RO-9187是高效的HCV病毒复制抑制剂，IC₅₀值为171 nM。

RO-9187 is a potent inhibitor of HCV virus replication with an IC 50 of 171 nM.

Solid

IC50: 171 nM (HCV)

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

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

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Klumpp K, et al. 2-deoxy-4-azido nucleoside analogs are highly potent inhibitors of hepatitis C virus replication despite the lack of 2-alpha-hydroxyl groups. J Biol Chem. 2008 Jan 25;283(4):2167-75.

In Vitro: DMSO : 100 mg/mL (351.83 mM; Need ultrasonic)H₂O : 7.14 mg/mL (25.12 mM; Need ultrasonic)配制储备液