Cytochrome P450

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  1. CYP17 inhibitor

    Abiraterone (CB-7598) inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1), an enzyme which is expressed in testicular, adrenal, and prostatic tumor tissues.
  2. CYP17 inhibitor

    Alizarin is novelly used as a staining agent in biological research because it stains free calcium and certain calcium compounds a red or light purple color.
  3. Protein kinase inhibitor

    Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.

  4. CYP17 inhibitor

    Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor.
  5. Lipoxygenase Inhibitor

    Baicalein is a flavonoid originally isolated from the roots of Scutellaria baicalensis Georgi. Baicalein inhibits lipid peroxidation, as assessed by production of TBARS, with an IC50 value of 5 µM.

  6. Chloramphenicol is a bacteriostatic antimicrobial.
  7. cytochrome P4503A4 inhibitor

    Clarithromycin is a macrolide antibiotic. It prevents bacteria from growing by interfering with their protein synthesis.
  8. Action of clotrimazole is against the division and growing of fungi.Clotrimazole alters the permeability of the fungal cell wall and inhibits the activity of enzymes within the cell. It specifically inhibits the biosynthesis of ergosterol and other sterols required for cell membrane production.
  9. Iron chelator

    Deferasirox is a rationally-designed oral iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.
  10. CYP2D6 inhibitor

    Haloperidol (Haldol) is an antipsychotic and butyrophenone.
  11. Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.
  12. P450 inhibitor

    As an antifungal, ketoconazole is structurally similar to imidazole, and interferes with the fungal synthesis of ergosterol, a constituent of fungal cell membranes, as well as certain enzymes.
  13. Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450).
  14. Naringenin is a flavanone, a type of flavonoid, that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.
  15. TXAS inhibitor

    Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM.
  16. CYP3A4 inhibitor

    Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14?? demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.
  17. Sodium danshensu is a sodium salt of danshensu from the widely used Chinese herb Danshen (Salvia miltiorrhiza Bunge). In vitro and in vivo studies revealed that danshensu possessed diverse pharmacological effects, including relaxation of coronary artery, anticoagulation, protection of myocardial ischemia-reperfusion injury, and antiarrhythmia activities
  18. CYP17 inhibitor

    Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion.
  19. CYP17A1 inhibitor

    TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme.
  20. CYP17 inhibitor

    Abiraterone acetate (CB7630) is an orally active acetate ester of the steroidal compound Abiraterone with antiandrogen activity. Abiraterone inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1).
  21. CYP17 inhibitor

    TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor.
  22. TH-302 is a selectively targeting hypoxic regions of solid tumors hypoxia-activated prodrug.
  23. CYP3A Inhibitor

    Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate.
  24. Androgen Receptor antagonist

    Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity.
  25. Luliconazole is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.
  26. anti-inflammatory corticosteroid

    Clobetasol propionate is a anti-inflammatory corticosteroid used to treat various skin disorders.
  27. Hydroxyflutamide (Hydroxyniphtholide) is a metabolite of flutamide found to inhibit the proliferation of estradiol-induced growth of MCF-7 breast cancer cells.
  28. TMS is a potent, selective and competitive inhibitor of cytochrome P450 1B1, an enzyme overexpressed in certain tumors (IC50= 6 nM). 5N/A- and 520-fold selective over P450 1A1 and 1A2 respectively.
  29. CYP3A4 enzyme inhibitor

    Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties.
  30. CYP3A4 inhibitor

    PF 4981517 is a potent and selective inhibitor of CYP3A4 (IC50 values are 0.03, 17 and 70 μM for CYP3A4, CYP3A5 and CYP3A7 respectively).
  31. CYP17 inhibitor

    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.
  32. Cytochrome P450 inhibitor

    Talarozole R enantiomer inhibits the metabolism of retinoic acid by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase.
  33. Cytochrome P450 inhibitor

    ABT (1-Aminobenzotriazole )is a suicide substrate for (CYP)cytochrome P-450 and chloroperoxidase.
  34. Fluorescent P450 substrate

    3-Cyano-7-ethoxycoumarin is a fluorogenic substrate suitable for the continuous determination of cytochrome P450 mixed-function monooxygenases. It is a fluorescent probe useful in microsomal dealkylase studies.
  35. CYP2C19 and CYP2B6 substrate

    Mephenytoin is a CYP2C19 substrate. Anticonvulsant.
  36. cytochrome P450 substrate

    Methoxyresorufin is a fluorometric substrate for cytochrome P450 linked enzymes.

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