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

Danshensu(丹参素),是一种传统中药中的中草药,具有潜在的抗肿瘤和抗血管生成的效果。

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.

Selective
S1952 Methoxsalen

Methoxsalen是在一些植物中发现的天然存在的呋喃香豆素化合物,包括补骨脂,用于治疗牛皮癣,湿疹,白癜风及一些暴露在阳光下的皮肤淋巴瘤。是CYP2A5/6抑制剂。

Selective
S2268 Baicalein

Baicalein是CYP2C9和脯氨酰肽链内切酶抑制剂。

Selective
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.

Selective
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