Search Result
Results for "
orally effective
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
19
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-135825
-
|
|
Autophagy
|
Neurological Disease
|
|
TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment .
|
-
-
- HY-112094S
-
|
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
WNK-IN-11-d3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11-d3 is effective at regulating cardiovascular homeostasis[1].
|
-
-
- HY-109127A
-
|
BCX7353 dihydrochloride
|
Ser/Thr Protease
|
Others
|
|
Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE .
|
-
-
- HY-109127
-
|
BCX7353
|
Ser/Thr Protease
|
Others
|
|
Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE .
|
-
-
- HY-145685
-
|
|
Others
|
Cancer
|
|
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer .
|
-
-
- HY-118911
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC50: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors .
|
-
-
- HY-157585S
-
-
-
- HY-137849
-
|
|
PARP
|
Cancer
|
|
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
|
-
-
- HY-B1045
-
-
-
- HY-160019
-
|
|
Deubiquitinase
Mitophagy
|
Neurological Disease
|
|
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
|
-
-
- HY-U00207
-
-
-
- HY-U00363
-
-
-
- HY-70073
-
-
-
- HY-15009
-
-
-
- HY-160701
-
|
|
CDK
|
Cancer
|
|
BLU-222 is an orally effective and selective CDK2 inhibitor. BLU-222 has antitumor activity .
|
-
-
- HY-107456
-
-
-
- HY-10116
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI-540 is a bicyclic thienopyrimidine derivative and an orally active PI3K inhibitor. PI-540 has anti-cancer cell proliferation properties and high tissue distribution. PI-540 can inhibit different isoforms of PI3K, with IC50s of 10 nM (P110α), 3510 nM (P110β), 410 nM (P110δ), and 33110 nM (P110γ). PI-540 also inhibits mTOR (IC50: 61 nM) and DNA-PK (IC50: 525 nM) .
|
-
-
- HY-B1895
-
-
-
- HY-100419
-
|
|
VEGFR
|
Cancer
|
|
BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM .
|
-
-
- HY-U00168
-
-
-
- HY-N11630
-
|
|
Influenza Virus
|
Others
|
|
Pinellic acid is a natural product that could be isolated from a medicinal plant Pinelliae tuber. Pinellic acid is an effective oral adjuvant for nasal influenza vaccine .
|
-
-
- HY-112712
-
|
|
HCV
|
Infection
|
|
Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a .
|
-
-
- HY-W353258
-
|
BAY 12-8039 monohydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Moxifloxacin (BAY 12-8039) hydrochloride monohydrate is an orally active bacterial inhibitor that is effective against Streptococcus pneumoniae. Moxifloxacin hydrochloride monohydrate can be used in tuberculosis research .
|
-
-
- HY-14155
-
|
|
MMP
|
Inflammation/Immunology
|
|
MMP145 (compound 27) is a potent, selective and orally active MMP-12 inhibitor. MMP145 is effective in inflammation and asthma reasearch .
|
-
-
- HY-157250
-
|
|
Apoptosis
|
Endocrinology
|
|
BHD is an effective, orally active and reversible contraceptive agent. BHD induces the apoptosis of spermatogenic cells rapidly and disruptes the blood-testis barrier effectively .
|
-
-
- HY-117281
-
-
-
- HY-148026
-
|
BGB 11417
|
Bcl-2 Family
|
Cancer
|
|
Sonrotoclax is a potent, orally active Bcl2 inhibitor. Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines .
|
-
-
- HY-120864
-
|
|
Wnt
|
Cancer
|
|
SEN461 is a potent and orally active Wnt pathway inhibitor. SEN461 shows effective anti-tumor activity and can be used for GBM research .
|
-
-
- HY-N2486
-
|
|
Fatty Acid Synthase (FASN)
Apoptosis
|
Cancer
|
|
Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects.
|
-
-
- HY-139626
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EPZ-719 is a selective, orally effective SETD2 inhibitor with an IC50 value of 0.005 μM. EPZ-719 has anticancer activity .
|
-
-
- HY-121565
-
|
|
Others
|
Metabolic Disease
Endocrinology
|
|
SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice .
