Search Result
Results for "
profile
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- 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 .
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-
-
- 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 .
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-
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- HY-155652
-
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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 .
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-
-
- HY-115494
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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 .
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-
-
- HY-123353
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Neladenoson bialanate; BAY-1067197
|
Adenosine Receptor
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Cardiovascular Disease
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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 .
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-
-
- HY-P9989
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REGN5458
|
CD3
TNF Receptor
|
Cancer
|
Linvoseltamab is a bispecific antibody targeting to both BCMA (TNFRSF17) and CD3 epsilon. Linvoseltamab shows safety profile and encouraging efficacy in relapsed/refractory multiple myeloma (RRMM) models .
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-
-
- HY-146380
-
|
Histone Demethylase
|
Cancer
|
S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC50 of 390 nM and Ki of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells .
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-
-
- HY-10096
-
|
GSK-3
|
Neurological Disease
|
TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .
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-
-
- HY-103112
-
|
5-HT Receptor
|
Neurological Disease
|
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
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-
-
- HY-103112A
-
|
5-HT Receptor
|
Neurological Disease
|
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
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-
-
- HY-103112B
-
|
5-HT Receptor
|
Neurological Disease
|
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
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-
-
- HY-W075766
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Nickel difluoride
|
Biochemical Assay Reagents
|
Others
|
Nickel(II) fluoride (Nickel difluoride) is a fluorinating agent and catalyst suitable for surface treatment of aluminum profiles and the production of inks, fluorescent lamps, and organic synthesis. Nickel(II) fluoride is a kind of biological materials or organic compounds that are widely used in life science research .
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-
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- HY-148254
-
|
Deubiquitinase
|
Cancer
|
8RK64 is a covalent UCHL1 inhibitor (IC50: 0.32 μM) . 8RK64 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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-
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- HY-115721
-
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Parasite
|
Infection
|
Antimalarial agent 2 is a novel orally efficacious antimalarials that suggests a fast in vitro killing profile.
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-
-
- HY-132867
-
|
Pim
|
Cancer
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MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.
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-
-
- HY-N2842
-
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Others
|
Inflammation/Immunology
|
α-Amyrin acetate, a natural triterpenoid, has anti-inflammatory activity, antispasmodic profile and the relaxant effect .
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-
-
- HY-W005178
-
|
Endogenous Metabolite
|
Others
|
Octadecanedioic acid, an endogenous metabolite, is a long-chain dicarboxylic acid that has been found in serum free fatty acid profile in Reye syndrome .
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-
-
- HY-13219
-
-
-
- HY-13829
-
|
HIV
|
Infection
|
BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile .
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-
-
- HY-108711
-
-
-
- HY-108609
-
-
-
- HY-122620
-
|
Thrombopoietin Receptor
|
Inflammation/Immunology
Cancer
|
Hetrombopag is a potent thrombopoietin receptor agonist. Hetrombopag is efficacious and well tolerated with a manageable safety profile. Hetrombopag has the potential for the research of immune thrombocytopenia .
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-
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- HY-P4062
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BIL
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Insulin Receptor
|
Metabolic Disease
|
Insulin peglispro (BIL) is a basal insulin with a flat, prolonged activity profile. Insulin peglispro can exhibit better glycaemic control compared to conventional insulins .
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- HY-111199
-
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FAAH
|
Neurological Disease
|
JP83 is an irreversible fatty acyl amide hydrolase (FAAH) inhibitor with an IC50 of 1.6 nM in competitive activity-based protein profiling (ABPP) experiments .
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-
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- HY-145285
-
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Apelin Receptor (APJ)
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Cardiovascular Disease
|
APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease .
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-
-
- HY-N1798
-
-
-
- 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 .
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-
-
- HY-109555
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HMR 1964
|
Insulin Receptor
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Metabolic Disease
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Insulin glulisine (HMR 1964) is a rapid-acting insulin analogue, it mimics the pharmacokinetic and pharmacodynamic profiles of physiological human insulin. Insulin glulisine can be used for the research of diabetes .
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-
-
- HY-114301
-
|
Sodium Channel
|
Neurological Disease
|
PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
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-
-
- HY-16421
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(-)-DRF 2725; NNC 61-0029
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PPAR
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Metabolic Disease
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Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.
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-
-
- HY-144291
-
|
Dopamine Receptor
|
Neurological Disease
|
LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved agent-agent interactions (DDI) risk profile .
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-
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- HY-135737
-
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Others
|
Others
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Dicaprylyl carbonate, a solid, plant-derived fat, is a dry emollient. Dicaprylyl carbonate has excellent dermatological compatibility and a comprehensive performance profile, such as solubilizing and dispersing ability for sun-care filters .
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-
-
- HY-114301A
-
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Sodium Channel
|
Neurological Disease
|
PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
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-
-
- HY-119926
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Hydroxylupanine
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Others
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Cardiovascular Disease
Neurological Disease
|
13-Hydroxylupanine (Hydroxylupanine) is the typical alkaloid profile of sweet lupins.13-Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle .
