Cobicistat

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Cobicistat

CAS No. : 1004316-88-4

MCE 国际站：Cobicistat

产品活性：Cobicistat 是有效，选择性的细胞色素酶 P450 3A (CYP3A) 抑制剂，IC₅₀ 值为30-285 nM。 Cobicistat 是一种药代动力学增强剂，可增强抗 HIV 活性分子的吸收。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Cytochrome P450  |  HIV

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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