|
-
-
- HY-130750
-
|
|
Reactive Oxygen Species
|
Neurological Disease
|
|
Phycocyanobilin, an orally active antioxidative agent, is an effective scavenger for various reactive oxygen species. Phycocyanobilin can be used for the research of Alzheimer’s disease .
|
-
-
- HY-129826
-
|
|
mAChR
|
Others
|
|
J-104129 is a selective and orally active muscarinic M3 receptor antagonist (Ki = 4.2 nM). J-104129 is effective in promoting bronchodilation .
|
-
-
- HY-14316A
-
|
Ebanicline dihydrochloride; ABT-594 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
|
-
-
- HY-119198
-
|
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
|
NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers .
|
-
-
- HY-B0378A
-
|
RS-10085
|
Angiotensin-converting Enzyme (ACE)
Apoptosis
|
Cardiovascular Disease
|
|
Moexipril hydrochloride (RS-10085) is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril hydrochloride exhibits antihypertensive and neuroprotective effects - .
|
-
-
- HY-B1691
-
|
Hexamine hippurate
|
|
|
|
Methenamine hippurate (Hexamine hippurate) is an orally active urinary antiseptic agent with a wide antibacterial spectrum. Methenamine hippurate is effective against most common urinary tract pathogens .
|
-
-
- HY-14316B
-
|
Ebanicline hydrochloride; ABT-594 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
|
-
-
- HY-156117
-
|
|
STING
|
Cancer
|
|
LB244 is a homologue of BB-Cl-amidine, which is an orally effective STING inhibitor (EC50=0.8 μM) and can be used to inhibit STING-dependent inflammatory diseases. The pharmacokinetic properties of LB244 indicate limited oral activity in mice .
|
-
-
- HY-119480
-
|
|
Bacterial
|
Infection
|
|
Megazol is an orally active antibacterial agent. Megazol has effective inhibitory against T. b. brueei with an EC50 of 0.01 μg/mL. Megazol can be used for the research of protozoan infections .
|
-
-
- HY-17412S
-
|
|
Isotope-Labeled Compounds
Antibiotic
|
Others
|
|
Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor .
|
-
-
- HY-139798
-
|
|
Bacterial
|
Infection
|
|
Iboxamycin is a potent antibiotic candidate bearing a fused bicyclic amino acid residue. Iboxamycin is orally bioavailable, safe and effective in researching both Gram-positive and Gram-negative bacterial infections in mice .
|
-
-
- HY-A0151
-
|
RP 7843; SKF 5883; Thioperazine
|
|
|
|
Thioproperazine (RP 7843) is an orally active antipsychotic agent with calming, antiemetic activity. Thioproperazine is effective in promoting the release of dopamine in rat striatum. Thioproperazine can be used in studies of schizophrenia and bipolar disorder .
|
-
-
- HY-A0093
-
|
KOE-1173 hydrochloride
|
Sodium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research .
|
-
-
- HY-14305A
-
|
|
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 .
|
-
-
- HY-120160
-
|
CP-86325
|
PPAR
|
Neurological Disease
Metabolic Disease
|
|
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
|
-
-
- HY-128571
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia .
|
-
-
- HY-116228
-
|
Caderofloxacin; CS-940
|
Bacterial
|
Infection
|
|
Cadrofloxacin (Caderofloxacin; CS-940), a orally active fluoroquinolone, is effective against aerobic/anaerobic Gram-positive and Gram-negative bacteria. Cadrofloxacin can be used for the research of infectious diseases .
|
-
-
- HY-A0124
-
|
(6R)-BH4; (6R)-Tetrahydro-L-biopterin
|
|
|
|
Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin can be used in study of phenylketonuria (PKU) .
|
-
-
- HY-W011309
-
|
1-O-HDG; HXDG
|
PPAR
PGE synthase
|
Inflammation/Immunology
|
|
1-O-Hexadecylglycerol can up-regulate PPAR-γ expression, inhibit pGE2, and exhibit anti-inflammatory properties . 1-O-Hexadecylglycerol is effective in oral administration .