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- HY-119926A
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Hydroxylupanine hydrochloride
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Others
|
Cardiovascular Disease
Neurological Disease
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13-Hydroxylupanine Hydroxylupanine is the typical alkaloid profile of sweet lupins. 13-Hydroxylupanine Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle .
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-
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- HY-117690
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family .
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-
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- HY-B2209B
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Vitamin B12a acetate
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Endogenous Metabolite
|
Metabolic Disease
|
Hydroxocobalamin acetate is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the research of vitamin B12 deficiency including pernicious anemia .
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-
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- HY-12883A
-
|
Sodium Channel
|
Neurological Disease
|
PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771 .
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-
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- HY-145362
-
|
LPL Receptor
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Others
|
S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).
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-
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- HY-B2209C
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Vitamin B12a hydrochloride
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Endogenous Metabolite
|
Metabolic Disease
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Hydroxocobalamin hydrochloride is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the research of vitamin B12 deficiency including pernicious anemia .
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- HY-148739
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
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dBRD 9-A is a PROTAC which can selective degrade BRD9. dBRD 9-A improves the bromine domain binding profile and reduces the binding activity of the whole BET family .
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-
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- HY-120802
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AZD-8871; LAS191351
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mAChR
Adrenergic Receptor
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Inflammation/Immunology
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Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile .
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-
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- HY-14305A
-
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p38 MAPK
Autophagy
|
Inflammation/Immunology
|
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease .
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-
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- HY-12352A
-
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STAT
Apoptosis
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Cancer
|
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study .
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-
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- 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 .
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-
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- HY-119402
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BCL6-IN-8c
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Bcl-2 Family
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Cancer
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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 .
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-
-
- HY-D1082
-
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Fluorescent Dye
|
Others
|
5-DTAF is a isomeric fluorescein derivative that directly react with polysaccharides and other alcohols in aqueous solution at pH > 9. The maximum of the 5-DTAF emission profile is at a wavelength of 518 nm after excitation at 488 nm .
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-
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- HY-157132
-
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FAAH
|
Neurological Disease
|
FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 value of 6.7 nM and a Ki value of 5 nM. FAAH-IN-8 has high blood-brain permeability and a significant antioxidant profile with no neurotoxicity .
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-
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- HY-110131
-
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nAChR
|
Neurological Disease
|
A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile .
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-
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- HY-161178
-
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Bacterial
|
Infection
|
LK-60 is a potent DprE1 inhibitor. LK-60 effectively inhibits the proliferation of Mycobacterium tuberculosis. LK-60 has good safety profiles to gut microbiota and human cells .
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-
- HY-120802A
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AZD-8871 saccharinate; LAS191351 saccharinate
|
mAChR
Adrenergic Receptor
|
Infection
Inflammation/Immunology
|
Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile .
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-
- HY-B2209
-
Vitamin B12a
|
Endogenous Metabolite
|
Metabolic Disease
|
Hydroxocobalamin (Vitamin B12a) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia .
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-
- HY-A0147
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OPC-17116; dl-Grepafloxacin
|
Antibiotic
Bacterial
|
Infection
|
Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile .
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-
- HY-B2209A
-
Vitamin B12a monohydrochloride
|
Endogenous Metabolite
|
Metabolic Disease
|
Hydroxocobalamin monohydrochloride (Vitamin B12a monohydrochloride) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia .
|
-
- HY-133145
-
-
- HY-133145A
-
|
Others
|
Inflammation/Immunology
Cancer
|
hDDAH-1-IN-2 is a selective, orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor. hDDAH-1-IN-2 reveals an excellent profile regarding cell toxicity/viability .
|
-
- HY-103006
-
NAI-N3
5 Publications Verification
|
Biochemical Assay Reagents
|
Others
|
NAI-N3 is a RNA acylation reagent that enables RNA purification. NAI-N3 is a dual-function SHAPE (selective 2-hydroxyl acylation and profiling experiment) probe (RNA structure probe and enrichment) .
|
-
- HY-A0147A
-
OPC-17116 hydrochloride; dl-Grepafloxacin hydrochloride
|
Antibiotic
Bacterial
|
Infection
|
Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin hydrochloride has high tissue penetration and a promising pharmacodynamic profile .
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-
- HY-151524
-
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC50 value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies .
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-
- HY-155653
-
|
BCRP
|
Cancer
|
ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) .
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-
- HY-139708
-
|
iGluR
|
Neurological Disease
|
NMDA receptor antagonist-3, a NMDA receptor antagonist, stands out with a remarkable percentage of recovery (40.0%, at 100 μM) and safe toxicological profile in SH-SY5Y and human adipose mesenchymal stem cells.
