CYP2 选择性抑制剂 | 化学产品

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S4221 Benzbromarone

Benzbromarone 是CYP2C9抑制剂,与CYP2C9 结合,Ki为19.3 nM。

Selective CYP2C9, Ki: 19.3 nM
S1794 Fenofibrate (NSC-281319)

Fenofibrate 是一种Fibrate类化合物,是纤维酸衍生物。

Selective CYP2C9, IC50: 9.7 μM; CYP2B6, IC50: 0.7 μM; CYP2C19, IC50: 0.2 μM
S0721 Ticlopidine

Ticlopidine is an inhibitor of adenosine diphosphate (ADP) receptor and an antiplatelet drug in the thienopyridine family.

Selective CYP2B6, Ki: 0.2 μM
S3673 Sulfaphenazole

Sulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).

Selective CYP2C9, Ki: 0.3 μM
S2262 Apigenin (LY 080400)

Apigenin是一种有效的CYP2C9抑制剂,Ki为2 μM.。

Selective CYP2C9, Ki: 2 μM
S0110 APD597

APD597 is a potent GPR119 agonist with EC50 of 46 nM for hGPR119. APD597 is intended for the treatment of type 2 diabetes.

Selective CYP2C9, IC50: 5.8 μM
S4741 Danshensu


Selective CYP2C9, IC50: 75.76 μM; CYP2E1, IC50: 36.63 μM
S9241 Polygalaxanthone III

Polygalaxanthone III is a natural product with the efficacy of tranquilization, glaangal, eliminating sputum and detumescence. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.

Selective CYP2E1, IC50: 50.56 μM
S3777 Gentiopicroside

Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.

S1952 Methoxsalen


S2268 Baicalein


S5658 Omeprazole Sodium

Omeprazole Sodium is the sodium salt form of omeprazole, which is a proton pump inhibitor and suppresses gastric acid secretion. Omeprazole Sodium is a metabolism-dependent inhibitor (MDI) of CYP2C19.

S4938 Cedrol

Cedrol, a natural occuring sesquiterpene alcohol, is a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) value of 0.9 μM. It also inhibits CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 μM while only weakly inhibits CYP2C8, CYP2C9, and CYP2C19 activities.

Pan CYP2B6, Ki: 0.9 μM
S2046 Pioglitazone HCl

Pioglitazone HCl是Pioglitazone的盐酸盐形式,是细胞色素P450 (CYP)2C8和CYP3A4酶抑制剂,作用于CYP2C8, CYP3A4和CYP2C9, Ki分别为1.7 μM, 11.8 μM和32.1 μM。

Pan CYP2C8, Ki: 1.7 μM; CYP2C9, Ki: 32.1 μM
S2187 Avasimibe (CI-1011)

Avasimibe抑制ACATIC50为3.3 μM,也抑制人P450同工酶CYP2C9, CYP1A2和CYP2C19,IC50分别为2.9 μM, 13.9 μM和26.5 μM,

Pan CYP2C9, IC50: 2.9 μM; CYP2C19, IC50: 26.5 μM
S3931 Ginsenoside Rd

Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP

Pan CYP2D6, IC50: 58.0 μM; CYP2C9, IC50: 85.1 μM