Search Result
Results for "
CYPs
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
71
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N4205
-
|
Cytochrome P450
|
Cancer
|
Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM) .
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- HY-156330
-
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HIV
Cytochrome P450
|
Infection
|
HIV-IN-9 (Compound 2b) is a HIV inhibitor (IC50: 6.65 μg/mL), and has high binding affinity with HIV-RT. HIV-IN-9 also inhibits CYP3A4, CYP1A2, CYP2C1, and CYP2D6 .
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- HY-116862
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DBF
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Cytochrome P450
Fluorescent Dye
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Others
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Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 µM (Ex=485nm,Em=535nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
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- HY-149769
-
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Others
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Cancer
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CP-506 (compound 26) is an anticancer compound and a substrate for nitroreductase and CYP oxidoreductases. CP-506 has anticancer activity .
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- HY-N8094
-
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Cytochrome P450
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Others
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Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
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-
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- HY-13600S1
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- HY-129993
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-
-
- HY-W267897
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7-BFC
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Cytochrome P450
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Others
|
7-Benzyloxy-4-(trifluoromethyl)coumarin (7-BFC) is a coumarin fluorescent substrate. 7-Benzyloxy-4-(trifluoromethyl)coumarin is a substrate for cDNA-expressed CYP1A2 and CYP3A4 and is metabolized to 7-hydroxy-4-trifluoromethylcoumarin (HFC). 7-Benzyloxy-4-(trifluoromethyl)coumarin is used for rapid CYP isoform metabolism and inhibition screening studies .
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- HY-163415
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Monoamine Oxidase
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Neurological Disease
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MAO-IN-5 (Compound ZINC000016952895) is a monoamine oxidase (MAO) inhibitor. According to the prediction of Swiss ADME, MAO-IN-5 can inhibit the CYP enzyme family, has blood-brain barrier (BBB) permeability, and has a high gastrointestinal absorption rate. MAO-IN-5 can be used in the study of neurological diseases .
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- HY-143906
-
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URAT1
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Inflammation/Immunology
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URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising agent candidate in the study of hyperuricemia and gout .
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- HY-144286
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CXCR
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Infection
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CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus .
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-
- HY-B0189
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TAK-370; AS-4370
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5-HT Receptor
Cytochrome P450
Potassium Channel
|
Neurological Disease
Cancer
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Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .
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- HY-B0189A
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TAK-370 citrate; AS-4370 citrate
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5-HT Receptor
Potassium Channel
Cytochrome P450
|
Neurological Disease
Cancer
|
Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .
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- HY-N8382
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Cytochrome P450
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Neurological Disease
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Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .
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- HY-151251
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Cytochrome P450
Virus Protease
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Infection
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CYP2C9/CYP2C19-IN-1 (compound 22d) is a potent CYP2C9/CYP2C19 inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C9/CYP2C19-IN-1 can be used in study of anti-ZIKV .
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- HY-151253
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Cytochrome P450
Virus Protease
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Infection
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CYP2C1/CYP2C19-IN-2 (compound 21d) is a potent CYP2C9/CYP2C19 inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C1/CYP2C19-IN-2 can be used in study of anti-ZIKV .
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- HY-13269
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HIV
HIV Integrase
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Infection
Inflammation/Immunology
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BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1) .
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- HY-151809
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Cytochrome P450
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Metabolic Disease
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CYP4A11/CYP4F2-IN-1 is a potent dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 19 nM and 17 nM, respectively. CYP4A11/CYP4F2-IN-1 has potential for the research of renal diseases .
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- HY-Y0110
-
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Endogenous Metabolite
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Others
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2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2).
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- HY-151810
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Cytochrome P450
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Metabolic Disease
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CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseases .
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- HY-155493
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Cytochrome P450
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Cancer
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CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and
aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer .
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- HY-146410
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Angiotensin Receptor
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Others
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AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
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- HY-152079
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Cytochrome P450
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Cancer
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CYP1B1-IN-3 is a potent and selective CYP1B1 inhibitor with IC50 values of 6.6, 347.3, >10000 nM for CYP1B1, CYP1A1, CYP1A2, respectively. CYP1B1-IN-3 inhibits cell migration and invasion. CYP1B1-IN-3 inhibits P-gp, AKT/ERK, FAK/SRC, and EMT pathways .
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- HY-162370
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Cytochrome P450
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Infection
Cancer
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CYP51-IN-16 (compound C6) is a phenylpyrimidine CYP51 inhibitor, and shows antifungal activity in in vitro. CYP51-IN-16 inhibits tumor cell growth .
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- HY-135281
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- HY-144643
-
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Fungal
HDAC
Cytochrome P450
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Inflammation/Immunology
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CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis .
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- HY-149770
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Cytochrome P450
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Metabolic Disease
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CYP4A11/CYP4F2-IN-2 (compound 15) is an orally available inhibitor of CYP4A11/4F2 with IC50s of 120 nM and 220 nM, respectively. CYP4A11/CYP4F2-IN-2 inhibits 20-HETE production in rat kidney and has potential inhibitory effects on diabetic nephropathy and autosomal dominant polycystic kidney disease .
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- HY-133091
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7-O-Ethylumbelliferone
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Cytochrome P450
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Others
|
7-Ethoxycoumarin is a substrate for cytochrome P450(CYP450) and has been used in the functional characterization of various CYPs[1].
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- HY-18642
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PF-4981517
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Cytochrome P450
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Others
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CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on agent metabolism .
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- HY-157170
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- HY-B2015
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- HY-150581
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Cytochrome P450
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Infection
Inflammation/Immunology
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CYP3A4-IN-3 is a high-affinity specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.075 μM. CYP3A4-IN-3 is a ritonavir analogue, but with a simpler structure and twice the inhibitory effect of ritonavir. CYP3A4-IN-3 is used as an antiviral agent and immunosuppressant .
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- HY-118216
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Biloxazol
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Fungal
Cytochrome P450
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Infection
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Bitertanol (Biloxazol) is a potent antifungal agent. Bitertanol also is an CYP1A1, CYP2B, and CYP3A inducer in vivo and an CYP1A inhibitor in vitro .
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- HY-146177
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Bacterial
Cytochrome P450
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Infection
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CYP3A4 enzyme-IN-1 (compound 59) is a potent antibacterial agent, with a MIC of 1 μg/mL for MRSA. CYP3A4 enzyme-IN-1 exhibits low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6, and CYP3A4 enzymes .
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- HY-151140
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Cytochrome P450
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Others
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CYP11B1-IN-2 (compound 7aa) is an orally active, potent and selective CYP11B1 inhibitor, with IC50 values of 9 nM and 25 nM for human CYP11B1 and rat CYP11B1, respectively. CYP11B1-IN-2 can be used for the research of diseases caused by excessive cortisol .
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- HY-N2181A
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Cytochrome P450
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Inflammation/Immunology
Cancer
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DL-Acetylshikonin is a non-selective, reversible cytochrome P450 inhibitor with IC50 values of 1.4-4.0 μM. DL-Acetylshikonin has anti-cancer and anti-inflammatory activities .
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- HY-Y0110S
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Endogenous Metabolite
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Others
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2-Naphthol-d8 is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].
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- HY-Y0110S1
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Endogenous Metabolite
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Others
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2-Naphthol-d7 is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].
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- HY-150580
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Cytochrome P450
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Inflammation/Immunology
Cancer
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CYP3A4-IN-2 is a specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.055 μM. CYP3A4-IN-2 is a ritonavir analogue with increased hydrophobicity of the R2 side group and stronger inhibitory effect compared to ritonavir. CYP3A4-IN-2 can be used as an antiviral agent and immunosuppressants .
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- HY-151254
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Cytochrome P450
Influenza Virus
DNA/RNA Synthesis
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Infection
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CYP2C19-IN-1 (compound 20d) is a potent CYP2C19 inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C19-IN-1 inhibits RNA-dependent RNA polymerase (RdRP) with a Ki value of 6.16 µM. CYP2C19-IN-1 can be used in study of anti-ZIKV .
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- HY-157942
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Cytochrome P450
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Cancer
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CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .
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- HY-146393
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PROTACs
Cytochrome P450
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Cancer
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PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
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- HY-B2015S
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Cytochrome P450
Parasite
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Infection
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Carbosulfan-d18 is the deuterium labeled Carbosulfan. Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
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- HY-101516
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Cytochrome P450
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Cancer
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CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM .
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- HY-149617
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Cytochrome P450
PD-1/PD-L1
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Infection
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CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target (CYP51/PD-L1) inhibitor, with IC50 values of 0.17 and 0.021 μM, respectively. CYP51/PD-L1-IN-4 exhibits excellent antifungal and antidrug-resistant fungal activity in vitro. CYP51/PD-L1-IN-4 can be used for fungal infections research .
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- HY-163359
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Cytochrome P450
HDAC
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Cancer
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CYP17A1/HDAC6-IN-1 (compound 12) is a potent inhibitor of CYP17A1/HDAC6, with IC50 of 0.284μM and 0.6015 μM,respectively. CYP17A1/HDAC6-IN-1 has anti-tumor activity .
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- HY-156530
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Cytochrome P450
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Endocrinology
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CYP11A1-IN-1 (compound 30) is an inhibitor of CYP11A1, with IC50 value of 201-2000 nM. CYP11A1-IN-1 can be used for research in steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer .
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- HY-162051
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Cytochrome P450
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Cancer
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CYP1B1-IN-6 (compound 19) is a fluorescence molecular probes which inhibits CYP1B1 activity. CYP1B1-IN-6 can identify tumor sites in fluorescence imaging and photoacoustic imaging modes .
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- HY-144325
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Cytochrome P450
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Infection
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CYP121A1-IN-1 is a potent CYP121A1 inhibitor with favorable activity against Mycobacterium tuberculosis (H37Rv MIC90∼6.25 μM, ∼2.2 μg/mL). CYP121A1-IN-1 can markedly reduce the production of mycocyclosin via inhibiting the CYP121A1 mediated turnover of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin .
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- HY-157333
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- HY-133091S
-
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Cytochrome P450
Isotope-Labeled Compounds
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Others
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7-Ethoxycoumarin-d5 is deuterium labeled 7-Ethoxycoumarin. 7-Ethoxycoumarin is a substrate for cytochrome P450(CYP450) and has been used in the functional characterization of various CYPs[1].
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- HY-N6023
-
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Cytochrome P450
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Others
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Thermopsoside is a flavone derivative isolated from Aspalathus linearis. Thermopsoside exhibits inhibitory effects on CYP450 isozymes with IC50 values of 6.0 μM, 9.5 μM, 12.0 μM, 32.0 μM, for CYP3A4, CYP2C19, CYP2D6 and CYP2C9, respectively .
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- HY-152118
-
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Cytochrome P450
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Cancer
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CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes .
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- HY-N2071
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Cedrol
1 Publications Verification
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
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Infection
Inflammation/Immunology
Cancer
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Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
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- HY-101284
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DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
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- HY-101285
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DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
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- HY-113482
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1β-OH-DCA
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Endogenous Metabolite
Cytochrome P450
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Metabolic Disease
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1β-Hydroxydeoxycholic acid (1β-OH-DCA), a secondary bile acid, is a CYP3A biomarker. Deoxycholic acid is specifically metabolized into 1β-Hydroxydeoxycholic acid by CYP3A4 and CYP3A7 using recombinant human CYP450 enzymes .
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- HY-N0482
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- HY-N0893S
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- HY-B1184
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Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate .
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- HY-17356
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PPAR
Cytochrome P450
Autophagy
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Cardiovascular Disease
Cancer
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Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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- HY-152159
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Cytochrome P450
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Cancer
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CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo .
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- HY-B0822S1
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GABA Receptor
Cytochrome P450
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Inflammation/Immunology
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Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
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- HY-150574
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Cytochrome P450
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Infection
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CYP3A4-IN-1 (compound 5a) is a potent cytochrome P450 3A4 (CYP3A4) inhibitor with an IC50 value of 0.085 µM .
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- HY-N0319
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Cytochrome P450
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Cancer
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Salvianolic acid C is a noncompetitive Cytochrome P4502C8 (CYP2C8) inhibitor and a moderate mixed inhibitor of Cytochrome P45022J2 (CYP2J2), with Kis of 4.82 μM and 5.75 μM for CYP2C8 and CYP2J2, respectively.
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- HY-N0453
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- HY-148597
-
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FGFR
Cytochrome P450
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Cancer
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FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively .
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- HY-109040
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VT-1129
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Fungal
Cytochrome P450
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Infection
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Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes .
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- HY-150557
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Cytochrome P450
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Cancer
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CYP1B1-IN-1 (Compound 9e) is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 0.49 nM .
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- HY-17356S
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- HY-124527
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HET0016
2 Publications Verification
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Cytochrome P450
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Cardiovascular Disease
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HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth .
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- HY-150558
-
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Cytochrome P450
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Cancer
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CYP1B1-IN-2 (compound 9j) is a potent and selective CYP1B1 (cytochrome P450 1B1) inhibitor, with an IC50 of 0.52 nM .
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- HY-N3090
-
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Cytochrome P450
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Metabolic Disease
|
Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively .
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- HY-152196
-
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Cytochrome P450
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Cancer
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CYP1B1-IN-5 (Compound 6q) is a potent and selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 4.7 nM .