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-
- HY-111021
-
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LPL Receptor
|
Inflammation/Immunology
|
ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
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-
- HY-111021A
-
|
LPL Receptor
|
Inflammation/Immunology
|
ASP-4058 hydrochloride is a next-generation, selective and orally active agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
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-
- HY-W751418
-
(Z)-2-tetracos-15-enamidoethanesulfonic acid
|
FAAH
|
Neurological Disease
|
N-Nervonoyl taurine ((Z)-2-tetracos-15-enamidoethanesulfonic acid) is a fatty acid-taurine conjugate derived from nervonic acid. N-Nervonoyl taurine is a substrate of fatty acid amide hydrolase (FAAH) discovered during metabolite profiling .
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-
- HY-126943
-
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HDAC
|
Others
|
SAHA-BPyne is an activity-based protein profiling (ABPP) probe for detecting HDAC activity, which covalently labels the proximal proteins through a photoactivation. SAHA-BPyne inhibits HDAC activity in HeLa nuclear lysate with an IC50 of less than 5 μM .
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-
- HY-163505
-
|
Bacterial
|
Others
|
Anti-MRSA agent 11 suppresses fluoroquinolone-sensitive strain USA500 and -resistant MRSA isolate Mu50 (MIC =0.39 μg/mL). Anti-MRSA agent 11 displayes favorable in vivo half-life and safety profiles .
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-
- HY-15985
-
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Akt
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
CTX-0294885 is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
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-
- HY-15985A
-
|
Akt
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
CTX-0294885 hydrochloride is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 hydrochloride is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
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-
- HY-105040
-
LY2140023 hydrate
|
mGluR
|
Neurological Disease
|
Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia .
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-
- HY-N6861
-
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Apoptosis
|
Cancer
|
Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells .
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- HY-106588
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SKI 2053R
|
DNA Alkylator/Crosslinker
|
Cancer
|
Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles .
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-
- HY-114147
-
|
Bacterial
|
Infection
Inflammation/Immunology
|
Tuberculosis inhibitor 3 (compound 2i) displays potent anti-TB activity (MIC < 0.016 μg/mL) against agent-sensitive/resistant MTB strains. Tuberculosis inhibitor 3 (compound 2i) shows acceptable PK profiles with oral bioavailability .
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-
- HY-13556
-
LY353381; SERM III
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
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 .
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-
- 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 .
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-
- HY-149759
-
|
SHP2
ERK
|
Cancer
|
SHP2-IN-23 (compound 30) is an orally active SHP2 inhibitor (IC50=38 nM) with excellent in vivo efficacy and pharmacokinetic profiles. SHP2-IN-23 inhibits ERK phosphorylation with IC50=5 nM .
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-
- HY-101447A
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EPH 116 hydrochloride
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Others
|
Cancer
|
SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability .
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-
- 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 .
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-
- 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 .
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-
- HY-113603
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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 .
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-
- HY-15260C
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BMS-863233 hydrochloride
|
CDK
|
Cancer
|
XL413 (BMS-863233) hydrochloride is an orally active and selective CDC7 inhibitor (IC50=3.4 nM). XL413 hydrochloride has favorable pharmacokinetic profiles and significantly inhibits tumor growth in rodent models. XL413 hydrochloride can be used in cancer research .
|
-
- HY-B2209BR
-
Vitamin B12a acetate (Standard)
|
Endogenous Metabolite
|
Metabolic Disease
|
Hydroxocobalamin (acetate) (Standard) is the analytical standard of Hydroxocobalamin (acetate). This product is intended for research and analytical applications. Hydroxocobalamin acetate is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the research of vitamin B12 deficiency including pernicious anemia .
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-
- HY-108519
-
|
ROCK
|
Neurological Disease
|
AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain .
|
-
- 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-151100
-
|
GPR84
|
Inflammation/Immunology
|
GPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable .
|
-
- HY-P1112
-
-
- HY-145698
-
|
5-HT Receptor
|
Neurological Disease
|
UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT5AR .
|
-
- HY-143889
-
|
CDK
|
Cancer
|
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
|
-
- HY-151561
-
|
Parasite
|
Infection
|
WM382 is an orally active and potent dual plasmepsin IX/X (PMIX/X) inhibitor with IC50 values of 1.4 nM and 0.03 nM, respectively. WM382 has robust in vivo efficacy at multiple stages of the malaria parasite life cycle and an excellent resistance profile .
|
-
- HY-161029
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
T14-A24 is an orally active, reversible, competitive, and selective AChE inhibitor (Ki=22 nM, IC50=6 nM). T14-A24 has benign BBB penetration, remarkable neuroprotective effect, and safe toxicological profile .
|
-
- HY-162113
-
|
Bacterial
|
Infection
|
Antibacterial agent 174 (Compound 5g) is a antibacterial agent. Antibacterial agent 174 has potent anti-infective potential in vivo and appreciable pharmacokinetic profiles. Highly active antibacterial agent 174 has favorable biofilm removal performance, low hemolysis and acceptable mammalian cell toxicity .
|
-
- HY-125840
-
PT2977; MK-6482
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) .
|
-
- HY-138800
-
|
nAChR
|
Neurological Disease
|
Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. Spinosad has an excellent environmental and mammalian toxicological profile. Larvicidal activity .
