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-N2233
    Rhapontigenin 3'-O-glucoside
    Inhibitor 99.94%
    Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin. Rhapontigenin is a potent inactivator of human P450 1A1 and is a good candidate for a cancer chemopreventive agent.
    Rhapontigenin 3'-O-glucoside
  • HY-76316R
    Bergaptol (Standard)
    Inhibitor
    Bergaptol (Standard) is the analytical standard of Bergaptol. This product is intended for research and analytical applications. Bergaptol is an inhibitor of debenzylation of the CYP3A4 enzyme with an IC50 of 24.92 μM. Recent studies have shown that it has anti-proliferative and anti-cancer properties.
    Bergaptol (Standard)
  • HY-17514S2
    Itraconazole-d9
    Itraconazole-d9 is the deuterium labeled Itraconazole. 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>9</sub>
  • HY-N9508
    Perilla ketone
    99.9%
    Perilla ketone is a naturally occurring xenobiotic compound. Perilla ketone is activated by pulmonary P450 cytochrome enzymes in the lung, resulting in severe pulmonary damage and development of diffuse pulmonary edema.
    Perilla ketone
  • HY-130419
    (±)13(14)-EpDPA
    (±)13(14)-EpDPA (13,14-EpDPE) is the product of the reaction of cytochrome P-450 epoxygenase with Docosahexaenoic Acid (DHA).(±)13(14)-EpDPA has antihyperalgesic and vasorelaxative activities.
    (±)13(14)-EpDPA
  • HY-112734
    4'-Methylchrysoeriol
    Inhibitor 99.17%
    4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
    4'-Methylchrysoeriol
  • HY-136589
    Verapamil EP Impurity C hydrochloride
    Inhibitor 99.61%
    NSC-609249 hydrochloride is an impurity of Verapamil (HY-14275). Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.
    Verapamil EP Impurity C hydrochloride
  • HY-121580
    Tabimorelin
    Inhibitor 98.11%
    Tabimorelin (NN703) is an orally active growth hormone (GH) secretagogue. Tabimorelin is also a potent inhibitor of CYP3A4 activity.
    Tabimorelin
  • HY-D0144
    Resorufin methyl ether
    99.84%
    Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate. Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents.
    Resorufin methyl ether
  • HY-Z2667
    (R)-Esomeprazole
    Modulator
    (R)-Esomeprazole ((R)-Omeprazole; (+)-Omeprazole) is an orally active cytochrome P450 2C19, CYP3A4, and CYP2C9-related metabolic modulator. (R)-Esomeprazole can be used in studies of digestive system diseases and compound metabolic interactions.
    (R)-Esomeprazole
  • HY-148430
    4-Pyridylmethyl adamantanecarboxamide
    Inhibitor 99.83%
    4-Pyridylmethyl adamantanecarboxamide (Compound 11) is an Aromatase inhibitor with an IC50 of 1.5 μM against hAromatase. 4-Pyridylmethyl adamantanecarboxamide inhibits the C17,20-lyase activity of testicular cytochrome P45017α with an IC50 of 1600 nM, and also inhibits the 17α-hydroxylase activity of this enzyme with an IC50 of 7700 nM. 4-Pyridylmethyl adamantanecarboxamide can be used in the research of prostate cancer.
    4-Pyridylmethyl adamantanecarboxamide
  • HY-121870
    Dimethocaine
    Substrate 99.90%
    Dimethocaine (Larocaine) is a cocaine derivative and ester-type local anesthetic. Dimethocaine is metabolized by hP450 1A2, 2C19, 2D6, and 3A4 in vitro. Dimethocaine exhibits locomotor-promoting, reinforcing, and anxiogenic effects.
    Dimethocaine
  • HY-107939
    Paramethasone Acetate
    Inhibitor 98.0%
    Paramethasone Acetate is an orally active long-acting glucocorticoid. Paramethasone Acetate directly inhibits testicular aromatase, thereby reducing the synthesis of estradiol. Paramethasone Acetate suppresses the basal and midcycle luteinizing hormone surges in female animals and blocks estrogen synthesis. Paramethasone Acetate also decreases circulating levels of dihydrotestosterone, androstenedione and estradiol in male animals. Paramethasone Acetate inhibits cartilage degeneration and alleviates joint pathological damage in osteoarthritis models. Paramethasone Acetate can be used in research related to osteoarthritis and endocrinology.
    Paramethasone Acetate
  • HY-N13215
    Tongkat Ali Extract
    Activator
    Tongkat Ali Extract is the extract of Tongkat Ali, a testosterone modulator. Tongkat Ali Extract activates CYP17 enzyme to enhance conversion of pregnenolone and progesterone to dehydroepiandrosterone, androstenedione, and testosterone. Tongkat Ali Extract demonstrates antimalarial, antimicrobial, anticancer, and antidiabetic activity. Tongkat Ali Extract can be used for the research of diabetic and male infertility.
    Tongkat Ali Extract
  • HY-186072
    NT-0527
    Inhibitor 99.80%
    NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome.
    NT-0527
  • HY-120648A
    CAY 10462 dihydrochloride
    Inhibitor 98.02%
    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.
    CAY 10462 dihydrochloride
  • HY-120696
    SR9186
    Inhibitor 98.06%
    SR9186 (ML368) is a selective CYP3A4 inhibitor with IC50 values of 9, 4, and 38 nM for Midazolam → 1'-hydroxymidazolam, Testosterone → 6β-hydroxytestosterone, and Vincristine → Vincristine M1, respectively. SR-9186 inhibits the development of hepatic-stage P. falciparum and blocks ivermectin metabolism. SR-9186 can be used in breast cancer research.
    SR9186
  • HY-N6023
    Thermopsoside
    Inhibitor 98.0%
    Thermopsoside is a CYP450 isoenzyme inhibitor and PXR activator. Thermopsoside inhibits CYP3A4, CYP2C19, CYP2D6 and CYP2C9 with IC50 values of 6.0 μM, 9.5 μM, 12.0 μM and 32.0 μM, respectively.
    Thermopsoside
  • HY-163529
    HN0037
    Substrate 99.46%
    HN0037 is a selective, orally active Helicase-primase inhibitor. HN0037 is mainly metabolized by CYP3A4. HN0037 inhibits HSV replication by targeting the viral helicase-primase complex, which consists of three proteins encoded by UL5 (helicase), UL52 (primase), and UL8 (scaffold protein that promotes primer synthesis).
    HN0037
  • HY-N1882
    4,5-Dimethoxycanthin-6-one
    Inhibitor 98.68%
    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).
    4,5-Dimethoxycanthin-6-one
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