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- HY-B0105
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- HY-135810
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Desethylhydroxychloroquine
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Influenza Virus
Parasite
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Infection
Inflammation/Immunology
|
Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment .
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- HY-156150
-
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Fungal
Cytochrome P450
PD-1/PD-L1
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Infection
|
CYP51/PD-L1-IN-2 (compound L20) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-2 is a dual inhibitor of CYP51 (IC50: 0.263 μM) and PD-L1 (IC50: 0.017 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-2 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
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- HY-156151
-
|
Fungal
Cytochrome P450
PD-1/PD-L1
|
Infection
|
CYP51/PD-L1-IN-3 (compound L21) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-3 is a dual inhibitor of CYP51 (IC50: 0.205 μM) and PD-L1 (IC50: 0.039 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-3 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
|
-
- HY-156149
-
|
Fungal
Cytochrome P450
PD-1/PD-L1
|
Infection
|
CYP51/PD-L1-IN-1 (compound L11) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-1 is a dual inhibitor of CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-1 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
|
-
- HY-153671
-
|
Others
|
Infection
|
4'-Methyl-β-naphthoflavone is a metabolite of Naphthoflavones (benzoflavones) in fungal. Naphthoflavones are activators or inhibitors of CYP-450 .
|
-
- HY-17356S1
-
|
PPAR
Autophagy
Cytochrome P450
|
|
Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].
|
-
- HY-17356R
-
|
PPAR
Cytochrome P450
Autophagy
|
Cardiovascular Disease
Cancer
|
Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
- HY-N5132
-
|
Others
|
Others
|
(-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Foeniculum vulgare. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6 .
|
-
- HY-135644
-
CRV431
|
Sirtuin
|
Cancer
|
Rencofilstat (CRV431) is a pan-cyclophilin inhibitor with IC50 values of 2.5 nM, 3.1 nM, 2.8 nM, 7.3 nM for Cyp A, CypB, Cyp D and Cyp G, respectively. Rencofilstat reduces fibrosis and tumor growth in models of chronic liver disease .
|
-
- HY-N0893
-
-
- HY-13600
-
|
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
Clobetasol propionate is a potent and selective CYP3A5 inhibitor with an IC50 of 0.206 μM. Clobetasol propionate has no inhibiting on CYP3A4 or other major CYPs. Clobetasol propionate is a corticosteroid and has the potential for psoriasis and other dermatoses research .
|
-
- HY-135810A
-
Desethylhydroxychloroquine oxalate
|
Influenza Virus
Parasite
|
Infection
Inflammation/Immunology
|
Cletoquine oxalate (Desethylhydroxychloroquine oxalate) is a major active metabolite of Hydroxychloroquine. Cletoquine oxalate is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine oxalate is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine oxalate has antimalarial effects and has the potential for autoimmune diseases treatment .
|
-
- HY-10505
-
TAK-700
|
Cytochrome P450
|
Cancer
|
Orteronel (TAK-700) is a highly selective inhibitor of human 17,20-lyase (CYP17) with IC50 of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4 .
|
-
- HY-17356G
-
|
Cytochrome P450
PPAR
Autophagy
|
Cardiovascular Disease
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
- HY-135810S
-
Desethylhydroxychloroquine-d4
|
Isotope-Labeled Compounds
Influenza Virus
Parasite
|
Infection
Inflammation/Immunology
|
Cletoquine-d4 is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
|
-
- HY-18063
-
|
Potassium Channel
Cytochrome P450
|
Neurological Disease
|
ML252 is a selective inhibitor of potassium channel, targeting to KCNQ2 channel (Kv7.2) (IC50=69 nM). ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively .
|
-
- HY-B1184S1
-
-
- HY-I0736S
-
|
Drug Metabolite
Endogenous Metabolite
|
Others
|
Isonicotinic acid-d4 is the deuterium labeled Isonicotinic acid[1]. Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochrome P450 (CYP) enzymes, e.g., CYP2C[2].
|
-
- HY-135331
-
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
|
-
- HY-135810S1
-
Desethylhydroxychloroquine-d4-1
|
Isotope-Labeled Compounds
Influenza Virus
Parasite
|
Infection
Inflammation/Immunology
|
Cletoquine-d4-1 is the deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
|
-
- HY-B0105S1
-
Ketoconazol-d4; R 41400-d4
|
Fungal
Cytochrome P450
Ras
|
Infection
Cancer
|
Ketoconazole-d4 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
|
-
- HY-B0105S
-
-
- HY-B1184S2
-
-
- HY-N0598
-
20(S)-Ginsenoside F1
|
Cytochrome P450
Endogenous Metabolite
|
Cancer
|
Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
|
-
- HY-I0736
-
|
Drug Metabolite
Endogenous Metabolite
|
Others
|
Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochrome P450 (CYP) enzymes, e.g., CYP2C .
|
-
- HY-N7266
-
|
Cytochrome P450
Parasite
|
Infection
Cancer
|
Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 µM and 1.4 µM for Trypanosoma brucei (TB) and human CYP51, respectively .
|
-
- HY-130219
-
|
Endogenous Metabolite
|
Others
|
18-HETE (compound 3) is a monooxygenase metabolite of cytochrome P450 (CYP450).18- HETE consists of arachidonic acid bearing a hydroxy substituent at position 18 .
|
-
- HY-B0281AS
-
-
- HY-B0352AS
-
(S)-Org3770 d3; (S)-6-Azamianserin d3
|
5-HT Receptor
|
Neurological Disease
|
(S)-Mirtazapine-d3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].
|
-
- HY-B0852S
-
|
Cytochrome P450
Fungal
|
Infection
|
Tebuconazole-d9 is the deuterium labeled Tebuconazole. Tebuconazole is an agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively.
|
-
- HY-101217
-
|
Cytochrome P450
|
Endocrinology
|
BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.
|
-
- HY-148051
-
-
- HY-RS03434
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP11A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP11A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP11A1 Human Pre-designed siRNA Set A
CYP11A1 Human Pre-designed siRNA Set A
- HY-RS03437
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP17A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP17A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP17A1 Human Pre-designed siRNA Set A
CYP17A1 Human Pre-designed siRNA Set A
- HY-RS03438
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP19A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP19A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP19A1 Human Pre-designed siRNA Set A
CYP19A1 Human Pre-designed siRNA Set A
- HY-RS03439
-
|
Small Interfering RNA (siRNA)
|
Others
|
Cyp19a1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cyp19a1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Cyp19a1 Mouse Pre-designed siRNA Set A
Cyp19a1 Mouse Pre-designed siRNA Set A
- HY-RS03440
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP19A1 Rat Pre-designed siRNA Set A contains three designed siRNAs for CYP19A1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP19A1 Rat Pre-designed siRNA Set A
CYP19A1 Rat Pre-designed siRNA Set A
- HY-RS03441
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP1A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP1A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP1A1 Human Pre-designed siRNA Set A
CYP1A1 Human Pre-designed siRNA Set A
- HY-RS03442
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP1A2 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP1A2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP1A2 Human Pre-designed siRNA Set A
CYP1A2 Human Pre-designed siRNA Set A
- HY-RS03444
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP20A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP20A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP20A1 Human Pre-designed siRNA Set A
CYP20A1 Human Pre-designed siRNA Set A
- HY-RS03445
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP21A2 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP21A2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP21A2 Human Pre-designed siRNA Set A
CYP21A2 Human Pre-designed siRNA Set A
- HY-RS03446
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP24A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP24A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP24A1 Human Pre-designed siRNA Set A
CYP24A1 Human Pre-designed siRNA Set A
- HY-RS03447
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP26A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP26A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP26A1 Human Pre-designed siRNA Set A
CYP26A1 Human Pre-designed siRNA Set A
- HY-RS03450
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP27A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP27A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP27A1 Human Pre-designed siRNA Set A
CYP27A1 Human Pre-designed siRNA Set A
- HY-RS03453
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2A13 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2A13 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2A13 Human Pre-designed siRNA Set A
CYP2A13 Human Pre-designed siRNA Set A
- HY-RS03454
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2A6 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2A6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2A6 Human Pre-designed siRNA Set A
CYP2A6 Human Pre-designed siRNA Set A
- HY-RS03455
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2A7 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2A7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2A7 Human Pre-designed siRNA Set A
CYP2A7 Human Pre-designed siRNA Set A
- HY-RS03470
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP39A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP39A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP39A1 Human Pre-designed siRNA Set A
CYP39A1 Human Pre-designed siRNA Set A
- HY-RS03471
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP3A4 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP3A4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP3A4 Human Pre-designed siRNA Set A
CYP3A4 Human Pre-designed siRNA Set A
- HY-RS03472
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP3A43 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP3A43 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP3A43 Human Pre-designed siRNA Set A
CYP3A43 Human Pre-designed siRNA Set A
- HY-RS03473
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP3A5 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP3A5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP3A5 Human Pre-designed siRNA Set A
CYP3A5 Human Pre-designed siRNA Set A
- HY-RS03474
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP3A7 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP3A7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP3A7 Human Pre-designed siRNA Set A
CYP3A7 Human Pre-designed siRNA Set A
- HY-RS03475
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP46A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP46A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP46A1 Human Pre-designed siRNA Set A
CYP46A1 Human Pre-designed siRNA Set A
- HY-RS03476
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4A11 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4A11 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4A11 Human Pre-designed siRNA Set A
CYP4A11 Human Pre-designed siRNA Set A
- HY-RS03486
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP51A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP51A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP51A1 Human Pre-designed siRNA Set A
CYP51A1 Human Pre-designed siRNA Set A
- HY-RS03487
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP7A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP7A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP7A1 Human Pre-designed siRNA Set A
CYP7A1 Human Pre-designed siRNA Set A
- HY-148595
-
|
Cytochrome P450
|
Cancer
|
Antitumor agent-88 exhibits potent antimitotic activity and arrests cell in the G2/M phase. Antitumor agent-88 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells. Antitumor agent-88 is also a competitive inhibitor of CYP1A1 (Ki: 1.4 μM) .
|
-
- HY-155456
-
|
Cytochrome P450
|
Metabolic Disease
|
CD-6 is a flavonoid CYP2A6 inhibitor (IC50: 1.566 μM). CYP2A6 inhibits the metabolism of nicotine to cotinine, resulting in an increase in the amount of nicotine available in the blood, leading to increased smoking behavior. CD-6 mediates CYP2A6 inhibition and can be used in research on smoking cessation or smoking-related diseases .
|
-
- HY-13600R
-
|
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
Cancer
|
Clobetasol propionate (Standard) is the analytical standard of Clobetasol propionate. This product is intended for research and analytical applications. Clobetasol propionate is a potent and selective CYP3A5 inhibitor with an IC50 of 0.206 μM. Clobetasol propionate has no inhibiting on CYP3A4 or other major CYPs. Clobetasol propionate is a corticosteroid and has the potential for psoriasis and other dermatoses research .
|
-
- HY-16670
-
|
Cytochrome P450
|
Others
|
Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
|
-
- HY-16785B
-
INXN-1001 (S enantiomer); RG-115932 (S enantiomer)
|
Interleukin Related
|
Cancer
|
Veledimex S enantiomer (INXN-1001 S enantiomer) is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5 .
|
-
- HY-W754151
-
|
Isotope-Labeled Compounds
|
Others
|
N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
|
-
- HY-100641
-
Hydroxytolbutamide
|
|
|
4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic .
|
-
- HY-B1184A
-
(+)-Mephenytoin
|
Cytochrome P450
|
Neurological Disease
|
(S)-Mephenytoin ((+)-Mephenytoin) is an anticonvulsive agent. (S)-Mephenytoin is a substrate of the cytochrome P450 (CYP) isoform CYP2C19. (S)-Mephenytoin can be used for the analysis of cytochrome P450 metabolism .
