RO-9187

RO-9187是高效的HCV病毒复制抑制剂，IC50值为171 nM。

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库存: 现货

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5mg

￥2787.00

2230.00

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50mg

￥9725.00

7780.00

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100mg

￥0.00

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200mg

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货号: ajce59342
CAS: 876708-03-1
别名: 4-氨基-1-(4-C-叠氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮
分子式: C9H12N6O5
分子量: 284.23
纯度: >98%
溶解度: Water: 7.14 mg/mL (25.12 mM)
储存: Store at -20°C
库存: 现货

Background

RO-9187 is a potent inhibitor of HCV virus replication with an IC50 of 171 nM. IC50: 171 nM (HCV)[1]

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[1].

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[1].

[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.

Protocol

Animal experiment:

Rats: A 2-week oral range finding toxicity study is performed with RO-9187 and ribavirin in Hanover-Wistar rats. Five male and five female rats in each of five treatment groups are administered once daily doses of vehicle, 200, 600, or 2000 mg/kg RO-9187 or 200 mg/kg ribavirin by oral gavage for 14 days[1].

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