|
-
- 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-B2209R
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Hydroxocobalamin (Standard) is the analytical standard of Hydroxocobalamin. This product is intended for research and analytical applications. Hydroxocobalamin (Vitamin B12a) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia .
|
-
- HY-107784
-
|
Bacterial
|
Inflammation/Immunology
|
Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis .
|
-
- HY-130251
-
|
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
|
Cancer
|
DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile .
|
-
- HY-P1112A
-
|
Endothelin Receptor
|
Cardiovascular Disease
Neurological Disease
|
Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC50 value of 7.5 nM .
|
-
- HY-152535
-
|
Others
|
Infection
Inflammation/Immunology
|
ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti-mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner .
|
-
- HY-155804
-
|
Necroptosis
RIP kinase
|
Inflammation/Immunology
|
RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor with an IC50 of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species .
|
-
- HY-17552
-
Choline Alfoscerate; Alpha-GPC; L-α-GPC
|
Cholinesterase (ChE)
Endogenous Metabolite
|
Neurological Disease
|
sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia .
|
-
- HY-112613
-
UCB9608
1 Publications Verification
|
PI4K
|
Inflammation/Immunology
|
UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent .
|
-
- HY-120574
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
|
-
- HY-146697
-
|
Trk Receptor
c-Fms
PDGFR
Bcr-Abl
c-Kit
Apoptosis
|
Cancer
|
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .
|
-
- HY-149982
-
-
- HY-18767
-
Ivosidenib
Maximum Cited Publications
10 Publications Verification
AG-120
|
Isocitrate Dehydrogenase (IDH)
|
Metabolic Disease
Cancer
|
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity .
|
-
- HY-126321
-
|
ROR
|
Cancer
|
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy .
|
-
- HY-122051
-
AC1903
1 Publications Verification
|
TRP Channel
|
Metabolic Disease
|
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model .
|
-
- HY-N7539
-
|
Others
|
Metabolic Disease
|
Cognac oil, mainly found in wine lees, has unique fatty acid profiles, including Palmitic acid (59.26%), Linoleic acid (11.92%), Myristic acid (8.97%), Oleic acid (8.3%) and other fatty acids. Cognac oil leads to a general increase in the permeation of R6G (Rhodamine 6G) across all the membranes .
|
-
- HY-112081
-
|
DNA/RNA Synthesis
|
Cancer
|
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .
|
-
- 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-147698
-
|
CDK
Topoisomerase
Apoptosis
|
Cancer
|
ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile .
|
-
- HY-149940
-
|
SARS-CoV
|
Infection
|
SIMR3030 is a potent SARS-CoV-2 PLpro inhibitor with an IC50 value of 0.0399 µg/mL. SIMR3030 shows antiviral activity. SIMR3030 decreases SARS-CoV spike, ORF1b, IFN-α, IL-6 mRNA expression. SIMR3030 exhibits a satisfactory safety profile in mice .
|
-
- HY-161316
-
|
Others
|
Neurological Disease
Metabolic Disease
Cancer
|
NNMT-IN-5 (Compound 3-12) is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50 = 47.9 ± 0.6 nM). NNMT-IN-5 also has an excellent selectivity profile over a panel of human methyltransferases. NNMT-IN-5 can be used for the research of cancer, diabetes, metabolic disorders, and neurodegenerative diseases .
|
-
- HY-158183
-
|
Chloride Channel
|
Others
|
NMD670 is an orally active partial inhibitor of the skeletal muscle-specific chloride channel ClC-1. NMD670 increases muscle excitability in response to movement commands, enhances neuromuscular transmission, restores muscle function and improves muscle mobility. NMD670 has a favorable safety profile and improves muscle function in rats in a MG rat model .
|
-
- HY-132246
-
|
MAGL
|
Neurological Disease
|
WWL123 analogue-1 is an analogue of WWL123. WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM . WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice .
|
-
- HY-100375
-
ALKS 8700; BIIB098
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity .
|
-
- HY-103193
-
Colforsin dapropate hydrochloride
|
Adenylate Cyclase
|
Cardiovascular Disease
|
NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts .
|
-
- HY-16023B
-
EM-343; (Rac)-EM-652
|
Estrogen Receptor/ERR
|
Cancer
|
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380 .
|
-
- HY-114237
-
|
Sodium Channel
|
Neurological Disease
|
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects .
|
-
- HY-16636
-
|
mGluR
|
Neurological Disease
|
ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile . ML337 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-101119
-
|
Estrogen Receptor/ERR
|
Cancer
|
GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models .
|
-
- HY-147918
-
|
DNA/RNA Synthesis
|
Cancer
|
Anticancer agent 73 (compound CIB-3b) is a anticancer agent, potently targeting TAR RNA-binding protein 2 (TRBP) and disrupts its interaction with Dicer. Anticancer agent 73 can rebalance the expression profile of oncogenic or tumor-suppressive miRNAs. Anticancer agent 73 suppresses the proliferation and metastasis of HCC in vitro and in vivo .
