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RO-9187  ≥98%

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包装规格：10mg in glass bottle
产品描述：基本信息 产品编号：R10205 产品名称：RO-9187 CAS: 876708-03-1   储存条件 粉末 -20℃ 四年     分子式： C9H12N6O5 溶于液体 -80℃ 六个月 分子量 284.23 -20℃ 一个月 化学名：  4-Amino-1-[(2r,3s,4s,5r)-5-azido-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one   Solubility (25°C)   体外 DMSO   Ethanol   Water 7mg/mL (24.63mM; Need ultrasonic) 体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.5183mL 17.5914mL 35.1828mL 5mM 0.7037mL 3.5183mL 7.0366mL 10mM 0.3518mL 1.7591mL 3.5183mL   生物活性 产品描述 一种高效的HCV病毒复制抑制剂，IC50值为171nM。 靶点/IC50 HCV IC50: 171nM   体外研究 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′-Cmethyl 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 12μM RO9187   体内研究 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.   推荐实验方法(仅供参考) 动物实验:   Animal Administration 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 2000mg/kg RO-9187 or 200mg/kg ribavirin by oral gavage for 14 days.
保存条件：-20℃

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