Filibuvir

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

Filibuvir (PF-00868554;PF-868554) 是一种非核苷、有效、选择性、口服 HCV NS5B 抑制剂，IC50 为 19 nM，EC50 为 75 nM。

Filibuvir (PF-00868554;PF-868554) is a nonnucleoside, potent and selective, orally available HCV NS5B inhibitor with IC50 of 19 nM, EC50 of 75 nM (genotype 1b-Con1 replicon); has potent in vitro antiviral activity against a majority (95.8%) of genotype 1a and 1b replicons with an overall mean EC50 of 59 nM, without cytotoxic effect in several human cell lines (CC50>320 uM); exhibits good pharmacokinetic properties in preclinical animal species.HCV Infection Phase 2 Discontinued.

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.

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PF-00868554 | PF-868554

Microbiology/Virology

HCV

HCV

Infection

HCV Infection

877130-28-4

503.636

C29H37N5O3

>98% (HPLC)

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O=C1C(CC2=NN3C(C)=CC(C)=NC3=N2)=C(O)C[C@](CCC4=CC(CC)=NC(CC)=C4)(C5CCCC5)O1

(R)-6-Cyclopentyl-6-[2-(2,6-diethylpyridin-4-yl)ethyl]-3-[(5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl]-4-hydroxy-5,6-dihydro-2H-pyran-2-one

(-20℃)

With Ice Pack

≥ 2 years