CYP1 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S1739 Thiabendazole

Thiabendazole 抑制线粒体蠕虫特异性酶,延胡索酸还原酶,具有驱虫药的性能。是一种有效的CYP1A2的抑制剂。

Selective
S0176 DMU2139

DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.

Selective CYP1B1, IC50: 9 nM
S0175 DMU2105

DMU2105 is a potent and specific inhibitor of CYP1B1 with IC50 of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.

Selective CYP1B1, IC50: 10 nM
S5380 7-Hydroxyflavone

7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.

Selective CYP1A1, Ki: 0.015 μM
S9163 Rhapontigenin

Rhapontigenin (Protigenin), produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).

Selective CYP1A1, IC50: 400 nM
S2526 Alizarin

Alizarin强效抑制P450亚型CYP1A1, CYP1A2和CYP1B1IC50分别为6.2 μM, 10.0 μM and 2.7 μM,微弱抑制CYP2A6和CYP2E1,对CYP2C19,对CYP3A4和CYP3A5没有抑制作用。

Selective CYP1A1, IC50: 6.2 μM; CYP1A2, IC50: 10.0 μM; CYP1B1, IC50: 2.7 μM
S3291 Myristicin

Myristicin (Myristicine), a terpene-like active component in Nutmeg which is the seed of Myristica fragrans, is a weak inhibitor of monamine oxidase (MAO) and a mechanism-based inhibitor of CYP1A2.

Selective
S2394 Naringenin

Naringenin是来自于食用植物的一种天然的主要黄酮类化合物,有益人体健康,具有生物活性,是一种抗氧化剂,自由基清除剂,抗炎,碳水化合物代谢启动子及免疫系统的调制剂。

Selective
S2380 Diosmetin

Diosmetin 是在Spearmint, Oregano, 和许多其他植物中发现的生物类黄酮。

Selective
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 CYP1A2, IC50: 13.9 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 CYP1A2, IC50: 78.4 μM