|
-
- HY-RS03435
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP11B1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP11B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP11B1 Human Pre-designed siRNA Set A
CYP11B1 Human Pre-designed siRNA Set A
- HY-RS03436
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP11B2 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP11B2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP11B2 Human Pre-designed siRNA Set A
CYP11B2 Human Pre-designed siRNA Set A
- HY-RS03443
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP1B1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP1B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP1B1 Human Pre-designed siRNA Set A
CYP1B1 Human Pre-designed siRNA Set A
- HY-RS03448
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP26B1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP26B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP26B1 Human Pre-designed siRNA Set A
CYP26B1 Human Pre-designed siRNA Set A
- HY-RS03449
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP26C1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP26C1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP26C1 Human Pre-designed siRNA Set A
CYP26C1 Human Pre-designed siRNA Set A
- HY-RS03451
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP27B1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP27B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP27B1 Human Pre-designed siRNA Set A
CYP27B1 Human Pre-designed siRNA Set A
- HY-RS03452
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP27C1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP27C1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP27C1 Human Pre-designed siRNA Set A
CYP27C1 Human Pre-designed siRNA Set A
- HY-RS03456
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2B6 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2B6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2B6 Human Pre-designed siRNA Set A
CYP2B6 Human Pre-designed siRNA Set A
- HY-RS03457
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2C18 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2C18 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2C18 Human Pre-designed siRNA Set A
CYP2C18 Human Pre-designed siRNA Set A
- HY-RS03458
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2C19 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2C19 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2C19 Human Pre-designed siRNA Set A
CYP2C19 Human Pre-designed siRNA Set A
- HY-RS03459
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2C8 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2C8 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2C8 Human Pre-designed siRNA Set A
CYP2C8 Human Pre-designed siRNA Set A
- HY-RS03460
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2C9 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2C9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2C9 Human Pre-designed siRNA Set A
CYP2C9 Human Pre-designed siRNA Set A
- HY-RS03461
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2D6 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2D6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2D6 Human Pre-designed siRNA Set A
CYP2D6 Human Pre-designed siRNA Set A
- HY-RS03462
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2D7 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2D7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2D7 Human Pre-designed siRNA Set A
CYP2D7 Human Pre-designed siRNA Set A
- HY-RS03463
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2E1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2E1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2E1 Human Pre-designed siRNA Set A
CYP2E1 Human Pre-designed siRNA Set A
- HY-RS03464
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2F1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2F1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2F1 Human Pre-designed siRNA Set A
CYP2F1 Human Pre-designed siRNA Set A
- HY-RS03465
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2J2 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2J2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2J2 Human Pre-designed siRNA Set A
CYP2J2 Human Pre-designed siRNA Set A
- HY-RS03466
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2R1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2R1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2R1 Human Pre-designed siRNA Set A
CYP2R1 Human Pre-designed siRNA Set A
- HY-RS03467
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2S1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2S1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2S1 Human Pre-designed siRNA Set A
CYP2S1 Human Pre-designed siRNA Set A
- HY-RS03468
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2U1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2U1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2U1 Human Pre-designed siRNA Set A
CYP2U1 Human Pre-designed siRNA Set A
- HY-RS03469
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP2W1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2W1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP2W1 Human Pre-designed siRNA Set A
CYP2W1 Human Pre-designed siRNA Set A
- HY-RS03477
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4B1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4B1 Human Pre-designed siRNA Set A
CYP4B1 Human Pre-designed siRNA Set A
- HY-RS03478
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4F11 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4F11 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4F11 Human Pre-designed siRNA Set A
CYP4F11 Human Pre-designed siRNA Set A
- HY-RS03479
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4F12 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4F12 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4F12 Human Pre-designed siRNA Set A
CYP4F12 Human Pre-designed siRNA Set A
- HY-RS03480
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4F2 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4F2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4F2 Human Pre-designed siRNA Set A
CYP4F2 Human Pre-designed siRNA Set A
- HY-RS03481
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4F22 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4F22 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4F22 Human Pre-designed siRNA Set A
CYP4F22 Human Pre-designed siRNA Set A
- HY-RS03482
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4F3 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4F3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4F3 Human Pre-designed siRNA Set A
CYP4F3 Human Pre-designed siRNA Set A
- HY-RS03483
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4V2 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4V2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4V2 Human Pre-designed siRNA Set A
CYP4V2 Human Pre-designed siRNA Set A
- HY-RS03484
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4X1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4X1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4X1 Human Pre-designed siRNA Set A
CYP4X1 Human Pre-designed siRNA Set A
- HY-RS03485
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP4Z1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP4Z1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP4Z1 Human Pre-designed siRNA Set A
CYP4Z1 Human Pre-designed siRNA Set A
- HY-RS03488
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP7B1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP7B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP7B1 Human Pre-designed siRNA Set A
CYP7B1 Human Pre-designed siRNA Set A
- HY-RS03489
-
|
Small Interfering RNA (siRNA)
|
Others
|
CYP8B1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP8B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
CYP8B1 Human Pre-designed siRNA Set A
CYP8B1 Human Pre-designed siRNA Set A
- HY-108938
-
|
Cytochrome P450
Fungal
Parasite
|
Infection
|
SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h) .
|
-
- HY-114759
-
|
Cytochrome P450
|
Neurological Disease
Metabolic Disease
Cancer
|
MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor . MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 μM, respectively . MS-PPOH 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-W040468
-
|
Cytochrome P450
|
Metabolic Disease
|
2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human CYP2B6 inhibitor with an IC50 of 5.1 μM and a Ki of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC50=74 μM), CYP3A (IC50=200 μM) .
|
-
- HY-128920
-
|
Cytochrome P450
|
Cancer
|
Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity . Phortress free base leads to DNA damage and cell cycle arrest .
|
-
- HY-122410
-
|
Cytochrome P450
|
Others
|
Dihydrolanosterol is a subtrate of CYP51 and a cholesterol biosynthesis inhibitor. .
|
-
- HY-116568
-
-
- HY-12946A
-
|
|
|
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
|
-
- HY-12946
-
|
|
|
BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
|
-
- HY-100665
-
OPC-14857; DM-14857
|
5-HT Receptor
|
Neurological Disease
|
Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
|
-
- HY-W355700
-
|
Drug Metabolite
|
Infection
|
1-Oleoyl-2-hydroxy-sn-glycero-3-phosphoethanolamine is the main degradation product of deltamethrin metabolized by the prokaryotic protein (CYP6A14 and CYP6N6) complexes in vitro .
|
-
- HY-19340
-
TMS
5 Publications Verification
(E)-2,3',4,5'-tetramethoxystilbene
|
Cytochrome P450
|
Cancer
|
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .
|
-
- HY-30152
-
-
- 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-N1407
-
|
|
|
Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM .
|
-
- HY-W019847
-
|
Cytochrome P450
|
Infection
Metabolic Disease
|
Azamulin is an irreversible, highly selective inhibitior of human CYP3Aa. Azamulin has CYP3A inhibition activity with IC50 values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection .
|
-
- HY-113575
-
OPC-14857 hydrochloride; DM-14857 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
Dehydroaripiprazole (OPC-14857) hydrochloride is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole hydrochloride. Dehydroaripiprazole hydrochloride has with antipsychotic activity equivalent to Aripiprazole .
|
-
- HY-N0922
-
-
- HY-N2194
-
5-Geranoxypsoralen; Bergamotine; Bergaptin
|
|
|
Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
|
-
- HY-N0043
-
-
- HY-W011235
-
|
5-HT Receptor
Calcium Channel
Drug Metabolite
|
Neurological Disease
|
Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity .
|
-
- HY-B0281A
-
-
- HY-B0693
-
-
- HY-151239
-
AR 00440993
|
Cytochrome P450
|
Cancer
|
ONT-993 is an aliphatic hydroxylated metabolite. ONT-993 inhibits CYP2D6 (IC50=7.9 µM) and causes metabolism-dependent inactivation of CYP3A (KI=1.6 µM) .
|
-
- HY-100386
-
PCR 5332
|
|
|
Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
|
-
- HY-129105
-
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
|
Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
|
-
- HY-119996
-
|
Others
|
Inflammation/Immunology
|
AR-C141990 (Compound 30) is a potent blocker of the monocarboxylate transporter MCT1 with a Ki of 4.8 nM. AR-C141990 (Compound 30) inhibits CYP3A4 and CYP2C9 with IC50 values of 16 μM .
|
-
- HY-N2260
-
(-)-Cephaeline dihydrochloride; NSC 32944
|
Cytochrome P450
|
Infection
|
Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
|
-
- HY-70013
-
CB-7598
|
Cytochrome P450
|
Cancer
|
Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
|
-
- HY-W010195
-
|
Cytochrome P450
|
Others
|
2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM .
|
-
- HY-151437
-
|
Fungal
|
Infection
|
Antifungal agent 40 is an antifungal agent which extends into the narrow hydrophobic pocket II of C.alb. CYP51. Antifungal agent 40 has an inhibitory effect on lanosterol 14α-demethylase (CYP51). Antifungal agent 40 inhibits biofilm formation .
|
-
- HY-120425
-
|
Others
|
Infection
|
Ethiprole is an insecticide.Metabolic sulfones are produced faster than Fipronil (HY-B0822) in CYP3A4-expressing cells and in vivo in mouse brain and liver.Ethiprole's sulfide, sulfoxide, sulfone and desulfinyl derivatives have better biological activity .
|
-
- HY-B0105A
-
-
- HY-156628
-
-
- HY-13463BS
-
AKR-501-d8 hydrochloride; E5501-d8 hydrochloride; YM477-d8 hydrochloride
|
Isotope-Labeled Compounds
Thrombopoietin Receptor
|
Cardiovascular Disease
|
Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A[1][2][3].
|
-
- HY-147807
-
|
HIV
Cytochrome P450
|
Infection
|
HIV-1 inhibitor-40 (Compound 4ab) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an EC50 of 1.9 nM. HIV-1 inhibitor-40 displays weak CYP sensitivity with IC50 values of 5.16 μM and 4.51 μM against CYP2C9 and CYP2C19, respectively. HIV-1 inhibitor-40 has no apparent in vivo acute toxicity .
|
-
- HY-B0352A
-
(S)-Org3770; (S)-6-Azamianserin
|
5-HT Receptor
|
Neurological Disease
|
(S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception. (S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2 .
|
-
- HY-103392
-
BCX2600
|
Cytochrome P450
|
Neurological Disease
|
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively.
|
-
- HY-17643
-
VT-1161
|
|
|
Oteseconazole (VT-1161) is a potent and orally active anti-fungal agent. Oteseconazole potently binds to and inhibits Candida albicans cytochrome P45051 (CYP51) activity (Kd ≤39 nM), shows no obvious effect on human CYP51. Oteseconazole also can be used for the research of dermatophytes .
|
-
- HY-U00048
-
-
- HY-130550
-
-
- HY-N0043R
-
Gypenoside VIII (Standard)
|
NF-κB
COX
Calcium Channel
Cytochrome P450
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
|
-
- HY-14874
-
FYX-051
|
Xanthine Oxidase
Cytochrome P450
|
Metabolic Disease
|
Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
|
-
- HY-B0725S
-
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
|
Doxepin-d3 (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].
|
-
- HY-100665S
-
OPC-14857-d8; DM-14857-d8
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
|
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
|
-
- HY-14531
-
R115866
|
RAR/RXR
Cytochrome P450
Autophagy
|
Inflammation/Immunology
|
Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
|
-
- HY-B0352BS
-
(R)-Org3770 d3; (R)-6-Azamianserin d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
|
(R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
|
-
- HY-155710
-
|
Fungal
|
Infection
|
Antifungal agent 68 (compound 10) is an antifungal agent against Candida and Cryptococcus gattii. Antifungal agent 68 inhibits fungal ergosterol biosynthesis, possibly by targeting lanosterol 14α-demethylase (CYP51). There is an interaction between the imidazole ring of antifungal agent 68 and the heme group of CYP51 .
|
-
- HY-N0693
-
-
- HY-N3769
-
-
- HY-121213
-
|
Cytochrome P450
|
Cancer
|
Erysolin is a CYP1A inhibitor with antigenic toxicity. Erysolin reduces benzo(a)pyrene-induced genotoxicity .
|
-
- HY-100641S
-
Hydroxytolbutamide-d9
|
Potassium Channel
Autophagy
|
Metabolic Disease
Cancer
|
4-Hydroxytolbutamide-d9 is the deuterium labeled 4-Hydroxytolbutamide. 4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic[1][2].
|
-
- HY-70013S
-
CB-7598-d4
|
Cytochrome P450
|
Cancer
|
Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
|
-
- HY-100665R
-
OPC-14857 (Standard); DM-14857 (Standard)
|
5-HT Receptor
|
Neurological Disease
|
Dehydroaripiprazole (Standard) is the analytical standard of Dehydroaripiprazole. This product is intended for research and analytical applications. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
|
-
- HY-B0852
-
|
Cytochrome P450
Fungal
Apoptosis
|
Infection
|
Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells .
|
-
- HY-100386S
-
PCR 5332-d4
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cardiovascular Disease
|
Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].
|
-
- HY-10882
-
-
- HY-N0370
-
5-Methoxypsoralen
|
Cytochrome P450
Autophagy
|
Cancer
|
Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
|
-
- HY-N1201
-
-
- HY-N0779
-
Isosilybinin
|
Cytochrome P450
|
Cancer
|
Isosilybin (Isosilybinin) is a flavonoid from Silybum marianum; inhibits CYP3A4 induction with an IC50 of 74 μM.
|
-
- HY-W008772
-
|
Drug Metabolite
|
Others
|
4-Hydroxymephenytoin is a metabolism of an antiepileptic agent mephenytoin, which is used as a CYP2C19 substrate.
|
-
- HY-W011956
-
-
- HY-122277
-
-
- HY-N12530
-
-
- HY-151485
-
|
Parasite
|
Infection
|
Anti-infective agent 5 (compound 74) is an orally active inhibitor of Trypanosoma cruzi with an IC50 value of 0.10 μM. Anti-infective agent 5 effectively reduces parasite burden in vivo. Anti-infective agent 5 can be used for the research of infection .
|
-
- HY-N4110
-
|
Cytochrome P450
|
Metabolic Disease
|
Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79 μM and 6.16 μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54 μM and 18.02 μM, respectively .
|
-
- HY-147810
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT7 receptor ligand 1 (Compound 5c) is a 5-HT7 receptor ligand with a Ki of 8 nM. 5-HT7 receptor ligand 1 is not hepatotoxic and exhibit moderate potential interaction with other agents metabolized by CYP3A4 or CYP2D6 .
|
-
- HY-N0921
-
(+)-Dihydromethysticin
|
Cytochrome P450
|
Inflammation/Immunology
|
Dihydromethysticin is one of the six major kavalactones found in the kava plant; has marked activity on the induction of CYP3A23.
|
-
- HY-103223
-
NSC 710305
|
Cytochrome P450
|
Cancer
|
Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1 .
