产品
编 号:F578224
分子式:C29H37N5O3
分子量:503.64
产品类型
结构图
CAS No: 877130-28-4
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产品详情
生物活性:
Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively. Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation.
体外研究:
Filibuvir (0.01-10000 nM; 48 h) inhibits the WT 1b replicon in a dose-dependent manner, with an EC50 of ~70 nM in Huh7.5 cells harboring the HCV replicon. Filibuvir binds to the HCV polymerase with a dissociation constant of 29 nM. Filibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis. Filibuvir has no obvious effect on de novo-initiated RNA synthesis (IC50=~5 μM) but decreases primer extension from PE46, with an IC50 of 73 nM.