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Cobicistat(GS-9350)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cobicistat(GS-9350)图片
CAS NO:1004316-88-4
规格:98%
分子量:776.02
包装与价格:
包装价格(元)
5mg电议
10mg电议
200mg电议

产品介绍
Selective CYP3A inhibitor
CAS:1004316-88-4
分子式:C40H53N7O5S2
分子量:776.02
纯度:98%
存储:Store at -20°C

Background:

Cobicistat is a selective inhibitor of cytochrome P450 (CYP) 3A enzymes with IC50 values ranging from 0.03 to 0.285μM [1].


Cobicistat is a selective CYP3A inhibitor without intrinsic anti-HIV activity and is indicated in EU as a pharmacokinetic enhancer of the HIV-1 protease inhibitors atazanavir and darunavir in adults. Cobicistat is also developed to form a fixed-dose tablet in combination with elvitegravir, emtricitabine and TDF. Cobicistat inhibits CYP3A in vitro across a variety of substrates with IC50 values ranging from 0.03 to 0.285μM. Cobicistat is absorbed rapidly after oral administration in patients infected with HIV-1 with the Cmax of 1.2μg/ml. In the 48-week analysis of the phase III study, once-daily oral cobicistat is generally well tolerated. The tolerability of the cobicistat-boosted atazanavir remains similar longer term, with jaundice, ocular icterus and nausea in a 96-week analysis of the phase III study [1].


参考文献:
[1] Deeks ED. Cobicistat: a review of its use as a pharmacokinetic enhancer of atazanavir and darunavir in patients with HIV-1 infection. Drugs. 2014 Feb;74(2):195-206.