|
-
- HY-155074
-
|
EGFR
|
Cancer
|
EGFR-IN-79 (compound 21) is an EGFR inhibior with antitumor activity. EGFR-IN-79 induces ROS-independent apoptosis and EGFR/AKT/mTOR-mediated autophagy. EGFR-IN-79 induces cell death at both proliferating and quiescent zones of EJ28 spheroids. EGFR-IN-79 exhibits safety profile in the zebrafish-based model .
|
-
- HY-158245
-
|
Acetolactate Synthase (ALS)
|
Others
|
Herbicide safener-2 (Compound III-7) is a herbicide safener with the same pharmacokinetic profile as the safener mefenpyr-diethyl (HY-136376). Herbicide safener-2 competitively binds to the acetolactate synthase (ALS) active site with mesosulfuron-methyl (HY-126987). Herbicide safener-2 protects crops against herbicide injury .
|
-
- HY-11048
-
NS11394
3 Publications Verification
|
GABA Receptor
|
Neurological Disease
|
NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .
|
-
- 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-139562
-
|
FXR
|
Metabolic Disease
|
BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis .
|
-
- HY-147547
-
|
Amyloid-β
|
Neurological Disease
|
SV5 is a potent anti-Alzheimer agent. SV5 can significantly protect SHSY-5Y cells against Aβ1-42-induced death. SV5 shows moderate antioxidant and good neuroprotective activities. SV5 shows the high stability in human plasma and the best pharmacological profile .
|
-
- HY-149014
-
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life .
|
-
- HY-143330
-
|
Monoamine Oxidase
|
Neurological Disease
|
MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
|
-
- HY-162121
-
|
Others
|
Cancer
|
Antitumor agent-129 (Compound 68) is a thiazolidin-4-one sulfone derivative and an Osteosarcoma (OS) inhibitor with an IC50 value of 0.217 μM, a half-life of 73.8 min (mouse liver microsome) and an excellent pharmacokinetic profile (in vivo bioavailability F = 115%, intraperitoneal administration). Antitumor agent-129 is a potential candidate for OS research .
|
-
- HY-113430
-
5-Heneicosylresorcinol
|
Fungal
|
Infection
|
5-n-Heneicosylresorcinol (5-Heneicosylresorcinol) is an active n-alkyl(enyl)resorcinols (AR) occurring in cereal products from Colombia. Antifungal activity .
|
-
- HY-12995A
-
|
FLAP
|
Inflammation/Immunology
|
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production .
|
-
- HY-N6652
-
Uracil 1-β-D-arabinofuranoside
|
Others
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties . 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells .
|
-
- HY-135303
-
|
GPR84
|
Inflammation/Immunology
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis . GLPG1205 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-150654
-
|
Histone Methyltransferase
|
Cancer
|
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
|
-
- HY-151813
-
|
Others
|
Cancer
|
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
|
-
- HY-151915
-
|
ATM/ATR
mTOR
|
Cancer
|
ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC50 of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC50 of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects .
|
-
- HY-153855
-
RXC004
|
Wnt
Acyltransferase
Porcupine
|
Cancer
|
Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research .
|
-
- HY-149844
-
|
Fungal
|
Infection
|
S-F24 is an antifungal agent with excellent broad-spectrum. S-F24 inhibits CYP3A4 with an IC50 value of 0.4 μM. S-F24 displays a good safety profile with high selectivity, low hemolytic effects, and low tendency to induce resistance. S-F24 can be used for research on fungal infections .
|
-
- 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-162010
-
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile.
MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors treatment research .
|
-
- HY-163468
-
|
Src
|
Cancer
|
SRC-3-IN-1(compound SI-10) is a steroid receptor coactivator 3 (SRC-3) inhibitor(IC50=3.3 μM). SRC-3-IN-1 has good water solubility, oral bioavailability, and improved selectivity profile. SRC-3-IN-1 can be used in prostate cancer research .
|
-
- HY-137466
-
|
Topoisomerase
|
Cancer
|
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research .
|
-
- HY-138657
-
|
Phosphatase
|
Cancer
|
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model .
|
-
- HY-145294
-
|
ROCK
|
Neurological Disease
|
ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 has good multitarget profile and good tolerability. ROCK2-IN-5 has the potential for thr research of Amyotrophic lateral sclerosis (ALS) with a SOD1 mutation .
|
-
- HY-150550
-
|
COX
|
Inflammation/Immunology
|
COX-2-IN-26 is a potent, selective and orally active COX-2 inhibitor with IC50 values of 10.61, 0.067, 1.96 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-26 shows anti-inflammatory activity. COX-2-IN-26 shows gastrointestinal safety profile .
|
-
- HY-151424
-
|
Proteasome
|
Cancer
|
Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 .
|
-
- HY-151933
-
|
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
|
-
- HY-122229
-
|
HIV
|
Infection
|
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
|
-
- HY-131335
-
|
p38 MAPK
|
Inflammation/Immunology
|
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .
