|
ACT-129968; KYTH-105
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP1 and hEP2 with IC50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis .
|
-
- HY-19393
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
SCH 351591 is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 58 nM. SCH 351591 can inhibit all 4 PDE4 subtypes (A, B, C, and D). SCH 351591 has the potential for the asthma and chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-163697
-
|
|
Wee1
Apoptosis
|
Cancer
|
|
WEE1-IN-7 (compound 12h) is a potent and orally activeWEE1 inhibitor with an IC50 value of 2.1 nM. WEE1-IN-7 induces apoptosis and cell cycle arrest at the S phase. WEE1-IN-7 shows antitumor activity .
|
-
- HY-116399
-
![Cucurbit[8]uril](http://file.medchemexpress.com/product_pic/hy-103689.gif)