|
-
- HY-116643
-
-
- HY-N12529
-
-
- HY-100243A
-
(±)-Norcisapride; rel-Ticalopride
|
Others
|
Neurological Disease
|
Norcisapride is a metabolite of cisapride (HY-14149). Norcisapride can be converted into UNK under CYP3A4 .
|
-
- HY-135161
-
|
Drug Metabolite
|
Others
|
EDDP perchlorate is an N-desmethyl metabolite of Methadone by intestinal, hepatic, and cytochrome P450 (CYP) 3A4 .
|
-
- HY-N0515
-
|
PPAR
NF-κB
Calcium Channel
|
Cardiovascular Disease
Inflammation/Immunology
|
Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside . Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years .
|
-
- HY-155732
-
|
Parasite
|
Infection
|
NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively .
|
-
- HY-106019C
-
R75251 dihydrochloride
|
Cytochrome P450
RAR/RXR
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties .
|
-
- HY-163324A
-
|
Cytochrome P450
|
Others
|
2-Me PeER is a rhodamine dye-based fluorescent probe that detects CYP3A4 activity. In fluorescence-activated cell sorting (FACS) based on CYP3A4 activity, homogeneous and functional human induced pluripotent stem cell (hiPSC)-derived hepatocytes and intestinal epithelial cells can be obtained with the aid of 2-Me PeER .
|
-
- HY-N0125
-
|
Cytochrome P450
|
Cancer
|
Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
|
-
- HY-111202
-
-
- HY-122410S
-
-
- HY-17508
-
|
Bacterial
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
|
-
- HY-103392S
-
|
Isotope-Labeled Compounds
Cytochrome P450
|
Neurological Disease
|
Stiripentol-d9 is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively[1][2].
|
-
- HY-128859
-
|
Cytochrome P450
|
Metabolic Disease
|
EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively .
|
-
- HY-135390
-
Ro 64-1056
|
Drug Metabolite
|
Cardiovascular Disease
|
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .
|
-
- HY-N2425
-
|
Cholinesterase (ChE)
|
Metabolic Disease
|
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
|
-
- HY-135334
-
|
Drug Metabolite
Btk
Cytochrome P450
|
Cancer
|
ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM .
|
-
- HY-106019
-
R75251
|
Cytochrome P450
RAR/RXR
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties .
|
-
- HY-14874S
-
FYX-051-d4
|
Isotope-Labeled Compounds
Xanthine Oxidase
Cytochrome P450
|
Metabolic Disease
|
Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].
|
-
- HY-N0382
-
Norizalpinin; 3,5,7-Trihydroxyflavone
|
Cytochrome P450
Autophagy
|
Cancer
|
Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
|
-
- HY-N7534
-
|
Others
|
Others
|
(+)-Epipinoresinol is a lignan compound. CYP81Q3 specifically catalyzes methylenedioxy bridge (MDB) formation in (+)-Epipinoresinol to produce (+)-Pluviatilol .
|
-
- HY-108881
-
-
- HY-146688
-
|
Cytochrome P450
|
Cancer
|
SYN20028567 is an aromatase (CYP19) inhibitor with an IC50 of 9.4 nM. SYN20028567 can be used for breast cancer research .
|
-
- HY-148375
-
|
Drug Metabolite
|
Others
|
Abiraterone sulfate is a metabolite of Abiraterone (HY-148377). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity .
|
-
- HY-119804
-
|
Cytochrome P450
|
Neurological Disease
|
Licopyranocoumarin is an isoflavonoid that shows CYP3A4 inhibitory activity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities .
|
-
- HY-145546
-
|
Cytochrome P450
|
Metabolic Disease
|
14(15)-EpETE is the epoxide of cytochrome P450 (CYP450) and is involved in the regulation of vascular tone and renal function .
|
-
- HY-N0904
-
Ginsenoside compound K; Ginsenoside K
|
COX
NO Synthase
Cytochrome P450
|
Inflammation/Immunology
|
Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
|
-
- HY-16718
-
PF-00251802
|
Glucocorticoid Receptor
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
|
-
- HY-W008364
-
|
Cytochrome P450
Cannabinoid Receptor
|
Neurological Disease
|
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
|
-
- HY-N1882
-
|
|
|
4,5-Dimethoxycanthin-6-one is a potent and uncompetitive inhibitor of CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 1.7μM and a Ki value of 2.6 μM. 4,5-Dimethoxycanthin-6-one, as an alkaloid, is isolated from the wood of Picrasma quassioides BENNET (Simaroubaceae) .
|
-
- HY-16718A
-
PF-00251802 hydrochloride
|
Glucocorticoid Receptor
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
|
-
- HY-135560
-
Nicotellin
|
Cytochrome P450
|
Neurological Disease
|
Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochrome P-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke .
|
-
- 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-B0852R
-
|
Cytochrome P450
Fungal
Apoptosis
|
Infection
|
Tebuconazole (Standard) is the analytical standard of Tebuconazole. This product is intended for research and analytical applications. Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells .
|
-
- HY-70006
-
TOK-001; VN-124-1
|
Cytochrome P450
|
Cancer
|
Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
|
-
- HY-100901
-
|
Cytochrome P450
|
Metabolic Disease
|
CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
|
-
- HY-100902
-
|
Cytochrome P450
|
Metabolic Disease
|
CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
|
-
- HY-148376
-
|
Drug Metabolite
|
Cancer
|
Abiraterone N-oxide is a metabolite of Abiraterone (HY-148377). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity .
|
-
- HY-121580
-
NN703
|
Cytochrome P450
|
Endocrinology
|
Tabimorelin (NN703) is an orally active growth hormone (GH) secretagogue. Tabimorelin is also a potent inhibitor of CYP3A4 activity .
|
-
- HY-13463B
-
AKR-501 hydrochloride; E5501 hydrochloride; YM477 hydrochloride
|
Thrombopoietin Receptor
|
Cardiovascular Disease
|
Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-117766
-
|
Fungal
Cytochrome P450
|
Infection
|
PC945, a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. PC945 is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively .
|
-
- HY-13463
-
AKR-501; E5501; YM477
|
Thrombopoietin Receptor
|
Inflammation/Immunology
|
Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-13463A
-
AKR-501 maleate; E5501 maleate; YM477 maleate
|
Thrombopoietin Receptor
|
Inflammation/Immunology
|
Avatrombopag maleate (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag maleate mimics the biological activities of TPO. Avatrombopag maleate increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag maleate is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-119647
-
|
COX
Cytochrome P450
|
Others
|
PPOH, a fatty acid derivative, is a selective cyclooxygenase (COX) inhibitor that inhibits arachidonic acid cyclooxygenase activity in renal cortical microsomes. In addition, PPOH acts on CYP4A2 and CYP4A3 with the IC50 values of 22 μM and 6.5 μM, respectively . PPOH 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-155666
-
|
Androgen Receptor
|
Cancer
|
YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC50 value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC50 value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer .
|
-
- HY-75054
-
CB7630
|
Cytochrome P450
|
Cancer
|
Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
|
-
- HY-N2129
-
-
- HY-N2586
-
|
Others
|
Inflammation/Immunology
|
Tenuifoliside C, isolated from polygala tenuifolia willd, significantly inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 .
|
-
- HY-N10421
-
(-)-Dihydrocubebin
|
Others
|
Others
|
Dihydrocubebin is a compound isolated from Piper cubeba as potent and selective inhibitors against cytochrome P450 3A4 (CYP3A4) .
|
-
- HY-163324
-
|
Fluorescent Dye
|
Others
|
2-Me PeER (chloride) is a fluorogenic probe for CYP3A4 activity that can be used in living cells . Ex / Em = 520 / 550 nm
|
-
- HY-15565
-
APD668
1 Publications Verification
|
GPR119
Cytochrome P450
Potassium Channel
|
Metabolic Disease
|
APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
|
-
- HY-114415
-
|
Parasite
|
Infection
|
AWZ1066S is a highly potent, specific and orally active anti-Wolbachia agent with EC50 value of 121 nM. AWZ1066S also is a weak CYP2C9 inhibitor and a weak CYP3A4 inducer with IC50 values of 9.7 μM and 37 uM, respectively. AWZ1066S can be used for the research of tropical diseases such as Onchocerciasis (river blindness) and lymphatic filariasis (elephantiasis) .
|
-
- HY-N7454
-
|
Antibiotic
Bacterial
|
Infection
|
Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
|
-
- HY-N11706
-
(+)-β-Cedrene
|
Fungal
|
Infection
Inflammation/Immunology
|
β-Cedrene ((+)-β-Cedrene) is a sesquiterpene compound that can be isolated from Centaurea kotschyi var. kotschyi and Centaurea kotschyi var. decumbens, exhibiting antibacterial, anti-inflammatory, antispasmodic, tonic, diuretic, sedative, insecticidal, and antifungal activities. β-Cedrene is also a potent competitive inhibitor of the CYP2B6-mediatedbupropion hydroxylase, with a Ki value of 1.6 μM .
|
-
- HY-145786
-
|
Cytochrome P450
|
Cancer
|
Abiraterone decanoate is a potent Abiraterone proagent. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery .
|
-
- HY-120648
-
|
Cytochrome P450
|
Cardiovascular Disease
|
CAY 10434 is a potent CYP4A hydroxylase inhibitor. CAY 10434 improves contractile response to angiotensin II with the maximal contractile response (Emax) 6764 mg .
|
-
- HY-120648A
-
|
Cytochrome P450
|
Cardiovascular Disease
|
CAY 10434 dihydrochloride is a potent CYP4A hydroxylase inhibitor. CAY 10434 dihydrochloride improves contractile response to angiotensin II with the maximal contractile response (Emax) 6764 mg .
|
-
- HY-103540
-
NN703 hemifumarate
|
Cytochrome P450
|
Endocrinology
|
Tabimorelin (NN703) hemifumarate is an orally active growth hormone (GH) secretagogue. Tabimorelin hemifumarate is also a potent inhibitor of CYP3A4 activity .
|
-
- HY-N8354
-
6′,7′-DHB
|
Cytochrome P450
|
Cardiovascular Disease
|
6',7'-Dihydroxybergamottin (6′,7′-DHB) is a furanocoumarin that inhibits CYP3A4 and is found in grapefruit juice and Seville orange juice .
|
-
- HY-163015
-
|
Others
|
Infection
|
RNA polymerase-IN-1 (compound 4) is s DNA-dependent RNA polymerase inhibitor. RNA polymerase-IN-1 inhibits CYP isozymes .
|
-
- HY-163016
-
|
Others
|
Infection
|
RNA polymerase-IN-2 (compound 5) is s DNA-dependent RNA polymerase inhibitor. RNA polymerase-IN-2 inhibits CYP isozymes .
|
-
- HY-U00373
-
-
- HY-112690A
-
Remofovir mesylate
|
Cytochrome P450
|
Metabolic Disease
|
Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
|
-
- HY-111421
-
-
- HY-N0370S
-
-
- HY-101284A
-
|
Others
|
Cancer
|
(E/Z)-DMU2105 is the E/Z isomer of DMU2105 (HY-101284). DMU2105 is a CYP1B1 inhibitor .
|
-
- HY-17459
-
(S)-(+)-Clopidogrel bisulfate; (S)-(+)-Clopidogrel hydrogen sulfate
|
Cytochrome P450
P2Y Receptor
|
Cardiovascular Disease
Cancer
|
Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively . Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation .Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor .
|
-
- HY-A0016S
-
|
mAChR
Sodium Channel
Calcium Channel
Adrenergic Receptor
Cytochrome P450
Autophagy
|
Cardiovascular Disease
|
Dronedarone-d6 (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4[1][2][3][4].
|
-
- HY-N1483
-
|
Potassium Channel
|
Cardiovascular Disease
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
|
-
- HY-117026
-
|
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
|
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
|
-
- HY-119695AS
-
Tenivastatin-d6 ammonium
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Cardiovascular Disease
|
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1].
|
-
- HY-17508S1
-
|
Isotope-Labeled Compounds
|
Others
|
Clarithromycin-d3is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
|
-
- HY-17508R
-
|
Bacterial
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
|
-
- HY-15996B
-
VT-464 (racemate)
|
Cytochrome P450
|
Cancer
|
Seviteronel racemate (VT-464 racemate) is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)inhibition.
|
-
- HY-76316
-
-
- HY-N2262
-
|
|
|
8-Geranyloxypsoralen is a furanocoumarin isolated from grapefruit, acts as a potent inhibitor of P450 3A4 (CYP3A4) with an IC50 of 3.93 μM .
|
-
- HY-N6989
-
|
Cytochrome P450
|
Metabolic Disease
|
Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin is a highly selective probe for human cytochrome P450 2A6 (CYP2A6) .
|
-
- HY-117580
-
OH-PRED
|
Drug Metabolite
|
Inflammation/Immunology
|
16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochrome P450 3A (CYP3A) enzymes .
|
-
- HY-21065
-
Ticrynafen; ANP 3624
|
Others
|
Metabolic Disease
|
Tienilic acid (Ticrynafen; ANP 3624) acts as a diuretic hypotensive agent. However, Tienilic acid induces hepatotoxicity. Tienilic acid is converted into electrophilic metabolites by cytochrome P450 (CYP) in vitro .