|
-
- HY-124364
-
|
HBV
Cytochrome P450
|
Infection
Metabolic Disease
|
RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes. RO6889678 is metabolized by a combination of CYP3A4-mediated oxidation and UDP-glucuronosyltransferase UGT1A3- and UGT1A1-mediated direct glucuronidation .
|
-
- HY-150023
-
|
EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
|
Cancer
|
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
|
-
- HY-155518
-
|
IRAK
|
Inflammation/Immunology
|
IRAK4-IN-25 (compound 38) is an orally acitve and potent IRAK4 inhibitor (IC50=7.3 nM), with low clearance (Cl=12 mL/min/kg). IRAK4-IN-25 inhibits production of pro-inflammatory cytokines, and shows in vitro safety and ADME profiles. IRAK4-IN-25 can be used for research in inflammatory and autoimmune disorders .
|
-
- HY-156793
-
|
Others
|
Others
|
hRIO2 kinase ligand-1 (com 9) is a ligand of hRIO2 kinase, with a Kd value of 520 nM .
|
-
- HY-128656
-
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders .
|
-
- HY-137464A
-
OATD-01
1 Publications Verification
|
Others
|
Inflammation/Immunology
|
OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research .
|
-
- HY-155992
-
|
Sigma Receptor
|
Neurological Disease
|
WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
|
-
- HY-155489
-
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
|
-
- 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-136576
-
|
LPL Receptor
Drug Metabolite
|
Inflammation/Immunology
|
RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC50=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile .
|
-
- HY-125881
-
|
LPL Receptor
|
Inflammation/Immunology
|
ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile .
|
-
- HY-126250
-
|
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
|
NPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death . NPD-1335 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-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-136205
-
Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide
|
TRP Channel
|
Infection
Inflammation/Immunology
|
IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel (TRPC) agonist and has the potential for the study of respiratory infection . IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling . IA-Alkyne 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-17552S
-
Choline Alfoscerate-d9; Alpha-GPC-d9; L-α-GPC-d9
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
Endogenous Metabolite
|
Neurological Disease
|
sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
|
-
- HY-10063
-
TC-1734; ACD3480
|
nAChR
|
Neurological Disease
|
Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
|
-
- HY-139602
-
|
Flavivirus
Dengue virus
Virus Protease
|
Infection
|
(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .
|
-
- HY-150680
-
|
SARS-CoV
Histone Methyltransferase
DNA Methyltransferase
|
Infection
|
SARS-CoV-2 nsp14-IN-1 (Compound 3) is a prototypic bisubstrate inhibitor of SARS-CoV-2 Nsp14 MTase with an IC50 value of 0.061 μM. SARS-CoV-2 nsp14-IN-1 (Compound 3) has an excellent selectivity profile over a panel of human methyltransferases, can against apanel of 10 human MTases including histone lysine, proteinarginine, and DNA and RNA MTases .
|
-
- HY-151872
-
|
HDAC
Ferroptosis
|
Cancer
|
HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI50~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 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-157928
-
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
|
-
- HY-105048A
-
|
Bacterial
|
Infection
|
Omiganan pentahydrochloride is a cationic peptide compound with a broad antibacterial profile. Omiganan pentahydrochloride is capable of inhibiting a variety of bacteria, including yeast, and is active against both gram-positive and gram-negative bacteria. Omiganan pentahydrochloride is able to interact with the bacterial cell membrane, causing the destruction of the cell membrane and the death of the bacteria. Omiganan pentahydrochloride can be used for the study of antimicrobial activity against pathogens commonly associated with catheter-associated infections, including strains with drug-resistant phenotypes .
|
-
- HY-120965
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Several different arachidonoyl amino acids, including N-arachidonoyl dopamine (NADA) and N-arachidonoyl serine (ARA-S), have been isolated and characterized from bovine brain.1 During mass spectral lipidomic analysis of rat brain, a series of fatty acyl amides of a third amino acid, taurine, is discovered. N-Palmitoyl taurine is a prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling. Its function is currently under investigation.
|
-
- HY-136528
-
|
Deubiquitinase
Apoptosis
|
Cancer
|
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells .
|
-
- HY-101144
-
TCD-717
|
Others
|
Cancer
|
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .
|
-
- HY-108417
-
|
STAT
JAK
Bcr-Abl
|
Cancer
|
Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors .
|
-
- HY-144437
-
|
TGF-β Receptor
|
Cancer
|
ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .
|
-
- HY-146372
-
|
CXCR
|
Cancer
|
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately .
|
-
- HY-155726
-
|
Others
|
Others
|
Cy-FBP/SBPase-IN-1 (compound S5) is a Cy-FBP/SBPase inhibitor, which is an important regulatory enzyme in cyanobacterial photosynthesis. Thus Cy-FBP/SBPase-IN-1 inhibits Calvin cycle and photosystem, and decreases photosynthetic efficiency in cyanobacterial photosynthesis. Cy-FBP/SBPase-IN-1 potently inhibits the growth of cyanobacteria, as well as Synechocystis sp.PCC6803. Cy-FBP/SBPase-IN-1 shows safety profile in human-derived cells and zebrafish models .
