1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Cytochrome P450

Cytochrome P450

CYPs

Cytochrome p450 comprises a superfamily of heme-thiolate proteins named for the spectral absorbance peak of their carbon-monoxide-bound species at 450 nm. Having been found in every class of organism, including Archaea, the p450 superfamily is believed to have originated from an ancestral gene that existed over 3 billion years ago. Repeated gene duplications have subsequently given rise to one of the largest of multigene families. These enzymes are notable both for the diversity of reactions that they catalyze and the range of chemically dissimilar substrates upon which they act. Cytochrome p450s support the oxidative, peroxidative and reductive metabolism of such endogenous and xenobiotic substrates as environmental pollutants, agrochemicals, plant allelochemicals, steroids, prostaglandins and fatty acids. In humans, Cytochrome p450s are best known for their central role in phase I drug metabolism where they are of critical importance to two of the most significant problems in clinical pharmacology: drug interactions and interindividual variability in drug metabolism.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N3680
    Danshenxinkun A
    99.95%
    Danshenxinkun A is a natural compound that could be isolated from Tanshen and is used in the study for heart diseases.
    Danshenxinkun A
  • HY-144652
    IDO1-IN-19
    Inhibitor 98.82%
    IDO1-IN-19 (Compound 17) is an orally active IDO1 inhibitor with an IC50 of CYP2C9 of 8.64 μM. IDO1-IN-19 also acts funciton on cardiac channels, with IC50s of 12 μM (IKr), 40 μM (INa), 8.3 μM (ICa), respectively. IDO1-IN-19 has the potential to study cancer diseases.
    IDO1-IN-19
  • HY-B2169
    Melperone
    Inhibitor 99.84%
    Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone
  • HY-B0589C
    (3S,5S)-Atorvastatin
    Activator
    (3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
    (3S,5S)-Atorvastatin
  • HY-125598
    Secologanin
    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.
    Secologanin
  • HY-106019C
    Liarozole dihydrochloride
    Inhibitor 99.04%
    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.
    Liarozole dihydrochloride
  • HY-B1812
    Veratrole
    Substrate 99.46%
    Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii.
    Veratrole
  • HY-W344044
    Levomepromazine maleate
    Inhibitor 99.92%
    Levomepromazine maleate (Methotrimeprazine maleate) is an N-substituted phenylthiazine antipsychotic sedative that blocks multiple receptors. Levomepromazine maleate is a potent inhibitor of CYP2D6 and is useful in the study of schizophreni.
    Levomepromazine maleate
  • HY-151239
    ONT-993
    Inhibitor 99.85%
    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).
    ONT-993
  • HY-113031
    16a-Hydroxydehydroisoandrosterone
    98.40%
    16a-Hydroxydehydroisoandrosterone (16α-Hydroxy-DHEA) is a metabolite of the endogenous steroid hormone dehydroepiandrosterone. 16α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosterone via 16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol.
    16a-Hydroxydehydroisoandrosterone
  • HY-W014701
    1,4-Dihydroxy-2-naphthoic acid
    Agonist 99.60%
    1,4-Dihydroxy-2-naphthoic acid is an aryl hydrocarbon receptor (AhR) agonist. 1,4-Dihydroxy-2-naphthoic acid is also a bacterially derived metabolite and has anti-inflammatory activity.
    1,4-Dihydroxy-2-naphthoic acid
  • HY-W010195
    2,6-Dimethylquinoline
    Inhibitor 99.95%
    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.
    2,6-Dimethylquinoline
  • HY-B1218R
    Sulfaphenazole (Standard)
    Inhibitor
    Sulfaphenazole (Standard) is the analytical standard of Sulfaphenazole. This product is intended for research and analytical applications. 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.
    Sulfaphenazole (Standard)
  • HY-101284
    DMU2105
    Inhibitor 99.54%
    DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
    DMU2105
  • HY-13463A
    Avatrombopag maleate
    Activator 99.88%
    Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC50: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A .
    Avatrombopag maleate
  • HY-12946
    BI 653048
    Inhibitor 99.84%
    BI 653048, a chemical probe, 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 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
    BI 653048
  • HY-17514S1
    Itraconazole-d3
    99.62%
    Itraconazole-d3 (R51211-d3) is the deuterium labeled Itraconazole (HY-17514). Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
    Itraconazole-d<sub>3</sub>
  • HY-101285
    DMU2139
    Inhibitor 98.0%
    DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
    DMU2139
  • HY-B0189B
    Mosapride citrate dihydrate
    Inducer 99.79%
    Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo.
    Mosapride citrate dihydrate
  • HY-103223
    Phortress
    Inducer 98.19%
    Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1.
    Phortress
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