Filibuvir 

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^[1]. Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation^[2].

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^[2].
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^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

503.64

C₂₉H₃₇N₅O₃

877130-28-4

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

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• [1]. Wagner F, et al. Antiviral activity of the hepatitis C virus polymerase inhibitor filibuvir in genotype 1-infected patients. Hepatology. 2011 Jul;54(1):50-9.  [Content Brief]

  [2]. Guanghui Yi, et al. Biochemical study of the comparative inhibition of hepatitis C virus RNA polymerase by VX-222 and filibuvir. Antimicrob Agents Chemother. 2012 Feb;56(2):830-7.  [Content Brief]