|
-
- HY-B1916
-
|
Spiramycin B; Spiramycin II; Foromacidin B
|
Antibiotic
Bacterial
Parasite
|
Infection
|
|
Acetylspiramycin (Spiramycin B) is an effective oral macrolide antibiotic produced by Streptomyces, It can inhibit the splenic lymphocyte transformation induced by phytohemagglutinin (PHA), LPS (HY-D1056) and antigen, reduce the procoagulant activity of macrophages, have good antibacterial effect on gram-positive bacteria, and is also an effective antigenic insect agent, which can be used to fight parasitic infection .
|
-
- HY-119816
-
|
|
Others
|
Cardiovascular Disease
|
|
Piretanide is an oral active, relatively safe and effective diuretic. Piretanide has the potential for the research of congestive heart failure with a potential advantage of having potassium-sparing properties. Piretanide can also be used for the research of hypertension [1] [2].
|
-
- HY-120160A
-
|
CP 86325 Sodium
|
PPAR
|
Neurological Disease
Metabolic Disease
|
|
Darglitazone Sodium, a thiazolidinedione, is an orally active, potent, and selective PPAR-γ (peroxisome proliferator-activated receptor) agonist. Darglitazone Sodium is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
|
-
- HY-101234
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
ICI 162846 is an orally active antagonist of H2 receptor. ICI 162846 inhibits acid production accompanied by an increase in the secretion of histamine in chronic duodenal ulcer (CDU) models. ICI 162846 is effective in preventing CDU .
|
-
- HY-10053
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .
|
-
- HY-B0657
-
|
Clodronate
|
Others
|
Others
|
|
Clodronic acid is an orally active bisphosphonate, which is used for researching osteoporosis and diseases associated with excessive bone resorption. Clodronic acid inhibits bone resorption through induction of osteoclast apoptosis. Clodronic acid is effective in the maintenance or improvement of bone mineral density .
|
-
- HY-101946
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
|
-
- HY-19910
-
|
SCYX-7158; AN5568
|
Parasite
|
Infection
|
|
Acoziborole (SCYX-7158) is an effective, safe and orally active antiprotozoal agent for the research of human african trypanosomiasis (HAT). In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 µg/mL .
|
-
- HY-119486
-
|
PF-06649751; CVL-751
|
Dopamine Receptor
|
Neurological Disease
|
|
Tavapadon (PF-06649751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease .
|
-
- HY-B0954A
-
|
|
|
|
|
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm .
|
-
- HY-148494
-
|
FLX475
|
CCR
|
Cancer
|
|
Tivumecirnon (FLX475) is an orally active CCR4 antagonist that blocks regulatory T cells from entering the tumor microenvironment, thereby reducing their interference with effective anti-tumor immune responses. Tivumecirnon has antitumor activity .
|
-
- HY-163374
-
|
|
CDK
|
Cancer
|
|
Cdc7-IN-20 (EP-05) is an orally effective and selective Cdc7 inhibitor with IC50 and Ki values of 0.93 and 0.11 nM, respectively. Cdc7-IN-20 has antitumor activity .
|
-
- HY-A0124A
-
|
(6R)-BH4 dihydrochloride; (6R)-Tetrahydro-L-biopterin dihydrochloride
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin also drives autoimmunity. Sapropterin can be used in study of phenylketonuria (PKU) .
|
-
- HY-B0615A
-
|
EN 313; Ethmozin; Moracizine
|
|
|
|
Moricizine Hydrochloride (EN 313) is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period .
|
-
- HY-155250
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 154 (compound 7) is a derivative of Fluoroqinolones and is an orally effective antibacterial agent. Antibacterial agent 154 inhibits Gram-positive and Gram-negative bacteria. Antibacterial agent 154 demonstrated in vivo efficacy in a mouse model of staphylococcal sepsis .
|
-
- HY-119832
-
|
EGIS-2062 free acid; EGYT-2062 free acid
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Setastine (EGIS-2062 (free acid); EGYT-2062 (free acid) is an orally effective, non-sedative and long acting anti-allergic agent. Setastine possesses potent histamine Hi-receptor blocking properties and can be used for allergies and rhinitis research [1]<.
