Cobicistat,1004316-88-4

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抑制剂描述：

产品名称：Cobicistat

产品别名：见爱必信官网

英文别名：Cobicistat

靶点：P450

CAS：1004316-88-4

纯度：98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC₅₀ of 30-285 nM.

溶解性：DMSO : 250 mg/mL (322.16 mM; Need ultrasonic)

体外研究：

Cobicistat (GS-9350) is a potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes as a pharmacoenhancer. GS-9350 inhibits CYP3A with IC₅₀ spectrum from 30 nM to 285 nM. In contrast to ritonavir, GS-9350 is devoid of anti-HIV activity, with IC₅₀ of > 30 μM against HIV-1 protease and EC₅₀ of > 30μM in MT-2 HIV infection assay, and is thus more suitable for use in boosting anti-HIV drugs without risking selection of potential drug-resistant HIV variants. GS-9350 shows reduced liability for drug interactions and may have potential improvements in tolerability over ritonavir. Cobicistat is a novel cytochrome P450 3A4 inhibitor in advanced clinical evaluation for use as a pharmacoenhancer of antiretroviral drugs. It lacks significant anti-HIV activity and is more selective than ritonavir in its enzyme inhibition.

体内研究：

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