RO-9187

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

一种有效的 HCV NS5B RNA 聚合酶抑制剂；抑制复制子系统中的 HCV 复制，IC50 为 171 nM。

A potent HCV NS5B RNA polymerase inhibitor; inhibits HCV replication in the replicon system with IC50 of 171 nM; RNA synthesis by HCV polymerases from either HCV genotypes 1a and 1b or containing S96T or S282T point mutations (IC50=600-1100 nM); shows good oral bioavailability in rats and no toxicologically significant findings.

RO-9187 is excellent substrates for deoxycytidine kinase and is phosphorylated with efficiencies up to 3-fold higher than deoxycytidine. RO-9187 inhibits RNA synthesis by HCV polymerases from either HCV genotypes 1a and 1b or containing S96T or S282T point mutations with similar potencies, suggesting no cross-resistance with either R1479 (4′-azidocytidine) or 2′-C-methyl nucleosides. The formation of RO-9187-TP increased in a time- and dose-dependent manner. The maximal triphosphate concentration at 24 h is 87 pmol/106 cells with half-maximal triphosphate formation achieved at 12 μM RO-9187.

Plasma exposures of RO-9187 in rats increase in a dose-dependent manner between 10 and 2000 mg/kg after oral dosing. Plasma concentrations of 1.4 and 26 μM (390 and 7454 ng/mL) are achieved in rats and dogs at the 10 mg/kg dose level, respectively. Plasma concentrations up to 57 μM are achieved in rats dosed with 2000 mg/kg/day.

RO 9187 | RO9187

Microbiology/Virology

HCV

HCV

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876708-03-1

284.2288

C9H12N6O5

>98% (HPLC)

10 mM in DMSO

C1=CN(C(=O)N=C1N)C2C(C(C(O2)(CO)N=[N+]=[N-])O)O

2(1H)-Pyrimidinone, 4-amino-1-(4-C-azido-β-D-arabinofuranosyl)-

(-20℃)

With Ice Pack

≥ 2 years