876708-03-1
基本信息
RO 9187
RO9187
4-Amino-1-(4-C-azido-beta-D-arabinofuranosyl)-2(1H)-pyrimidinone
物理化學性質
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-10870 | 4-氨基-1-(4-C-疊氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮 RO-9187 | 876708-03-1 | 5mg | 2000元 |
2024/11/08 | HY-10870 | 4-氨基-1-(4-C-疊氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮 RO-9187 | 876708-03-1 | 10 mM * 1 mLin DMSO | 2200元 |
2024/11/08 | HY-10870 | 4-氨基-1-(4-C-疊氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮 RO-9187 | 876708-03-1 | 10mg | 3400元 |
常見問題列表
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.
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.