Cytochrome P450

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  1. CYP17A1/androgen synthesis inhibitor

    Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues.
  2. XOR Inhibitor

    Topiroxostat (FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.
  3. CYP3A4 Inhibitor

    Azithromycin, derived from erythromycin, is a antibiotic. Azithromycin binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA.
  4. CYP2C19/CYP2B6 inhibitor

    Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia.
  5. cytochrome P450 inhibitor

    Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI).
  6. CYP2C9 inhibitor

    Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
  7. Chlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1.
  8. CYP1A1 inhibitor

    Bergamottin is a furanocoumarin found in grapefruit juice and lemon, lime, and bergamot oils that has diverse biological activities.
  9. CYP51 inhibitor

    Tebuconazole is a triazole fungicide used agriculturally to treat plant pathogenic fungi.
  10. human cytochrome P450IA2 inhibitor

    Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM.
  11. CYP2C9 inhibitor

    Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
  12. Cytochrome P450 inhibitor

    Proadifen hydrochloride is a Cytochrome P450 inhibitor (IC50 = 19μM).
  13. Phortress, also known as NSC-710305 and 5F-DF-203-L-lysinamide, is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
  14. EMT inhibitor

    EMT inhibitor-2 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.
  15. Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
  16. Cytochrome P450 inhibitor

    4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
  17. peptidoleukotrienes antagonist

    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 ?M.
  18. cytochrome P450 1B1 inhibitor

    1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1.
  19. androgen receptor/CYP17A1 dual inhibitor

    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80?nM and 22 nM, respectively.
  20. CYP3A inducer

    CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
  21. CYP3A inducer

    CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
  22. CYP1B1 inhibitor

    DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
  23. CYP1B1 inhibitor

    DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
  24. aldosterone synthase inhibitor

    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.
  25. CYP51 inhibitor

    Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM), shows no obvious effect on human CYP51.
  26. Small utrophin's translation modulator

    Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
  27. DAF-9 cytochrome P450 inhibitor

    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).
  28. CYP17 lyase inhibitor

    Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
  29. CYP3A4/5 inhibitor and substrate

    Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
  30. CYP26 inhibitor/RAMBA

    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.
  31. liver CYP3A4 substrate

    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.
  32. CYP450 dependent inhibitor

    Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).
  33. Cytochrome P450 hibitor

    Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 ?M and 22.8 ?M for CYP2A6; Gentiopicroside has antianti-inflammatoryand antioxidative effects.
  34. Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP).
  35. anti-inflammatory agent

    Cepharanthine is an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities.
  36. CYP3A4 inducer

    RO6889678 is an inhibitor of HBV with a complex ADME profile. RO6889678 showed an intracellular enrichment of 78-fold in hepatocytes, with an apparent intrinsic clearance of 5.2 ?l/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 ?l/min per mg protein, respectively.
  37. Orteronel (racemic) is a mixture of S-Orteronel and R-Orteronel isomers.
  38. Cholesterol 24-hydroxylase (CH24H) inhibitor

    Soticlestat, also known as TAK 935 and OV935, is an inhibitor of the enzyme cholesterol 24-hydroxylase (CH24H).
  39. CYP51 inhibitor

    SDZ285428 is a CYP51 inhibitor.

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