|
-
- HY-14330
-
|
Dopamine Receptor
|
Neurological Disease
|
ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
|
-
- HY-103409
-
|
Dopamine Receptor
|
Neurological Disease
|
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
|
-
- HY-147955
-
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
hCAI/II-IN-5 (compound MZ8) is a potent hCA I and hCA II (human carbonic anhydrase isoenzymes I and II) inhibitor, with IC50 values of 37.88 and 45.23 nM, respectively. hCAI/II-IN-5 also shows inhibition profile against α-Glycosidase and AChE, with IC50 values of 48.98 and 420.14 nM, respectively. hCAI/II-IN-5 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy .
|
-
- HY-114947
-
9-Deoxy-9-methylene PGE2
|
Prostaglandin Receptor
|
Metabolic Disease
|
9-deoxy-9-methylene Prostaglandin E2 (9-deoxy-9-methylene PGE2) is a stable, isosteric analog of PGE2. 9-deoxy-9-methylene PGE2 retains the biological profile of PGE2 with fewer side effects. In the rat 9-deoxy-9-methylene PGE2 is equipotent to PGE2 in decreasing blood pressure. It also stimulates the gerbil colon and primate uterus at the same potency as PGE2.
|
-
- HY-146353
-
|
HIV
|
Infection
Inflammation/Immunology
|
HIV-1 inhibitor-29 (compound 14d2) is a potent HIV-1 inhibitor with an EC50 of 2.18 μM for HIV-1 IIIB. HIV-1 inhibitor-29 has high anti-resistance profile toward F227L/V106A strain (EC50 = 0.974 μM), and exhibits low cytotoxicity in MT-4 cells (CC50 = 211 μM). HIV-1 inhibitor-29 can be used for researching AIDS .
|
-
- HY-144122
-
|
HIV
|
Infection
|
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability .
|
-
- HY-147954
-
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy .
|
-
- HY-151161
-
|
EGFR
|
Cancer
|
EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
|
-
- HY-151156
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
|
-
- HY-120964
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Several different arachidonoyl amino acids, including N-arachidonoyl dopamine (NADA) and N-arachidonoyl serine (ARA-S), have been isolated and characterized from bovine brain.1 During mass spectral lipidomic analysis of rat brain, a series of fatty acyl amides of a third amino acid, taurine, is discovered.2 This novel class of compounds is present in kidney and activates members of the transient receptor potential (TRP) family of calcium channels.3 N-Stearoyl taurine is a prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling.
|
-
- HY-147319
-
|
Others
|
Neurological Disease
|
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .
|
-
- HY-155517
-
|
NOD-like Receptor (NLR)
Pyroptosis
|
Inflammation/Immunology
|
INF200 (compound 5) is a sulfonylurea-based inhibitor of NLRP3 and NLRP3-mediated pyroptosis. INF200 has beneficial cardiometabolic effects in rat model of high-fat diet (HFD)-induced metaflammation,and shows anti-inflammatory activity to (10 μM) decreases IL-1β release in human macrophages. INF200 improves glucose and lipid profiles,and attenuates systemic inflammation and biomarkers of cardiac dysfunction (particularly BNP). INF200 also improves myocardial damage-dependent ischemia/reperfusion injury (IRI) in hemodynamic evaluation .
|
-
- HY-124322
-
|
Beta-secretase
|
Neurological Disease
Inflammation/Immunology
|
NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
|
-
- HY-10812
-
|
PI3K
mTOR
|
Cancer
|
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
|
-
- HY-149008
-
|
Amylases
|
Metabolic Disease
Cancer
|
α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease .
|
-
- HY-14362
-
|
ROCK
Ribosomal S6 Kinase (RSK)
|
Cardiovascular Disease
|
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
|
-
- HY-150537
-
|
Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
|
Neurological Disease
|
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-120973
-
|
Biochemical Assay Reagents
|
Others
|
(R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.)
|
-
-
-
HY-L0091V
-
|
981,244 compounds
|
Chemspace Lead-Like Compound Library contains 981,244 in-Stock lead-like compoundswith favorable physicochemical profiles and high Quantitative Estimation of Drug-likeness.
|
-
-
HY-L0093V
-
|
10,119 compounds
|
Diversity-based screening continues to be a vital tool for drug discovery. Efficiency and productivity can be improved by using screening libraries that offer maximum diversity whilst retaining drug-like properties. Chemspace Scaffold derived set composes 10,119 compounds, which including 3,373 scaffolds, 3 compounds per each. This library has exceptional coverage of drug-like chemical space.
|
-
-
HY-L021L
-
|
608 compounds
|
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE provides a unique collection of 608 natural product-like compounds that are structurally like Steroids, Tannins, Flavonoids, Quinones, Isoquinolines, etc. This library is an important source of lead compounds for drug discovery.