|
-
- HY-N0144
-
-
- HY-103687
-
3β-OH-5α-Abi
|
Drug Metabolite
|
Cancer
|
Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal agent, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
|
-
- HY-N0125S
-
-
- HY-D0144
-
Methoxyresorufin
|
Cytochrome P450
|
Others
|
Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate . Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents .
|
-
- HY-16276
-
LCI699
|
Mineralocorticoid Receptor
|
Inflammation/Immunology
Cancer
|
Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS) .
|
-
- HY-B0822
-
|
|
|
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .
|
-
- HY-135334S
-
|
Isotope-Labeled Compounds
Drug Metabolite
Btk
Cytochrome P450
|
Cancer
|
ACP-5862-d4 is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM[1][2].
|
-
- HY-16276A
-
LCI699 phosphate
|
Mineralocorticoid Receptor
|
Cancer
|
Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS) .
|
-
- HY-N0904R
-
Ginsenoside compound K(Standard); Ginsenoside K (Standard)
|
COX
NO Synthase
Cytochrome P450
|
Inflammation/Immunology
|
Ginsenoside C-K (Standard) is the analytical standard of Ginsenoside C-K. This product is intended for research and analytical applications. Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
|
-
- HY-N0494
-
Gentiopicrin
|
Cytochrome P450
HCV
|
Inflammation/Immunology
|
Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 µM and 22.8 µM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.
|
-
- HY-10882S
-
-
- HY-19264
-
|
|
|
264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action .
|
-
- HY-100638
-
NPC
|
|
|
RPR132595A (NPC) is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine .
|
-
- HY-N9434
-
|
Cytochrome P450
|
Metabolic Disease
|
5,7,2',6'-Tetrahydroxyflavone is a natural flavonoid that inhibits hepatic testosterone 6β-hydroxylation (CYP3A4) activity with an IC50 of 7.8 μM .
|
-
- HY-100638A
-
NPC hydrochloride
|
Drug Metabolite
|
Cancer
|
RPR132595A (NPC) hydrochloride is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine .
|
-
- HY-156883
-
|
Cytochrome P450
|
Others
|
Dasatinib analog-1 (compound 5826) inhibits CYP3A4 viability with a Ki value of 5.4 μM. Dasatinib analog-1 blocks the formation of glutathione adducts .
|
-
- HY-N1201R
-
4',5,7-Trihydroxyflavone(Standard); Apigenol(Standard); C.I. Natural Yellow 1 (Standard)
|
Autophagy
Cytochrome P450
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
Apigenin (Standard) is the analytical standard of Apigenin. This product is intended for research and analytical applications. Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
|
-
- HY-10882R
-
|
Fungal
Bacterial
Autophagy
Antibiotic
|
Infection
Cancer
|
Clotrimazole (Standard) is the analytical standard of Clotrimazole. This product is intended for research and analytical applications. Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.
|
-
- HY-N6264
-
-
- HY-N0688
-
|
Cytochrome P450
|
Inflammation/Immunology
|
Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp .
|
-
- HY-105124A
-
Ro 3-4787 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
|
-
- HY-D0145
-
Resorufin ethyl ether
|
Cytochrome P450
NO Synthase
|
Others
|
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
|
-
- HY-113327
-
|
Endogenous Metabolite
|
Cancer
|
1,3,7-Trimethyluric acid is the metabolite of caffeine. The metabolic ratio 1,3,7-Trimethyluric acid to caffeine can be evaluated as a biomarker to describe variability in CYP3A activity in a cohort .
|
-
- HY-107534
-
|
GnRH Receptor
|
Endocrinology
|
AG-045572 is a GnRH receptor antagonist with Kis of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone .
|
-
- HY-B0725
-
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 . Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant .. Doxepin has therapeutic effects in atopic dermatitis,chronic urticarial,can improve cognitive processes, protect central nervous system .. Doxepin has also been proposed as a protective factor against oxidative stress ..
|
-
- HY-141547
-
|
Sodium Channel
Cytochrome P450
|
Inflammation/Immunology
|
Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain .
|
-
- HY-150084
-
(±)14(15)-EET
|
Cytochrome P450
|
Cancer
|
(±)14,15-Epoxyeicosatrienoic acid ((±)14(15)-EET) is the Cytochrome P450 metabolite of arachidonic acid. While CYP3A4 may be involved in breast cancer cell growth, (±)14,15-Epoxyeicosatrienoic acid may promote mitosis and anchorage-dependent cloning through STAT3 affected by CYP3A4. (±)14,15-Epoxyeicosatrienoic acid exhibits STAT3-dependent cell growth promotion and may also participate in the autocrine/paracrine pathway that drives cell growth .
|
-
- HY-N6972
-
|
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
- HY-N0382S
-
-
- HY-130353
-
N-desethylamiodarone hydrochloride; LB 33020 hydrochloride
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM .
|
-
- HY-135335S
-
|
Drug Metabolite
|
Metabolic Disease
|
3'-Hydroxy Repaglinide-d5 is the deuterium labeled 3'-Hydroxy Repaglinide. 3'-Hydroxy Repaglinide is a main CYP2C8 metabolite of Repaglinide[1].
|
-
- HY-10493
-
GS-9350
|
Cytochrome P450
HIV
|
Infection
Cancer
|
Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.
|
-
- HY-137789
-
LY 213829
|
COX
|
Cancer
|
Tazofelone (LY 213829) is a cyclooxygenase-II (COX-II) inhibitor. Tazofelone transform into sulfoxide and quinol metabolites is primarily mediated by CYP3A. Tazofelone can be used for the research of inflammatory bowel disease .
|
-
- HY-W087008
-
|
Cytochrome P450
|
Endocrinology
Cancer
|
7-Hydroxyflavanone is a potent inhibitor of aromatase (CYP19) activity with the IC50 of 65 μM. 7-Hydroxyflavanone exerts various biological effects, including anticarcinogenic, antioxidant and (anti-)estrogenic effects, and modula
|
-
- HY-134217
-
|
Aryl Hydrocarbon Receptor
|
Cancer
|
KYN-101 is a potent, selective and orally active AHR inhibitor. KYN-101 decreases the CYP1A1 mRNA expression. KYN-101 shows anti-cancer activity .
|
-
- HY-N0125R
-
|
Cytochrome P450
|
Cancer
|
Diosmetin (Standard) is the analytical standard of Diosmetin. This product is intended for research and analytical applications. Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
|
-
- HY-135335
-
|
Drug Metabolite
|
Metabolic Disease
|
3'-Hydroxy Repaglinide is a main CYP2C8 metabolite of Repaglinide. Repaglinide is a carbamoylmethyl benzoic acid (CMBA) derivative, which recently has become available for the treatment of type II diabetes .
|
-
- HY-75054S
-
CB7630-d4
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cancer
|
Abiraterone acetate-d4 is the deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
|
-
- HY-151440
-
|
Fungal
|
Infection
|
Antifungal agent 42 is an antifungal agent. Antifungal agent 42 has an inhibitory effect on lanosterol 14α-demethylase (CYP51) of C.alb.. Antifungal agent 42 inhibits biofilm formation .
|
-
- HY-105124
-
-
- HY-14225
-
|
CRFR
Cytochrome P450
|
Neurological Disease
|
BMS-764459 is a CRF1 antagonist. BMS-764459 can be used for the research of neurological disorders such as depression and anxiety. BMS-764459 is also an atypical CYP1A1 inducer .
|
-
- HY-N0382R
-
Norizalpinin (Standard); 3,5,7-Trihydroxyflavone (Standard)
|
Cytochrome P450
Autophagy
|
Cancer
|
Galangin (Standard) is the analytical standard of Galangin. This product is intended for research and analytical applications. Galangin (Norizalpinin) is?an?agonist/antagonist?of the?arylhydrocarbon?receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
|
-
- HY-12594
-
ABT-450; Veruprevir
|
HCV Protease
HCV
SARS-CoV
|
Infection
|
Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor) .
|
-
- HY-117102
-
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
|
-
- HY-17459S
-
(S)-(+)-Clopidogrel bisulfate-d3; (S)-(+)-Clopidogrel-d3 hydrogen sulfate
|
P2Y Receptor
Cytochrome P450
|
|
Clopidogrel-d3 (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate[1]. Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation.Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor[2][3][4][5][6].
|
-
- HY-17459R
-
(S)-(+)-Clopidogrel bisulfate (Standard); (S)-(+)-Clopidogrel hydrogen sulfate (Standard)
|
Cytochrome P450
P2Y Receptor
|
Cardiovascular Disease
Cancer
|
Clopidogrel (hydrogen sulfate) (Standard) is the analytical standard of Clopidogrel (hydrogen sulfate). This product is intended for research and analytical applications. Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively . Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation .Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor .
|
-
- HY-17613
-
KHK7580
|
CaSR
|
Metabolic Disease
|
Evocalcet (KHK7580) is an orally active calcium sensing receptor (CaSR) agonist. Evocalcet inhibits the secretion of parathyroid hormone (PTH) from parathyroid gland cells. Evocalcet can be used for the research of hyperparathyroidism .
|
-
- HY-W008772S
-
|
Drug Metabolite
|
Others
|
4-Hydroxymephenytoin-d3 is the deuterium labeled 4-Hydroxymephenytoin. 4-Hydroxymephenytoin is a metabolism of an antiepileptic agent mephenytoin, which is used as a CYP2C19 substrate[1][2].
|
-
- HY-100331
-
|
|
|
MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.
|
-
- HY-W271064
-
|
Fluorescent Dye
|
Others
|
1-Methylpyrene is a ubiquitous environmental pollutant and rodent carcinogen. Its mutagenic activity depends on sequential activation by various CYP and sulfotransferase (SULT) enzymes. 1-Methylpyrene induces chromosome loss and mitotic disturbance, proba
|
-
- HY-137193
-
|
Drug Metabolite
|
Cancer
|
5,6-Dihydroabiraterone is the metabolism of Abiraterone (HY-70013). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, and shows antitumor activity in CRPC (castration-resistant prostate cancer) .
|
-
- HY-153618
-
|
Fungal
|
Infection
|
Antifungal agent 53 (A03) is a potent inhibitor of Candida albicans CYP51 with antifungal activity. Antifungal agent 53 prevents the formation of fungi biofilms. Antifungal agent 53 also exhibits good safety .
|
-
- HY-116601
-
|
Others
|
Others
|
6-Hydroxywarfarin is a metabolite of (+) -warfarin. 6-Hydroxywarfarin is a weaker vitamin K antagonist. 6-Hydroxywarfarin is metabolized by the cytochrome P450 isomer 2C9 (CYP2C9) .
|
-
- HY-14273
-
BAL-4815; RO-0094815
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
|
Isavuconazole (BAL-4815) is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi. Isavuconazole inhibits ergosterol biosynthesis and results in the disruption of fungal membrane structure and function. Isavuconazole is a moderate inhibitor of CYP3A4.
|
-
- HY-100064
-
|
|
|
O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays .
|
-
- HY-12433
-
-
- HY-113151
-
-
- HY-75054R
-
CB7630 (Standard)
|
Cytochrome P450
|
Cancer
|
Abiraterone acetate (Standard) is the analytical standard of Abiraterone acetate. This product is intended for research and analytical applications. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
|
-
- HY-111052
-
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
|
-
- HY-12594A
-
ABT-450 dihydrate; Veruprevir dihydrate
|
HCV Protease
HCV
SARS-CoV
|
Infection
|
Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor) .
|
-
- HY-148907
-
|
Biochemical Assay Reagents
|
Cancer
|
CS640 is a selective inhibitor of calmodulin-dependent kinases. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, PIP5K1C, MEK5, RIPK4 and MLK3 with IC50 values of 0.08, 0.03, 0.001, 0.001, 11.2, 0.025, 5.69 and 2.75 μM, respectively. CS640 also shows inhibitory effects to CYP450 2C9 and CYP450 2C19 with IC50 values of 6 and 10 μM, respectively .
|
-
- HY-B0822R
-
|
GABA Receptor
Cytochrome P450
Apoptosis
|
Neurological Disease
|
Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .
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-
- HY-B0476
-
Acetophenetidin
|
COX
|
Inflammation/Immunology
|
Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
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-
- HY-15996A
-
VT-464 (R enantiomer)
|
Cytochrome P450
|
Cancer
|
Seviteronel R enantiomer (VT-464 R enantiomer) is the R enantiomer of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM); Seviteronel (VT-464) R enantiomer's activity is unknown.
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-
- HY-19958
-
|
|
|
XEN907 is a potent and spirooxindole blocker of NaV1.7, with an IC50 of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain .
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-
- HY-115493
-
|
CXCR
|
Others
|
TIQ-15 is a potent CXCR4 antagonist with an IC50 value of 6 nM for CXCR4 Ca 2+ flux. TIQ-15 inhibits CYP450 2D6 with an IC50 value of 0.32 μM .
|
-
- HY-118283
-
AG1908
|
Proton Pump
|
Metabolic Disease
|
5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole in plasma. Lansoprazole is metabolized by CYP2C19 forming 5-Hydroxylansoprazole. Lansoprazole is a gastric proton-pump inhibitor and is effective in the treatment of various peptic diseases .
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-
- HY-125598
-
|
Others
|
Others
|
Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochrome P450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin .
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-
- HY-N10344
-
|
Others
|
Cancer
|
Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochrome P450 (CYP) 1A1 activity .
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-
- HY-N9203
-
|
Bacterial
|
Infection
|
Pinobanksin 5-methyl ether can be isolated from Georgian Propolises. Pinobanksin 5-methyl ether has anti-helicobacter activity. Pinobanksin 5-methyl ether is effective inducer of CYP9Q enzyme .
