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Tegobuvir

CAS No. : 1000787-75-6

MCE 国际站：Tegobuvir

产品活性：Tegobuvir 是一种特异性的，共价的 HCV NS5B polymerase 抑制剂。

研究领域：Anti-infection

作用靶点：HCV

In Vitro: Tegobuvir rapidly increases the proportion of replicons with the Y448H mutation in a dose-dependent manner. After 3 days of treatment, 1.2%, 6.8%, and > 50% of the replicon population expresses Y448H with the use of Tegobuvir at 1, 10, and 20 times its 50% effective concentration, respectively. Tegobuvir exerts anti-HCV activity utilizing a unique chemical activation and subsequent direct interaction with the NS5B protein. Treatment of HCV subgenomic replicon cells with Tegobuvir results in a modified form of NS5B with a distinctly altered mobility on a SDS-PAGE gel. Tegobuvir is potent in GT1a and 1b with mean EC₅₀s of 19.8 and 1.5 nM respectively. For genotype 3a, 4a, and 6a Con chimeras, tegobuvir EC₅₀s are all greater than 100 nM. The F445C NS5B mutations in GT3a, 4a, and 6a chimeric replicons restore tegobuvir potency to EC₅₀ levels comparable to GT1a.

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