|
-
- HY-17595
-
|
|
Parasite
Apoptosis
Microtubule/Tubulin
|
Infection
Cancer
|
|
Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
|
-
- HY-19447A
-
|
LB80380 maleate
|
HBV
|
Infection
|
|
Besifovir Dipivoxil maleate (LB80380 maleate) is an oral proagent of LB80317. Besifovir Dipivoxil maleate (LB80380 maleate) is effective in hepatitis B virus (HBV) DNA suppression for both treatment-naive and lamivudine-resistant chronic hepatitis B (CHB) patients in preliminary studies [2]
|
-
- HY-B0976
-
|
Th-1165; Phenoterol
|
|
|
|
Fenoterol (Th-1165), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research .
|
-
- HY-13571AS1
-
|
|
Isotope-Labeled Compounds
Glucocorticoid Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Beclometasone dipropionate-d10 is the deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
|
-
- HY-13571AS
-
|
|
Isotope-Labeled Compounds
Glucocorticoid Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Beclometasone dipropionate-d6 is deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
|
-
- HY-116387A
-
|
BRL 6231
|
Dihydrofolate reductase (DHFR)
Parasite
|
Infection
|
|
WR99210 hydrochloride is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 hydrochloride shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains as well as T. gondii .
|
-
- HY-16784
-
|
IDX719; IDX18719
|
HCV
HCV Protease
|
Infection
|
|
Samatasvir (IDX71) is a potent, orally active NS5A inhibitor of HCV replication. Samatasvir is effective and selective against infectious HCV and replicons, with EC50s falling within a tight range of 2 to 24 pM in genotype 1 through 5 replicons .
|
-
- HY-100886
-
|
|
|
|
|
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth .
|
-
- HY-107064
-
|
CGP 9000; Oraspor
|
Bacterial
Antibiotic
|
Infection
|
|
Cefroxadine (CGP 9000) is an orally active cephalosporin antibiotic. Cefroxadine is more effective than cephalexin against Escherichia coli and Klebsiella pneumoniae with MIC values of 3.13 and 1.56 μg/mL respectively with a concentration of 10 6 μg/mL. Cefroxadine can be used for the research of infection .
|
-
- HY-13676
-
|
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
|
-
- HY-112299
-
|
TAS6417; CLN-081
|
EGFR
Apoptosis
|
Cancer
|
|
Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM .
|
-
- HY-B0976A
-
|
Th-1165a; Phenoterol hydrobromide
|
|
|
|
Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research .
|
-
- HY-147268
-
|
RAF/KIN_2787
|
Raf
p38 MAPK
|
Cancer
|
|
Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity .
|
-
- HY-147017
-
|
GSK286
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
GSK2556286 (GSK286) is an orally active inhibitor of M. tuberculosis. GSK2556286 inhibits growth within human macrophages (IC50 = 0.07 μM). GSK2556286 is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and agent-sensitive (DS) M. tuberculosis.
|
-
- HY-100500
-
|
KBT 1585 hydrochloride
|
Penicillin-binding protein (PBP)
Bacterial
|
Cancer
|
|
Lenampicillin hydrochloride (KBT 1585 hydrochloride) is an orally active proagent of Ampicillin and is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins (transpeptidase). Lenampicillin hydrochloride has improved absorption and decreased side effects compares to Ampicillin and is applied in the investigation of the suppurative skin and soft tissue infection .
|
-
- HY-137958A
-
|
AT-511
|
HCV
SARS-CoV
|
Infection
|
|
Bemnifosbuvir (AT-511) is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC90=0.47 μM). Bemnifosbuvir has pangenotypic antiviral activity .
|
-
- HY-145829
-
|
|
JAK
Apoptosis
|
Inflammation/Immunology
|
|
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
|
-
- HY-19490A
-
|
(S)-AQW-051
|
nAChR
|
Neurological Disease
|
|
(S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia .
|
-
- HY-131723
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P450 3A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults .
|
-
- HY-105634A
-
|
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies .
|
-
- HY-W094474
-
|
hydrate/monohydrateortrihydrate
|
GSK-3
Apoptosis
|
Infection
Neurological Disease
|
|
Lithium chloride hydrate, an orally active mood stabilizer, is a potent virus inhibitor and effective immunomodulatory agent. Lithium chloride hydrate has antidepressant activity by inhibiting GSK3β and promoting neurogenesis. Lithium chloride hydrate alleviates cognition dysfunction and the symptoms of acute mania and depression. Lithium chloride hydrate can also be used for research of virus infection and Alzheimer's disease .