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-
- HY-122277S
-
-
- HY-149977
-
|
Cytochrome P450
|
Cancer
|
Anticancer agent 111 (compound 11) is a potent cytochrome P450 inhibitor with an IC50 value of 3 μM for CYP3A4. Anticancer agent 111 has anticancer activity. Anticancer agent 111 can be used in research of cancer .
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-
- HY-155376
-
|
mTOR
|
Cancer
|
mTOR inhibitor-14 (compound 14c) is a potent mTOR inhibitor. mTOR inhibitor-14 also shows minimal CYP2C8 inhibition. mTOR inhibitor-14 can inhibit tumor growth .
|
-
- HY-155141
-
|
Cytochrome P450
|
Cancer
|
hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .
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-
- HY-B0725R
-
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
Doxepin (Hydrochloride) (Standard) is the analytical standard of Doxepin (Hydrochloride). This product is intended for research and analytical applications. Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 . Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant .. Doxepin has therapeutic effects in atopic dermatitis,chronic urticarial,can improve cognitive processes, protect central nervous system .. Doxepin has also been proposed as a protective factor against oxidative stress ..
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-
- HY-B0352B
-
(R)-Org3770; (R)-6-Azamianserin
|
5-HT Receptor
|
Neurological Disease
|
(R)-Mirtazapine ((R)-Org3770) is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4 .
|
-
- HY-15550
-
-
- HY-N0927
-
Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine
|
|
|
(-)-Isocorypalmine (Tetrahydrocolumbamine), isolated from the crude base fraction of Corydalis chaerophylla, is a dopamine receptor ligand . Recombinant CYP719A21 displays strict substrate specificity and high affinity (Km=4.63 ± 0.71 μM) for (-)-Isocorypalmine .
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-
- HY-111338
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
Tacrine is a potent acetylcholinesterse (AChE) inhibitor (IC50=109 nM), also acting as a CYP1A2 substrate agent. Tacrine exhibits certain hepatotoxicity in some individuals. Tacrine can be used for researching Alzheimer's disease (AD) .
|
-
- HY-100644
-
Trimethoprim 1-N-oxide
|
|
|
Trimethoprim N-oxide (Trimethoprim 1-N-oxide) belongs to human urinary metabolites. Trimethoprim N-oxide is generated by oxidation of nitrogen atoms in the pyrimidine ring. Trimethoprim N-oxide is formed predominantly by CYP1A2 in human liver microsomes .
|
-
- HY-N2625A
-
|
Cytochrome P450
|
Others
|
Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties .
|
-
- HY-A0064
-
(±)-Verapamil hydrochloride; CP-16533-1 hydrochloride
|
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Cardiovascular Disease
|
Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
|
-
- HY-14751
-
SCH619734
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-109619
-
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
|
-
- HY-100238
-
|
|
|
Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
|
-
- HY-136063
-
|
Fungal
Cytochrome P450
|
Infection
|
Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM) .
|
-
- HY-14275
-
Verapamil
Maximum Cited Publications
43 Publications Verification
(±)-Verapamil; CP-16533-1
|
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Metabolic Disease
Cancer
|
Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
|
-
- HY-144285
-
|
CXCR
HIV
|
Inflammation/Immunology
|
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
|
-
- HY-14751A
-
SCH619734 hydrochloride
|
Neurokinin Receptor
|
Neurological Disease
|
Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-152107
-
|
LRRK2
|
Neurological Disease
|
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes .
|
-
- HY-16436
-
SCH619734 hydrochloride hydrate
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-12035
-
AMG-208
1 Publications Verification
|
c-Met/HGFR
Cytochrome P450
|
Cancer
|
AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity .
|
-
- HY-15996
-
VT-464
|
Cytochrome P450
Androgen Receptor
|
Cancer
|
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) and an AR antagonist. Seviteronel demonstrates both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
|
-
- HY-130353S
-
|
Isotope-Labeled Compounds
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
Desethyl Amiodarone-d4 (hydrochloride) is the deuterium labeled Desethylamiodarone hydrochloride. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2][3].
|
-
- HY-130606
-
|
NAMPT
Cytochrome P450
|
Cancer
|
Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively .
|
-
- HY-134772
-
|
STAT
Cytochrome P450
|
Inflammation/Immunology
|
AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research .
|
-
- HY-156799
-
|
Cytochrome P450
|
Others
|
Cholesterol 24-hydroxylase-IN-2 is an inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), with the IC50 of 5.4 nM. Cholesterol 24-hydroxylase-IN-2 can be used in imaging of cholesterol 24-hydroxylase in mammals .
|
-
- HY-149866
-
|
Cytochrome P450
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC50 less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC50: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch .
|
-
- HY-B0258
-
-
- HY-19435A
-
|
iGluR
Cytochrome P450
|
Neurological Disease
|
GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1 .
|
-
- HY-117580S
-
OH-PRED-d3
|
Drug Metabolite
|
Inflammation/Immunology
|
16α-Hydroxyprednisolone-d3 is the deuterium labeled 16α-Hydroxyprednisolone. 16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochrome P450 3A (CYP3A) enzymes[1][2].
|
-
- HY-130353R
-
N-desethylamiodarone (hydrochloride)(Standard); LB 33020 hydrochloride (Standard)
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
Desethylamiodarone (hydrochloride) (Standard) is the analytical standard of Desethylamiodarone (hydrochloride). This product is intended for research and analytical applications. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM .
|
-
- HY-100620
-
APC
|
Topoisomerase
Cholinesterase (ChE)
|
Cancer
|
RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE .
|
-
- HY-B0873
-
|
|
|
Uniconazole, a plant growth retardant, is a potent inhibitor of abscisic acid (ABA) catabolism with an IC50 of 68 nM against ABA 8’-hydroxylase. Uniconazole is a potent competitive inhibitor of CYP707A3 activity with a Ki of 8 nM. Uniconazole evidently inhibits gibberellin biosynthesis, and brassinosteroid biosynthesis is also inhibited to some extent .
|
-
- HY-134039
-
5-Hydroxyxanthotoxin
|
Others
|
Inflammation/Immunology
|
5-Hydroxy-8-methoxypsoralen (5-Hydroxyxanthotoxin) is a metabolite of Xanthotoxin. Xanthotoxin is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight .
|
-
- HY-D0145S
-
Resorufin ethyl ether-d5
|
Isotope-Labeled Compounds
Cytochrome P450
NO Synthase
|
Others
|
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
|
-
- HY-N0692
-
Gomisin-A; TJN-101; Wuweizi alcohol-B
|
Reactive Oxygen Species
Cytochrome P450
Autophagy
|
Cancer
|
Schisandrol B (Gomisin-A) is a major active constituent of Schisandra chinensis with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and CYP3A and also has anti-inflammatory, anti-diabetic and antioxidant activities .
|
-
- HY-B0476S
-
Acetophenetidin-d5
|
COX
|
Inflammation/Immunology
|
Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
|
-
- HY-W087919
-
5-Methylfurfuryl alcohol
|
Others
|
Others
|
5-Methyl-2-furanmethanol is a natural product that can be isolated from the essential oil of D. rupicola Biv.. 5-Methyl-2-furanmethanol also acts as a oxidative product of 2,5 dimethylfuran (DMF) by cytochrome P450 (CYP) .
|
-
- HY-30151S
-
8-Methoxypsoralen-d3; Xanthotoxin-d3; 8-MOP-d3
|
Cytochrome P450
|
|
Methoxsalen-d3 is the deuterium labeled Methoxsalen[1]. Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight[2].
|
-
- HY-N2689
-
(R)-6′,7′-DHB
|
Cytochrome P450
|
Cancer
|
(R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with Kis of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research .
|
-
- HY-B0876
-
4-Methylpyrazole
|
Cytochrome P450
|
Metabolic Disease
|
Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-W008226
-
2,4,6-trihydroxyacetophenone; 1-(2,4,6-Trihydroxyphenyl)ethanone; THAP Monohydrate
|
Cytochrome P450
Bacterial
Antibiotic
|
Infection
Metabolic Disease
|
Phloracetophenone (2,4,6-trihydroxyacetophenone) is the aglycone part of acetophenone glycoside obtained from Curcuma comosa Roxb, with cholesterol-lowering activity. Phloracetophenone enhances cholesterol 7α-hydroxylase (CYP7A1) activity . Phloracetophenone stimulats bile secretion mediated through Mrp2 .
|
-
- HY-149813
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 14 (Compound 8a) is a high affinity P-gp inhibitor. P-gp inhibitor 14 reverses P-gp-mediated multidrug resistance (EC50=48.74 nM). P-gp inhibitor 14 has a weak inhibitory effect on CYP3A4 activity .
|
-
- HY-17614
-
SMT C1100; BMN 195; VOX-C1100
|
Cytochrome P450
|
Others
|
Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM .
|
-
- HY-N5011
-
|
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor .
|
-
- HY-N3841
-
epsilon-Viniferin
|
Cytochrome P450
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol and can be isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity .
|
-
- HY-100064S
-
|
EGFR
|
Cancer
|
O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
|
-
- HY-135111
-
|
Drug Metabolite
|
Infection
Metabolic Disease
Cancer
|
4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
|
-
- HY-100064S1
-
|
Isotope-Labeled Compounds
EGFR
|
Cancer
|
O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
|
-
- HY-144309
-
|
Cytochrome P450
|
Neurological Disease
|
Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective cholesterol 24-hydroxylase (CH24H or CYP46A1) inhibitor (IC50=8.5 nM). Cholesterol 24-hydroxylase-IN-1 can cross blood-brain barrier .
|
-
- HY-B0876A
-
4-Methylpyrazole hydrochloride
|
|
|
Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-148070
-
|
FLT3
FAK
Cytochrome P450
|
Cancer
|
FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC50s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC50 value of 12 nM. FLT3 ligand-2 can be used in the research of cancers .
|
-
- HY-D0146
-
BzRes; 7-Benzyloxyresorufin; 7-Benzyloxyphenoxazone
|
Fluorescent Dye
|
Others
|
Resorufin benzyl ether (BzRes), a fluorogenic enzyme substrate, can be used to detect CYP3A4 enzyme activity. Resorufin benzyl ether modified with a recognizing moiety boronate, can be used for ONOO - detection via a self-immolation mechanism. Ex/Em=530-570 nm/590 nm .
|
-
- HY-148822
-
|
NAMPT
|
Neurological Disease
|
Nampt activator-2 (compound 34) is a potent NAMPT activator, with EC50 of 0.023 μM. Nampt activator-2 shows moderate activity against CYP2C9 (0.060 μM), 2D6 (0.41 μM) and 2C19 (0.59 μM) .
|
-
- HY-B0476S1
-
|
COX
|
Inflammation/Immunology
|
Phenacetin- 13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
|
-
- HY-B0476R
-
Acetophenetidin (Standard)
|
COX
|
Inflammation/Immunology
|
Phenacetin (Standard) is the analytical standard of Phenacetin. This product is intended for research and analytical applications. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
|
-
- HY-110134
-
|
Constitutive Androstane Receptor
|
Metabolic Disease
|
S07662 is a human constitutive androstane receptor (hCAR) inhibitor with an IC50 of 0.7 μM. S07662 recruits the corepressor NCoR in cell-based assays and attenuate the expression of CYP2B6 mRNA in human primary hepatocytes induced by phenytoin (HY-B0448) and CITCO (HY-103244) .
|
-
- HY-B0113S
-
H 16868-d3
|
Proton Pump
Bacterial
Autophagy
|
Infection
Metabolic Disease
Cancer
|
Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
|
-
- HY-B0258S
-
CI-719-d6
|
PPAR
Cytochrome P450
|
Cardiovascular Disease
Metabolic Disease
|
Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
|
-
- HY-133116S
-
|
Adrenergic Receptor
|
Neurological Disease
|
4-Hydroxyatomoxetine-d3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine (Tomoxetine). 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine is a potent and selective noradrenal in re-uptake inhibitor[1].
|
-
- HY-A0064S
-
(±)-Verapamil-d3 hydrochloride; CP-16533-1-d3 hydrochloride
|
Isotope-Labeled Compounds
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Cardiovascular Disease
|
Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research[1][2][3].
|
-
- HY-133116
-
|
Adrenergic Receptor
|
Neurological Disease
|
4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
|
-
- HY-120696
-
ML368
|
Cytochrome P450
Parasite
|
Infection
|
SR9186 (ML368) is a potent CYP3A4 inhibitor with IC50 s for inhibition of midazolam → 1′hydroxymidazolam, testosterone → 6β-hydroxytestosterone, and vincristine → vincristine M1 of 9, 4, and 38 nM, respectively. SR-9186 inhibits liver-stage development of P. falciparum to block ivermectin metabolism .
|
-
- HY-147919
-
|
Fungal
|
Infection
|
Antifungal agent 33 (compound 4e) is a potent antifungal agent. Antifungal agent 33 exhibits remarkable antifungal activity against C. albicans, with a MIC of 16 μg/mL. Antifungal agent 33 shows potent inhibitory activity against Lanosterol 14α-demethylase (CYP51), with an IC50 of 0.19 μg/mL .
|
-
- HY-10493S
-
GS-9350-d8
|
Isotope-Labeled Compounds
HIV
Cytochrome P450
|
Infection
|
Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules .
