Cobicistat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种化合物增强剂，可作为人 CYP3A 的有效选择性抑制剂，IC50 为 30-285 nM。

A pharmacoenhancer that acts as potent and selective inhibitor of human CYP3A with IC50 of 30-285 nM; more selective than RTV with much reduced inhibitory activity toward CYP2D6, CYP2C8, and CYP2C9.HIV Infection Approved(In Vitro):In HIV-1 protease enzymatic assay and antiviral cellular assays. Cobicistat is inactive against HIV-1 protease (IC50>30 μM) . And Cobicistat has no inhibitory effect against HIV replication in a multicycle 5-day MT-2 HIV infection assay (EC50>30 μM). In assays using MT-2 cells, Cobicistat exhibits minimal cytotoxicity, with a CC50 value above 80 μM.The mode of inhibition of human CYP3A by Cobicistat and Ritonavir shares the same mechanism of action for the inhibition of CYP3A. It shows its inhibitory effects on CYP3A may involve directly at the heme group of the CYP3A enzyme.The minimal adverse effects of Cobicistat in these assays suggest a lower potential for toxicity related to altered lipid metabolism.In the lipid accumulation assay with the human adipocytes, Ritonavir shows a clear effect with an EC50 of 16 μM. However, Cobicistat exhibits no effect at a concentration up to 30 μM.In the glucose uptake assay with mouse adipocytes, Ritonavir shows a pronounced effect at the concentration of 10 μM. In contrast, the effects on glucose uptake by Cobicistat (10 μM) is significantly less.

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GS-9350 | GS 9350 | GS9350

Metabolic Enzyme/Protease

CYPs

CYP3A

Infection

HIV Infection

1004316-88-4

776.0227

C40H53N7O5S2

>98% (HPLC)

DMSO: ≥ 29 mg/mL

O=C(OCC1=CN=CS1)N[C@H](CC[C@@H](NC([C@@H](NC(N(CC2=CSC(C(C)C)=N2)C)=O)CCN3CCOCC3)=O)CC4=CC=CC=C4)CC5=CC=CC=C5

2,7,10,12-Tetraazatridecanoic acid, 12-methyl-13-[2-(1-methylethyl)-4-thiazolyl]-9-[2-(4-morpholinyl)ethyl]-8,11-dioxo-3,6-bis(phenylmethyl)-, 5-thiazolylmethyl ester, (3R,6R,9S)-

(-20℃)

With Ice Pack

≥ 2 years