|
-
- HY-17412S1
-
|
|
Isotope-Labeled Compounds
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Minocycline-d6 sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.
|
-
- HY-17409
-
|
|
Fungal
Antibiotic
Apoptosis
Bacterial
|
Infection
|
|
Nystatin is an orally active polyene antifungal antibiotic effective against yeast and mycoplasma. Nystatin increases the permeability of plasma membranes to small monovalent ions, including chloridion . Nystatin is a cholesterol-sequestering agent , partially prevents Oxaliplatin-induced lipid raft aggregation, DR4 and DR5 clustering, and thereby reduces apoptosis .
|
-
- HY-B0615AS
-
|
EN 313-d8; Ethmozin-d8; Moracizine-d8
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Moricizine-d8 (Hydrochloride) is the deuterium labeled Moricizine Hydrochloride (HY-B0615A). Moricizine Hydrochloride is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period[1][2].
|
-
- HY-116387
-
WR99210
2 Publications Verification
BRL 6231 free base
|
Dihydrofolate reductase (DHFR)
Parasite
|
Infection
|
|
WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondii .
|
-
- HY-106301
-
|
L-364,718; MK-329
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
|
-
- HY-10053S1
-
|
|
Isotope-Labeled Compounds
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
|
-
- HY-162037
-
|
|
CDK
FLT3
|
Cancer
|
|
CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation .
|
-
- HY-158050
-
|
|
c-Fms
|
|
|
PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC .
|
-
- HY-14532
-
|
CMX001; HDP-CDV
|
CMV
HSV
Orthopoxvirus
|
Infection
|
|
Brincidofovir (CMX001), the lipid-conjugated prodrug of Cidofovir (HY-17438), is an orally available, long-acting antiviral. Brincidofovir shows activity against a broad spectrum of DNA viruses including cytomegalovirus (CMV), adenovirus (ADV), varicella zoster virus, herpes simplex virus, polyomaviruses, papillomaviruses, poxviruses, and mixed double-stranded DNA virus infections. Brincidofovir, an oral antiviral in late stage development, has proven effective against orthopoxviruses in vitro and in vivo. .
|
-
- HY-13011
-
|
CH5424802; RO5424802; RG7853
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-17364
-
Temozolomide
Maximum Cited Publications
109 Publications Verification
NSC 362856; CCRG 81045; TMZ
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects .
|
-
- HY-17593
-
|
CEM-101; OP-1068
|
Bacterial
Antibiotic
|
Infection
|
|
Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis .
|
-
- HY-18754
-
|
|
p38 MAPK
Autophagy
|
Endocrinology
|
|
FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo .
|
-
- HY-122906
-
|
|
c-Fms
|
Inflammation/Immunology
|
|
JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis .
|
-
- HY-13676S
-
|
|
Isotope-Labeled Compounds
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
|
-
- HY-122114
-
|
|
Potassium Channel
|
Neurological Disease
|
|
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects .
|
-
- HY-18641
-
|
|
LPL Receptor
|
Cancer
|
|
Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA1 and LPA3-induced inositol phosphate production with Ki values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo .
|
-
- HY-16770
-
|
P-005672
|
Antibiotic
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne .
|
-
- HY-W749867
-
|
Calcium disodium EDTA dihydrate
|
Bacterial
|
Infection
Others
|
|
CaⅡ-EDTA disodium dihydrate (Calcium disodium EDTA dihydrate) is an orally active metal chelating reagent, exhibits bactericidal activities against periodontal pathogens Aggregatibacter actinomycetemcomitans, Prevotella intermedia and Porphyromonas gingivalis . CaⅡ-EDTA disodium dihydrate is effective chelating antidotes for lead- and cadmium poisoning .
|
-
- HY-B0364A
-
|
Dyclocaine hydrochloride
|
Bacterial
Fungal
Aldehyde Dehydrogenase (ALDH)
|
Infection
Cancer
|
|
Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 µM for ALDH2 and 76 µM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local anesthetic that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain .
|
-
- HY-B0688
-
|
4,4′-Diaminodiphenyl sulfone; DDS
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
- HY-18754A
-
|
FR 167653 sulfate
|
p38 MAPK
Autophagy
|
Endocrinology
|
|
FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo .
|
-
- HY-117048
-
|
PF-04191834
|
Lipoxygenase
|
Inflammation/Immunology
|
|
PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain .
|
-
- HY-13676S1
-
|
|
Isotope-Labeled Compounds
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
|
-
- HY-146466
-
|
|
Others
|
Cancer
|
|
Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition .
|
-
- HY-123801
-
|
GL-II-93
|
GABA Receptor
|
Others
|
|
MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAA receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases .
|
-
- HY-13676R
-
|
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate (Standard) is the analytical standard of Megestrol acetate. This product is intended for research and analytical applications. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
|
-
- HY-13011A
-
|
CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-107429
-
|
PF-04965842
|
JAK
|
Inflammation/Immunology
|
|
Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .
|
-
- HY-B0688S
-
|
4,4′-Diaminodiphenyl sulfone-d8; DDS-d8
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
Cancer
|
|
Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases[2][3][4][5].
|
-
- HY-137958
-
|
AT-527
|
HCV
SARS-CoV
|
Infection
|
|
Bemnifosbuvir hemisulfate (AT-527), a hemisulfate salt of AT-511, a guanosine nucleotide proagent, is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir hemisulfate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC90=0.47 μM). Bemnifosbuvir hemisulfate has pangenotypic antiviral activity .
|
-
- HY-144305
-
|
|
URAT1
GLUT
|
Infection
|
|
KPH2f is a safe, orally active, and effective dual URAT1/GLUT9 inhibitor with IC50s of 0.24 μM and 9.37 μM for URAT1 and GLUT9, respectively. KPH2f shows little effects on OAT1 and ABCG2 (IC50=32.14 and 26.74 μM) .
|
-
- HY-148792
-
|
PRAX-562
|
Sodium Channel
|
Neurological Disease
|
|
Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity .
|
-
- HY-155782
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 blocker muramyl dipeptide (MDP) induces growth of mononuclear cells and induces inflammatory cell factor infection. Zharp2-1 attenuates MDP-induced small inguinal peritonitis, or ameliorates by DNBS-induced large inguinal conjunctivitis .
|
-
- HY-107725A
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIBO3304 (diTFA) is an orally effective and selective neuropeptide Y (NPY) Y1 receptor antagonist. BIBO3304 (diTFA) has a high affinity for both human and rat Y1 receptors, with IC50 values of 0.38 and 0.72 nM, respectively. BIBO3304 (diTFA) promotes bone-tendon healing through the Wnt/β-catenin signaling pathway .
|
-
- HY-B0976AR
-
|
Th-1165a (Standard); Phenoterol hydrobromide (Standard)
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol (hydrobromide) (Standard) is the analytical standard of Fenoterol (hydrobromide). This product is intended for research and analytical applications. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research .
|
-
- HY-50878
-
|
PF-02341066
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-B1156
-
|
Cefradine; SQ-11436
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Cefradine) is a broad-spectrum and orally active cephalosporin. Cephradine is active against both gram-positive and gram-negative pathogens. Cephradine is effective in eradicating most penicillinase-producing organisms. Cephradine has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-108044
-
|
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC50 value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease .
|
-
- HY-144456
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable agent-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model .
|
-
- HY-50878B
-
|
PF-02341066 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
c-Met/HGFR
|
Cancer
|
|
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .
|
-
- HY-10221
-
|
SAHA; Suberoylanilide hydroxamic acid
|
HDAC
Autophagy
Mitophagy
Filovirus
Apoptosis
HPV
|
Infection
Cancer
|
|
Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis . Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification .
|
-
- HY-17364S
-
|
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide-d3 is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
|
-
- HY-B0976AS
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol-d6 (hydrobromide) (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
|
-
- HY-13011S
-
|
CH5424802-d8; RO5424802-d8; AF802-d8
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
- HY-13011S1
-
|
CH5424802-d6; RO5424802-d6; AF802-d6
|
Isotope-Labeled Compounds
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
- HY-107758
-
|
|
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM) .