|
-
- HY-112090
-
|
Epigenetic Reader Domain
HIV
|
Infection
Inflammation/Immunology
Cancer
|
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .
|
-
- HY-123777
-
|
Fungal
|
Infection
Inflammation/Immunology
|
VT-1598 is an orally active and selective fungal inhibitor targeting CYP51. VT-1598 shows anti-fungal activity against Candida auris . VT-1598 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-123777A
-
|
Cytochrome P450
|
Infection
|
VT-1598 tosylate is an orally active and selective fungal inhibitor targeting CYP51. VT-1598 tosylate shows anti-fungal activity against C. auris . VT-1598 (tosylate) 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-137258
-
|
Cytochrome P450
|
Metabolic Disease
|
(±)-N-3-Benzylnirvanol is a racemic mixture of (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol. (+)-N-3-Benzylnirvanol and (–)-N-3-Benzylnirvanol are potent and selective cytochrome P450 inhibitors with Ki values of 0.25 and 5.3 μM for CYP2C19, respectively .
|
-
- HY-153989
-
|
Ras
Cytochrome P450
|
Cancer
|
SOS1-IN-16 (Comp 54) is a selective inhibitor of SOS1 with an IC50 of 7.2 nM. SOS1-IN-16 has inhibitory activity of CYP3A4 when using testosterone as a substrate, with an IC50 of 8.9μM. SOS1-IN-16 can be used for cancer research .
|
-
- HY-14275S1
-
-
- HY-A0064R
-
(±)-Verapamil hydrochloride (Standard); CP-16533-1 hydrochloride (Standard)
|
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Cardiovascular Disease
Cancer
|
Verapamil (hydrochloride) (Standard) is the analytical standard of Verapamil (hydrochloride). This product is intended for research and analytical applications. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
|
-
- HY-15550S
-
|
Drug Metabolite
|
Neurological Disease
Inflammation/Immunology
|
4'-Hydroxy diclofenac-d4 is the deuterium labeled 4'-Hydroxy diclofenac. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[1][2].
|
-
- HY-B1462S
-
|
Cytochrome P450
|
Inflammation/Immunology
|
Chlorzoxazone-d3 is the deuterium labeled Chlorzoxazone. Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes.Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochrome P450 2E1 (CYP2E1) activity in humans.
|
-
- HY-N1457
-
|
|
|
Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A .
|
-
- HY-19323A
-
(S)-AZD6738
|
ATM/ATR
|
Cancer
|
(S)-Ceralasertib ((S)-AZD6738) is extracted from patent WO2011154737A1, Compound II, exhibits an IC50 of 2.578 nM .
(S)-Ceralasertib is a potent and selective sulfoximine morpholinopyrimidine ATR inhibitor with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics.
(S)-Ceralasertib is developed improving aqueous solubility and eliminates CYP3A4 time-dependent inhibition .
|
-
- HY-117147
-
|
Cytochrome P450
|
Metabolic Disease
|
GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism .
|
-
- HY-117147A
-
|
Cytochrome P450
|
Metabolic Disease
|
GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism .
|
-
- HY-108263B
-
(R)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
(R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML) .
|
-
- HY-152468
-
|
Apoptosis
|
Cancer
|
Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro .
|
-
- HY-153970
-
|
URAT1
|
Inflammation/Immunology
|
URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor, with an IC50 of 12 nM. URAT1 inhibitor 7 exhibits microsomal stability (HLM <13 µL/min/mg). URAT1 inhibitor 7 also inhibits CYP2C9, with an IC50 of 4.2 μM. URAT1 inhibitor 7 can be used for gout research .
|
-
- HY-B0258R
-
CI-719 (Standard)
|
PPAR
Cytochrome P450
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
Gemfibrozil (Standard) is the analytical standard of Gemfibrozil. This product is intended for research and analytical applications. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
|
-
- HY-N3841A
-
|
Cytochrome P450
|
Metabolic Disease
|
δ-Viniferin is a resveratrol dehydrodimer, an isomer of ε-Viniferin (HY-N3841) . ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity.
|
-
- HY-N0453R
-
-
- HY-163110
-
|
HIV
Reverse Transcriptase
|
Infection
|
NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC50 of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics .
|
-
- HY-A0016
-
SR 33589
|
mAChR
Sodium Channel
Calcium Channel
Adrenergic Receptor
Cytochrome P450
Autophagy
|
Cardiovascular Disease
|
Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4 .
|
-
- HY-17367
-
BMS-232632
|
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
Endogenous Metabolite
|
Infection
Cancer
|
Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM .
|
-
- HY-B0113
-
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-17367A
-
BMS-232632 sulfate
|
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
Endogenous Metabolite
|
Infection
Cancer
|
Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV 3CL pro inhibitor with an IC50 of
3.49 μM .
|
-
- HY-14405A
-
GW679769B
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .
|
-
- HY-N2259
-
(+)-Curcumenol
|
|
|
Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells .
|
-
- HY-B0113A
-
H 16868 sodium
|
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria . Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-146458
-
|
Bacterial
Cytochrome P450
|
Infection
|
Antibacterial agent 102 (compound 32) possesses potent in vitro and in vivo antibacterial activity, with MICs < 0.5 μg/mL in Staphylococcus aureus (S. aureus). Antibacterial agent 102 also moderately inhibits CYP3A4 with an IC50 value of 6.148 μM. Antibacterial agent 102 can reduce Methicillin-resistant Staphylococcus aureus (MRSA) load in thigh infected mice .
|
-
- HY-150080
-
BMS-986180
|
HIV
HIV Integrase
|
Infection
|
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
|
-
- HY-15550S1
-
|
Drug Metabolite
|
|
4'-Hydroxy diclofenac- 13C6 is the 13C labeled 4'-Hydroxy diclofenac[1]. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[2][3].
|
-
- HY-152107A
-
|
LRRK2
|
Neurological Disease
|
(R,R)-LRRK2-IN-7 is the isomer of LRRK2-IN-7 (HY-152107). LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes.
|
-
- 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-113259S
-
|
Endogenous Metabolite
|
Metabolic Disease
|
7α-Hydroxy-4-cholesten-3-one-d7 is the deuterium labeled 7α-Hydroxy-4-cholesten-3-one. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1[1][2].
|
-
- HY-117010
-
|
Cytochrome P450
HSV
SGLT
|
Infection
Metabolic Disease
|
Kushenol K, a flavonoid antioxidant isolated from the roots of Sophora flavescens. Kushenol K is a cytochrome P-450 3A4 (CYP3A4) inhibitor with a Ki value of 1.35 μM . Kushenol K shows weak antiviral activity against HSV-2 (EC50 of 147 μM) . Kushenol K also inhibits the activity of SGLT1 and SGLT2 .
|
-
- HY-123319A
-
|
Bacterial
Antibiotic
|
Infection
|
Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
|
-
- HY-123319
-
|
Bacterial
Antibiotic
|
Infection
|
Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
|
-
- HY-147841
-
|
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .
|
-
- HY-150775
-
|
Cytochrome P450
|
Cancer
|
Nonsteroidal aromatase inhibitor 1 (Compound 13h) is a nonsteroidal aromatase (CYP19A1) inhibitor (IC50=0.09 nM). Nonsteroidal aromatase inhibitor 1 has potential for breast cancer research . Nonsteroidal aromatase inhibitor 1 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-148592
-
|
Cytochrome P450
|
Cancer
|
Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity .
|
-
- HY-50845
-
BMS-708163
|
γ-secretase
Notch
|
Cancer
|
Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.
|
-
- HY-124421
-
NSC-703786
|
Aryl Hydrocarbon Receptor
|
Others
|
5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38 .
|
-
- HY-A0064S1
-
(±)-Verapamil-d6 hydrochloride; CP-16533-1-d6 hydrochloride
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
Verapamil-d6 (CP-16533-1-d6) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
|
-
- HY-157929
-
|
Keap1-Nrf2
|
Inflammation/Immunology
Cancer
|
Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs .
|
-
- HY-133152
-
DM-3411
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .
|
-
- HY-144652
-
-
- HY-119209
-
|
5-HT Receptor
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction .
|
-
- HY-Y0698
-
Acetothioamide; TAA; Thiacetamide
|
Necroptosis
|
Inflammation/Immunology
|
Thioacetamide (TAA) is an indirect hepatotoxin and causes parenchymal cell necrosis. Thioacetamide requires metabolic activation by microsomal CYP2E1 to thioacetamide-S-oxide initially and then to thioacetamide-S-dioxide, which is a highly reactive metabolite, and its reactive metabolites covalently bind to proteins and lipids thereby causing oxidative stress and centrilobular necrosis. Thioacetamide can induce chronic liver fibrosis, encephalopathy and other events model .
|
-
- HY-138115
-
7β, 27-OHC
|
ROR
|
Inflammation/Immunology
|
7ß,27-Dihydroxycholesterol (7β, 27-OHC) is a potent and selective activator of RORγt (Ki=120 nM). 7ß,27-Dihydroxycholesterol promotes the differentiation of mouse and human CD4 + Th17 cells. 7ß,27-Dihydroxycholesterol also increases the production of IL-17 depended on CYP27A1 .
|
-
- 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-17367S3
-
-
- HY-17367S2
-
-
- HY-108263A
-
(S)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML) .
|
-
- 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-17367S4
-
-
- HY-146464
-
|
Fungal
|
Infection
|
Antifungal agent 30 (compound A18) is a potent antifungal agent. Antifungal agent 30 shows excellent antifungal activity against Candida albicans (CPCC400616) and Aspergillus fumigatus, with MIC of 0.03 and 0.5 μg/mL, respectively. Antifungal agent 30 also shows excellent antifungal activity against fluconazole-resistant strains. The potent antifungal activity of Antifungal agent 30 mainly causes by hydrogen and coordination bond interaction with the CYP51 .
|
-
- HY-B1324A
-
Ro 13-8996 free base
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-134664
-
|
Cytochrome P450
Monoamine Oxidase
|
Inflammation/Immunology
|
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate is an irreversible CYP2A6 inhibitor with IC50s of 8.64 μM and 22.3 μM with pre-incubation and co-incubaition, respectively. 8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate also inhibits MAO-A and MAO-B with IC50s of 60.2 and 38.6 μM, 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-13690
-
2,4′-DDD; o,p'-DDD
|
Apoptosis
|
Cancer
|
Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions .
|
-
- HY-B1218
-
|
Cytochrome P450
Antibiotic
Bacterial
Necroptosis
Apoptosis
|
Infection
Cardiovascular Disease
|
Sulfaphenazole is a selective inhibitor of human cytochrome P450 (CYP) 2C9 enzyme. Sulfaphenazole is a cytoprotective agent against light-induced death of photoreceptors. Sulfaphenazole inhibits light-induced necrosis and mitochondrial stress-initiated apoptosis. Sulfaphenazole is an off patent sulfonamide antibiotic and demonstrates bactericidal activity through enhanced M1 macrophage activity. Sulfaphenazole can significantly reduce infarct size and restore post-ischemic coronary flow following ischemia and reperfusion .
|
-
- HY-B1324
-
Ro 13-8996
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-B0113S1
-
H 16868-d3-1
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
|
-
- 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-147999
-
|
Bacterial
Fungal
Cytochrome P450
|
Infection
|
GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform .
|
-
- HY-B0653A
-
(S)-(-)-Bupivacaine monohydrochloride
|
Sodium Channel
Ferroptosis
|
Neurological Disease
Cancer
|
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local anaesthetic. Levobupivacaine hydrochloride exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
|
-
- HY-B0113S3
-
H 16868-13C,d3
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
|
-
- HY-133152S
-
DM-3411 d8
|
Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
|
-
- HY-119293
-
K777
1 Publications Verification
|
Cathepsin
CCR
Cytochrome P450
Parasite
SARS-CoV
Filovirus
|
Infection
Cancer
|
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
|
-
- HY-132866
-
|
P-glycoprotein
|
Cancer
|
YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity .
|
-
- HY-B0653
-
(S)-(-)-Bupivacaine
|
Sodium Channel
Ferroptosis
|
Neurological Disease
Cancer
|
Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
|
-
- HY-148825
-
-
- HY-13404
-
INC280; INCB28060
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-10965
-
KW-3902
|
Adenosine Receptor
|
Neurological Disease
|
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450) .
Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .
|
-
- HY-13404B
-
INC280 hydrochloride; INCB-28060 hydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404C
-
INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404A
-
INC280 dihydrochloride; INCB28060 dihydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-163436
-
|
FXR
Cytochrome P450
RAR/RXR
PPAR
ROR
|
Metabolic Disease
|
F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders .
|
-
- HY-101016
-
|
|
|
17-ODYA is a CYP450 ω-hydroxylase inhibitor. 17-ODYA is also a potent inhibitor (IC50<100 nM) of the formation of 20-hydroxyeicosatetraenoic acid (20-HETE), epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids by rat renal cortical microsomes incubated with arachidonic acid. 17-ODYA completely attenuates the isoproterenol (ISO)-induced apoptosis, and necrosis in cultured cardiomyocytes . 17-ODYA 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-131968
-
|
JAK
Cytochrome P450
|
Inflammation/Immunology
|
BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium .
|
-
- HY-13690S1
-
2,4′-DDD-13C6; o,p'-DDD-13C6
|
Apoptosis
|
Cancer
|
Mitotane- 13C6 is the 13C labeled Mitotane[1]. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions[2][3][4][5].
|
-
- HY-13690S2
-
2,4′-DDD-d8; o,p'-DDD-d8
|
Apoptosis
|
Cancer
|
Mitotane-d8 is the deuterium labeled Mitotane[1]. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions[2][3][4][5].
|
-
- HY-113259
-
|
Endogenous Metabolite
|
Metabolic Disease
|
7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
|
-
- HY-144123
-
|
HIV
|
Infection
|
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
|
-
- HY-157959
-
(±)-Orphenadrine
|
iGluR
Cytochrome P450
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and cytochrome P450 (CYP) 2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation .
|
-
- HY-113259R
-
|
Endogenous Metabolite
|
Metabolic Disease
|
7α-Hydroxy-4-cholesten-3-one (Standard) is the analytical standard of 7α-Hydroxy-4-cholesten-3-one. This product is intended for research and analytical applications. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-D0144
-
Methoxyresorufin
|
Chromogenic Substrates
|
Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate . Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents .
|
-
- HY-D0145
-
Resorufin ethyl ether
|
Chromogenic Substrates
|
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
|
-
- HY-116862
-
DBF
|
Fluorescent Dyes/Probes
|
Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 µM (Ex=485nm,Em=535nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
|
-
- HY-162051
-
|
Fluorescent Dyes/Probes
|
CYP1B1-IN-6 (compound 19) is a fluorescence molecular probes which inhibits CYP1B1 activity. CYP1B1-IN-6 can identify tumor sites in fluorescence imaging and photoacoustic imaging modes .
|
-
- HY-17356G
-
|
Fluorescent Dye
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
- HY-W271064
-
|
Fluorescent Dyes/Probes
|
1-Methylpyrene is a ubiquitous environmental pollutant and rodent carcinogen. Its mutagenic activity depends on sequential activation by various CYP and sulfotransferase (SULT) enzymes. 1-Methylpyrene induces chromosome loss and mitotic disturbance, proba
|
-
- HY-D0146
-
BzRes; 7-Benzyloxyresorufin; 7-Benzyloxyphenoxazone
|
Dyes
|
Resorufin benzyl ether (BzRes), a fluorogenic enzyme substrate, can be used to detect CYP3A4 enzyme activity. Resorufin benzyl ether modified with a recognizing moiety boronate, can be used for ONOO - detection via a self-immolation mechanism. Ex/Em=530-570 nm/590 nm .
|
Cat. No. |
Product Name |
Type |
-
- HY-17356G
-
|
Biochemical Assay Reagents
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-144285
-
|
CXCR
HIV
|
Inflammation/Immunology
|
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N4205
-
-
-
- HY-Y0110
-
-
-
- HY-133091
-
-
-
- HY-N8094
-
-
-
- HY-N8382
-
-
-
- HY-N2181A
-
-
-
- HY-N6023
-
-
-
- HY-N2071
-
Cedrol
1 Publications Verification
(+)-Cedrol; α-Cedrol
|
Cedrus deodara (Roxburgh) G. Don
Classification of Application Fields
Pinaceae
Terpenoids
Sesquiterpenes
Source classification
Plants
Inflammation/Immunology
Disease Research Fields
Cancer
|
Cytochrome P450
Fungal
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
|
-
-
- HY-113482
-
-
-
- HY-N0482
-
-
-
- HY-N0319
-
-
-
- HY-N0453
-
-
-
- HY-N3090
-
-
-
- HY-N5132
-
-
-
- HY-N0893
-
-
-
- HY-N0598
-
-
-
- HY-I0736
-
-
-
- HY-N7266
-
-
-
- HY-122410
-
-
-
- HY-30152
-
-
-
- HY-N0922
-
-
-
- HY-N0043
-
-
-
- HY-N2260
-
-
-
- HY-W010195
-
-
-
- HY-130550
-
-
-
- HY-N0043R
-
-
-
- HY-N0693
-
-
-
- HY-N3769
-
-
-
- HY-N0370
-
-
-
- HY-N1201
-
-
-
- HY-N0779
-
-
-
- HY-W008772
-
-
-
- HY-W011956
-
-
-
- HY-N12530
-
-
-
- HY-N4110
-
-
-
- HY-N0921
-
-
-
- HY-N12529
-
-
-
- HY-N0515
-
-
-
- HY-N0125
-
-
-
- HY-N2425
-
-
-
- HY-N0382
-
-
-
- HY-N7534
-
-
-
- HY-119804
-
-
-
- HY-N0904
-
-
-
- HY-W008364
-
-
-
- HY-N2129
-
-
-
- HY-N2586
-
-
-
- HY-N10421
-
-
-
- HY-N7454
-
-
-
- HY-N11706
-
-
- HY-N8354
-
-
- HY-N1483
-
-
- HY-76316
-
-
- HY-N6989
-
-
- HY-N0144
-
-
- HY-N0904R
-
-
- HY-N0494
-
-
- HY-N9434
-
-
- HY-N1201R
-
-
- HY-N6264
-
-
- HY-N0688
-
-
- HY-113327
-
-
- HY-150084
-
(±)14(15)-EET
|
Structural Classification
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Cytochrome P450
|
(±)14,15-Epoxyeicosatrienoic acid ((±)14(15)-EET) is the Cytochrome P450 metabolite of arachidonic acid. While CYP3A4 may be involved in breast cancer cell growth, (±)14,15-Epoxyeicosatrienoic acid may promote mitosis and anchorage-dependent cloning through STAT3 affected by CYP3A4. (±)14,15-Epoxyeicosatrienoic acid exhibits STAT3-dependent cell growth promotion and may also participate in the autocrine/paracrine pathway that drives cell growth .
|
-
- HY-N6972
-
-
- HY-W087008
-
-
- HY-N0125R
-
-
- HY-N0382R
-
-
- HY-113151
-
-
- HY-125598
-
-
- HY-N10344
-
-
- HY-N9203
-
-
- HY-N2625A
-
-
- HY-134039
-
-
- HY-N0692
-
-
- HY-W087919
-
-
- HY-N2689
-
-
- HY-W008226
-
-
- HY-N5011
-
-
- HY-N3841
-
-
- HY-N3841A
-
-
- HY-N0453R
-
-
- HY-17367
-
-
- HY-17367A
-
-
- HY-117010
-
-
- HY-134664
-
-
- HY-113259
-
-
- HY-113259R
-
-
Cat. No. |
Product Name |
Chemical Structure |
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- HY-Y0110S1
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2-Naphthol-d7 is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].
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- HY-13600S1
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Clobetasol propionate-d5 is a deuterium substitute of Clobetasol propionate. Clobetasol propionate is a potent, selective CYP3A5 inhibitor with a IC50 of 0.206 μM and has potential for use in the study of psoriasis and other skin diseases .
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- HY-Y0110S
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2-Naphthol-d8 is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].
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- HY-B2015S
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Carbosulfan-d18 is the deuterium labeled Carbosulfan. Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
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- HY-133091S
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7-Ethoxycoumarin-d5 is deuterium labeled 7-Ethoxycoumarin. 7-Ethoxycoumarin is a substrate for cytochrome P450(CYP450) and has been used in the functional characterization of various CYPs[1].
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- HY-N0893S
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Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
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- HY-B0822S1
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Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
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- HY-17356S
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Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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- HY-17356S1
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Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].
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- HY-135810S
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Cletoquine-d4 is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
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- HY-B1184S1
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Mephenytoin-d5 is the deuterium labeled Mephenytoin. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[1].
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- HY-I0736S
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Isonicotinic acid-d4 is the deuterium labeled Isonicotinic acid[1]. Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochrome P450 (CYP) enzymes, e.g., CYP2C[2].
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- HY-135810S1
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Cletoquine-d4-1 is the deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
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- HY-B0105S1
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Ketoconazole-d4 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
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- HY-B0105S
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Ketoconazole-d8 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
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- HY-B1184S2
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Mephenytoin-d8 is the deuterium labeled Mephenytoin[1]. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[2].
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- HY-B0281AS
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Ranitidine-d6 (hydrochloride) is the deuterium labeled Ranitidine hydrochloride. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9[1][2].
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- HY-B0352AS
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(S)-Mirtazapine-d3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].
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- HY-B0852S
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Tebuconazole-d9 is the deuterium labeled Tebuconazole. Tebuconazole is an agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively.
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- HY-W754151
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N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
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- HY-13463BS
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Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A[1][2][3].
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- HY-B0725S
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Doxepin-d3 (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].
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- HY-100665S
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Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
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- HY-B0352BS
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(R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
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- HY-100641S
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4-Hydroxytolbutamide-d9 is the deuterium labeled 4-Hydroxytolbutamide. 4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic[1][2].
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- HY-70013S
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Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
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- HY-100386S
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Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].
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- HY-122410S
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Dihydrolanosterol-d7 is deuterium labeled Dihydrolanosterol. Dihydrolanosterol is a subtrate of CYP51 and a cholesterol biosynthesis inhibitor[1].
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- HY-103392S
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Stiripentol-d9 is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively[1][2].
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- HY-14874S
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Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].
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- HY-N0370S
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Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
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- HY-A0016S
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Dronedarone-d6 (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4[1][2][3][4].
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- HY-119695AS
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Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1].
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- HY-17508S1
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Clarithromycin-d3is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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- HY-N0125S
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Diosmetin-d3 is the deuterium labeled Diosmetin. Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
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- HY-135334S
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ACP-5862-d4 is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM[1][2].
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- HY-10882S
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Clotrimazole-d5 is the deuterium labeled Clotrimazole. Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity[1][2].
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- HY-N0382S
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Galangin- 13C3 is the 13C-labeled Galangin. Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
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- HY-135335S
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3'-Hydroxy Repaglinide-d5 is the deuterium labeled 3'-Hydroxy Repaglinide. 3'-Hydroxy Repaglinide is a main CYP2C8 metabolite of Repaglinide[1].
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- HY-75054S
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Abiraterone acetate-d4 is the deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
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- HY-17459S
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Clopidogrel-d3 (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate[1]. Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation.Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor[2][3][4][5][6].
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- HY-W008772S
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4-Hydroxymephenytoin-d3 is the deuterium labeled 4-Hydroxymephenytoin. 4-Hydroxymephenytoin is a metabolism of an antiepileptic agent mephenytoin, which is used as a CYP2C19 substrate[1][2].
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- HY-122277S
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1'-Hydroxy bufuralol-d9 is a deuterium labeled 1'-Hydroxy bufuralol (HY-122277). 1'-Hydroxy bufuralol, the main metabolite of bufuralol, can reflect CYP2D activity .
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- HY-130353S
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Desethyl Amiodarone-d4 (hydrochloride) is the deuterium labeled Desethylamiodarone hydrochloride. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2][3].
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- HY-117580S
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16α-Hydroxyprednisolone-d3 is the deuterium labeled 16α-Hydroxyprednisolone. 16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochrome P450 3A (CYP3A) enzymes[1][2].
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- HY-D0145S
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7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
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- HY-B0476S
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Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
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- HY-30151S
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Methoxsalen-d3 is the deuterium labeled Methoxsalen[1]. Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight[2].
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- HY-100064S
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O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
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- HY-100064S1
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O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
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- HY-B0476S1
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Phenacetin- 13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
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- HY-B0113S
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Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
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- HY-B0258S
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Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
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- HY-133116S
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4-Hydroxyatomoxetine-d3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine (Tomoxetine). 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine is a potent and selective noradrenal in re-uptake inhibitor[1].
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- HY-A0064S
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Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research[1][2][3].
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- HY-10493S
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Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules .
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- HY-14275S1
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Verapamil-d7 is the deuterium labeled Verapamil (HY-14275). Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
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- HY-15550S
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4'-Hydroxy diclofenac-d4 is the deuterium labeled 4'-Hydroxy diclofenac. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[1][2].
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- HY-B1462S
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Chlorzoxazone-d3 is the deuterium labeled Chlorzoxazone. Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes.Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochrome P450 2E1 (CYP2E1) activity in humans.
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- HY-15550S1
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4'-Hydroxy diclofenac- 13C6 is the 13C labeled 4'-Hydroxy diclofenac[1]. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[2][3].
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- HY-113259S
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7α-Hydroxy-4-cholesten-3-one-d7 is the deuterium labeled 7α-Hydroxy-4-cholesten-3-one. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1[1][2].
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- HY-A0064S1
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Verapamil-d6 (CP-16533-1-d6) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
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- HY-17367S3
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Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
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- HY-17367S2
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Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
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- HY-17367S4
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Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
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- HY-B0113S1
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Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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- HY-B0113S3
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Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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- HY-133152S
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Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
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- HY-131968
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BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium .
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- HY-13690S1
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Mitotane- 13C6 is the 13C labeled Mitotane[1]. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions[2][3][4][5].
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- HY-13690S2
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Mitotane-d8 is the deuterium labeled Mitotane[1]. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions[2][3][4][5].
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Classification |
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- HY-114759
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Alkynes
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MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor . MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 μM, respectively . MS-PPOH 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-119647
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Alkynes
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PPOH, a fatty acid derivative, is a selective cyclooxygenase (COX) inhibitor that inhibits arachidonic acid cyclooxygenase activity in renal cortical microsomes. In addition, PPOH acts on CYP4A2 and CYP4A3 with the IC50 values of 22 μM and 6.5 μM, respectively . PPOH 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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