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.
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.
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.
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.
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 3 mg/mL 7 mg/mL
S2476 Itraconazole <1 mg/mL 4 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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