|
-
- HY-B0688S1
-
|
4,4′-Diaminodiphenyl sulfone-d4; DDS-d4
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
|
-
- HY-15485
-
|
|
Phosphodiesterase (PDE)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma .
|
-
- HY-15790
-
-
- HY-50878S
-
|
PF-02341066-d5
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-B2163
-
|
|
PPAR
Reactive Oxygen Species
STAT
NF-κB
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed .
|
-
- HY-N6973
-
|
|
RANKL/RANK
Apoptosis
|
Inflammation/Immunology
|
|
Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research .
|
-
- HY-128449
-
|
Cefradine monohydrate
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Cefradine) monohydrate is a broad-spectrum and orally active cephalosporin. Cephradine monohydrate is active against both grampositive and gram-negative pathogens and effective in eradicating most penicillinase-producing organisms known to be resistant to penicillin G, penicillin V, and ampicillin. Cephradine monohydrate has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine monohydrate blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-B0648
-
|
17α-Hydroxy-6α-methylprogesterone; U8840
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Medroxyprogesterone (17α-Hydroxy-6α-methylprogesterone) is a synthetic human variant of progesterone that is a progesterone receptor agonist with oral activity. Medroxyprogesterone can induce cell proliferation through the PI3K/Akt signaling pathway. Medroxyprogesterone has an inhibitory effect on atherosclerosis in mice. The progesterone agonist activity of Medroxyprogesterone is less effective than Medroxyprogesterone acetate (HY-B0469) .
|
-
- HY-123639
-
|
N-(2-Phenylethyl)-indomethacin amide
|
COX
|
Inflammation/Immunology
Cancer
|
|
LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC50 of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively .
|
-
- HY-101676
-
|
NID 525
|
Leukotriene Receptor
PPAR
Cytochrome P450
|
Metabolic Disease
|
|
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
|
-
- HY-50878A
-
|
PF-02341066 hydrochloride
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-19719
-
|
ARQ-092
|
Akt
Parasite
|
Infection
Cancer
|
|
Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib is effective against Leishmania .
|
-
- HY-115412
-
|
SAHA-d5; Suberoylanilide hydroxamic acid-d5
|
HDAC
Autophagy
Mitophagy
Filovirus
Apoptosis
HPV
|
Infection
Cancer
|
|
Vorinostat-d5 (SAHA-d5) is the deuterium labeled Vorinostat. Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis . Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification .
|
-
- HY-19719A
-
|
ARQ-092 hydrochloride
|
Akt
Parasite
|
Infection
Cancer
|
|
Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib hydrochloride is effective against Leishmania .
|
-
- HY-B0688S2
-
|
4,4′-Diaminodiphenyl sulfone-13C12; DDS-13C12
|
Isotope-Labeled Compounds
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
- HY-146434
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
TGFβ-IN-2 (Compound 9d) inhibits TGF-β-induced total collagen accumulation in NRK-49F cells with the IC50 of 4.31 μM. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 can be used as a potential effective compound for anti-fibrosis in vivo by oral administration .
|
-
- HY-15196
-
TAK-285
2 Publications Verification
|
EGFR
|
Cancer
|
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) .
|
-
- HY-100769
-
|
YL0919
|
5-HT Receptor
|
Neurological Disease
|
|
Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder .
|
-
- HY-13208
-
|
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
|
IAP
Apoptosis
|
Cancer
|
|
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
|
-
- HY-147531
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 106 (compound 8) is an orally active and potent antibacterial agent with antibiofilm activity. Antibacterial agent 106 shows potent antibacterial effect against multi-agent resistant (MDR)-Gram positive pathogens. Antibacterial agent 106 is highly effective in clearing 99.7% of the intracellular methicillin-resistant S. aureus (MRSA) harbored inside macrophages . Antibacterial agent 106 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-114504
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models .
|
-
- HY-161356
-
|
|
SARS-CoV
|
Infection
|
|
BPR3P0128 is an orally active, non-nucleoside RNA-dependent RNA polymerase (RdRp) inhibitor that has been shown to inhibit the activity of various SARS-CoV-2 variants. The EC50 for SARS-CoV-2 and HCoV-229E are 0.62 µM and 0.14 µM. BPR3P0128 demonstrates effective anti-pancoronavirus activity within the submicromolar range. PR3P0128 shows synergistic antiviral activity when combined with Remdesivir (HY-104077) .