|
-
-
HY-L0121V
-
|
10,000 compounds
|
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 10K Natural Product-like Compound Library consists of 10,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
|
Cat. No. |
Product Name |
Type |
-
- HY-D1082
-
|
Fluorescent Dyes/Probes
|
5-DTAF is a isomeric fluorescein derivative that directly react with polysaccharides and other alcohols in aqueous solution at pH > 9. The maximum of the 5-DTAF emission profile is at a wavelength of 518 nm after excitation at 488 nm .
|
Cat. No. |
Product Name |
Type |
-
- HY-W075766
-
Nickel difluoride
|
Biochemical Assay Reagents
|
Nickel(II) fluoride (Nickel difluoride) is a fluorinating agent and catalyst suitable for surface treatment of aluminum profiles and the production of inks, fluorescent lamps, and organic synthesis. Nickel(II) fluoride is a kind of biological materials or organic compounds that are widely used in life science research .
|
-
- HY-120973
-
|
Biochemical Assay Reagents
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(R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.)
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-109555
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HMR 1964
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Insulin Receptor
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Metabolic Disease
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Insulin glulisine (HMR 1964) is a rapid-acting insulin analogue, it mimics the pharmacokinetic and pharmacodynamic profiles of physiological human insulin. Insulin glulisine can be used for the research of diabetes .
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- HY-P4062
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BIL
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Insulin Receptor
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Metabolic Disease
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Insulin peglispro (BIL) is a basal insulin with a flat, prolonged activity profile. Insulin peglispro can exhibit better glycaemic control compared to conventional insulins .
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- HY-P4209
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Peptides
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Others
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Boc-GRR-AMC is a tri-peptide Substrate. Boc-GRR-AMC can be used for a fluorogenic West Nile virus (WNV) substrate, profiling the substrate specificity for the NS2B-NS3 proteases or determining the pH optimum of LdMC activity .
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- HY-P1112
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- HY-P4209A
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Peptides
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Others
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Boc-GRR-AMC (TFA) is a tri-peptide Substrate. Boc-GRR-AMC can be used for a fluorogenic West Nile virus (WNV) substrate, profiling the substrate specificity for the NS2B-NS3 proteases or determining the pH optimum of LdMC activity .
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- HY-P1112A
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Endothelin Receptor
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Cardiovascular Disease
Neurological Disease
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Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC50 value of 7.5 nM .
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- HY-105048A
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Bacterial
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Infection
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Omiganan pentahydrochloride is a cationic peptide compound with a broad antibacterial profile. Omiganan pentahydrochloride is capable of inhibiting a variety of bacteria, including yeast, and is active against both gram-positive and gram-negative bacteria. Omiganan pentahydrochloride is able to interact with the bacterial cell membrane, causing the destruction of the cell membrane and the death of the bacteria. Omiganan pentahydrochloride can be used for the study of antimicrobial activity against pathogens commonly associated with catheter-associated infections, including strains with drug-resistant phenotypes .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P9989
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REGN5458
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CD3
TNF Receptor
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Cancer
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Linvoseltamab is a bispecific antibody targeting to both BCMA (TNFRSF17) and CD3 epsilon. Linvoseltamab shows safety profile and encouraging efficacy in relapsed/refractory multiple myeloma (RRMM) models .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-17552S
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sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
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Cat. No. |
Product Name |
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Classification |
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- HY-148254
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Azide
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8RK64 is a covalent UCHL1 inhibitor (IC50: 0.32 μM) . 8RK64 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-103006
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NAI-N3
5 Publications Verification
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Azide
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NAI-N3 is a RNA acylation reagent that enables RNA purification. NAI-N3 is a dual-function SHAPE (selective 2-hydroxyl acylation and profiling experiment) probe (RNA structure probe and enrichment) .
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- HY-15286
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Alkynes
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Sodium 4-pentynoate is a alkynylacetate analogue, can be metabolically incorporated onto cellular proteins through biosynthetic mechanisms for profiling of acetylated proteins in diverse cell types . Sodium 4-pentynoate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-133870
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ITalk
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Alkynes
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Itaconate-alkyne (ITalk) is a specific bioorthogonal probe for quantitative and site-specific chemoproteomic profiling of Itaconation in living cells. Itaconate-alkyne, a functional analogue of Itaconate, exhibits comparable antiinflammatory effect with Itaconate and enables the labeling of bona fide targets of Itaconate . Itaconate-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-126943
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Alkynes
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SAHA-BPyne is an activity-based protein profiling (ABPP) probe for detecting HDAC activity, which covalently labels the proximal proteins through a photoactivation. SAHA-BPyne inhibits HDAC activity in HeLa nuclear lysate with an IC50 of less than 5 μM .
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- HY-136205
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Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide
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Alkynes
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IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel (TRPC) agonist and has the potential for the study of respiratory infection . IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling . IA-Alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-151872
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Alkynes
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HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI50~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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