P450 (e.g. CYP17)

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P450 (e.g. CYP17) Inhibitors (24)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1123 Abiraterone Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.
  • J Biol Chem, 2015, 290(6):3248-68
  • Prostate, 2013, 74(3):235-49
  • Chem Res Toxicol, 2012, 25(8):1720-31
S2246 Abiraterone Acetate Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay.
  • J Biol Chem, 2015, 290(6):3248-68
  • Endocrinology, 2014, 155(2):358-69
  • Prostate, 2013, 74(3):235-49
S1442 Voriconazole Voriconazole is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.
  • Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15
  • Antimicrob Agents Chemother, 2015, 59(5):2654-65
  • Antimicrob Agents Chemother, 2015, 59(9):5548-54
S2187 Avasimibe Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.
  • Nature, 2016, 531(7596):651-5
S1353 Ketoconazole Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.
S2476 Itraconazole Itraconazole is a relatively potent inhibitor of CYP3A4, used as a triazole antifungal agent.
  • Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15
  • Antimicrob Agents Chemother, 2015, 59(9):5548-54
  • PLoS One, 2014, 9(10):e109487
S1331 Fluconazole Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.
  • Antimicrob Agents Chemother, 2015, 59(4):2388-97
S2268 Baicalein Baicalein is a CYP2C9 and prolyl endopeptidase inhibitor.
  • J Nutr Biochem, 2013, 24(11):1953-62
  • Mol Cell Biochem, 2015, 10.1007/s11010-015-2429-8
S2262 Apigenin Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.
  • Int J Clin Exp Pathol, 2014, 7(7):3938-3947
S2344 Piperine Piperine (1-Piperoylpiperidine) is the alkaloid responsible for the pungency of black pepper and long pepper, which has also been used in some forms of traditional medicine and as an insecticide.
  • Int J Mol Med, 2015, 36(5):1369-76
S2380 Diosmetin Diosmetin is a bioflavonoid found in spearmint, oregano, and many other plants.
S2803 Galeterone Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.
  • Biochem Biophys Res Commun, 2016, 477(4):1005-10
S2394 Naringenin Naringenin is a natural predominant flavanone derived from plant food, which is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.
S4221 Benzbromarone Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
S2555 Clarithromycin Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.
S2900 Cobicistat (GS-9350) Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.
S2921 PF-4981517 PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.
S2067 Ozagrel HCl Ozagrel HCl is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
S2496 Ozagrel Ozagrel is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
S1195 TAK-700 (Orteronel) TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3.
  • Biochem Biophys Res Commun, 2016, 477(4):1005-10
S2046 Pioglitazone HCl Pioglitazone HCl is a selective peroxisome proliferator-activated receptor-gamma (PPARgamma) agonist, used to treat diabetes.
  • Drug metab dispos, 2013, 42(3):318-22
S2526 Alizarin Alizarin strongly inhibits P450 isoform CYP1A1, CYP1A2 and CYP1B1 with IC50 of 6.2 μM, 10.0 μM and 2.7 μM, respectively; weakly inhibits CYP2A6 and CYP2E1, and does not inhibit CYP2C19, CYP3A4 and CYP3A5.
S2401 Sodium Danshensu Sodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza.
S2329 Naringin Naringin is a flavanone glycoside, which exerts a variety of pharmacological effects such as antioxidant activity, blood lipid lowering, anticancer activity, and inhibition of cytochrome P450 enzymes.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1123 Abiraterone 0.02 mg/mL 0.1 mg/mL 0.2 mg/mL
S2246 Abiraterone Acetate <1 mg/mL <1 mg/mL 28 mg/mL
S1442 Voriconazole <1 mg/mL 70 mg/mL 20 mg/mL
S2187 Avasimibe <1 mg/mL 100 mg/mL 8 mg/mL
S1353 Ketoconazole <1 mg/mL 5 mg/mL 7 mg/mL
S2476 Itraconazole <1 mg/mL 7 mg/mL <1 mg/mL
S1331 Fluconazole <1 mg/mL 61 mg/mL 61 mg/mL
S2268 Baicalein <1 mg/mL 54 mg/mL <1 mg/mL
S2262 Apigenin <1 mg/mL 54 mg/mL <1 mg/mL
S2344 Piperine <1 mg/mL 57 mg/mL 57 mg/mL
S2380 Diosmetin <1 mg/mL 60 mg/mL <1 mg/mL
S2803 Galeterone <1 mg/mL 24 mg/mL 40 mg/mL
S2394 Naringenin <1 mg/mL 54 mg/mL 5 mg/mL
S4221 Benzbromarone <1 mg/mL 85 mg/mL 9 mg/mL
S2555 Clarithromycin <1 mg/mL 25 mg/mL <1 mg/mL
S2900 Cobicistat (GS-9350) <1 mg/mL 100 mg/mL 100 mg/mL
S2921 PF-4981517 <1 mg/mL 91 mg/mL <1 mg/mL
S2067 Ozagrel HCl 53 mg/mL 53 mg/mL 6 mg/mL
S2496 Ozagrel <1 mg/mL 46 mg/mL <1 mg/mL
S1195 TAK-700 (Orteronel) <1 mg/mL 61 mg/mL 8 mg/mL
S2046 Pioglitazone HCl <1 mg/mL 79 mg/mL 4 mg/mL
S2526 Alizarin <1 mg/mL 48 mg/mL <1 mg/mL
S2401 Sodium Danshensu 2 mg/mL 7 mg/mL <1 mg/mL
S2329 Naringin <1 mg/mL 116 mg/mL 2 mg/mL
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