|
-
- HY-112823B
-
|
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
|
-
- HY-112823
-
|
HS-10296
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-120793
-
|
TRB-N0224
|
Ras
Apoptosis
MMP
|
Inflammation/Immunology
Cancer
|
|
CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis .
|
-
- HY-145259
-
|
|
HDAC
Histone Demethylase
|
Cancer
|
|
HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor . HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-112823A
-
|
HS-10296 mesylate
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
|
-
- HY-145260
-
|
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
|
-
- HY-10122
-
|
KAD 3213; KMD 3213
|
Adrenergic Receptor
Bacterial
|
Endocrinology
Cancer
|
|
Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH .
|
-
- HY-10122S
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Endocrinology
Cancer
|
|
Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
|
-
- HY-116673
-
|
|
Histone Acetyltransferase
|
Neurological Disease
|
|
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
|
-
- HY-151260
-
|
|
Beta-secretase
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD) .
|
-
-
-
HY-L061
-
|
|
3489 compounds
|
|
Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.
MCE offers a unique collection of 3489 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.
|
| Cat. No. |
Product Name |
Type |
-
- HY-W353258
-
|
BAY 12-8039 monohydrate
|
Biochemical Assay Reagents
|
|
Moxifloxacin (BAY 12-8039) hydrochloride monohydrate is an orally active bacterial inhibitor that is effective against Streptococcus pneumoniae. Moxifloxacin hydrochloride monohydrate can be used in tuberculosis research .
|
-
- HY-W749867
-
|
Calcium disodium EDTA dihydrate
|
Chelators
|
|
CaⅡ-EDTA disodium dihydrate (Calcium disodium EDTA dihydrate) is an orally active metal chelating reagent, exhibits bactericidal activities against periodontal pathogens Aggregatibacter actinomycetemcomitans, Prevotella intermedia and Porphyromonas gingivalis . CaⅡ-EDTA disodium dihydrate is effective chelating antidotes for lead- and cadmium poisoning .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-112094S
-
|
|
|
WNK-IN-11-d3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11-d3 is effective at regulating cardiovascular homeostasis[1].
|
-
-
- HY-157585S
-
|
|
|
21-Dehydro Budesonide-d8-1 is deuterated labeled dehydrogenated Budesonide (HY-13580). Budesonide is an orally available glucocorticoid receptor agonist with anti-cancer activity. 21-Dehydro Budesonide-d8-1 acts as a probe for glucocorticoid receptors and is used in isotope tracing studies .
|
-
-
- HY-17412S
-
|
|
|
Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor .
|
-
-
- HY-13571AS1
-
|
|
|
Beclometasone dipropionate-d10 is the deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
|
-
-
- HY-13571AS
-
|
|
|
Beclometasone dipropionate-d6 is deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
|
-
-
- HY-17412S1
-
|
|
|
Minocycline-d6 sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.
|
-
-
- HY-B0615AS
-
|
|
|
Moricizine-d8 (Hydrochloride) is the deuterium labeled Moricizine Hydrochloride (HY-B0615A). Moricizine Hydrochloride is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period[1][2].
|
-
-
- HY-10053S1
-
|
|
|
Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
|
-
-
- HY-13676S
-
|
|
Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
|
-
-
- HY-13676S1
-
|
|
Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
|
-
-
- HY-B0688S
-
|
|
|
Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases[2][3][4][5].
|
-
-
- HY-17364S
-
|
|
|
Temozolomide-d3 is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
|
-
-
- HY-B0976AS
-
|
|
|
Fenoterol-d6 (hydrobromide) (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
|
-
-
- HY-13011S
-
|
|
|
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
-
- HY-13011S1
-
|
|
|
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
-
- HY-B0688S1
-
|
|
|
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
|
-
-
- HY-50878S
-
|
|
|
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
-
- HY-B0688S2
-
|
|
|
Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
-
- HY-10122S
-
|
|
|
Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-145259
-
|
|
|
Alkynes
|
|
HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor . HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
