Nesbuvir  ≥98%

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包装规格:5mg in glass bottle
溶解性:溶于DMSO(≥ 50 mg/mL)
产品描述:基本信息 产品编号:N10415 产品名称:Nesbuvir CAS: 691852-58-1   储存条件 粉末 -20℃ 四年     分子式: C22H23FN2O5S 溶于液体 -80℃ 六个月 分子量 446.49 -20℃ 一个月 化学名:  5-Cyclopropyl-2-(4-fluorophenyl)-6-((2-hydroxyethyl)(methylsulfonyl)amino)-N-methyl-1-benzofuran-3-carboxamide   Solubility (25°C)   体外 DMSO ≥50mg/mL (111.98mM) Ethanol   Water   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 2.2397mL 11.1985mL 22.3969mL 5mM 0.4479mL 2.2397mL 4.4794mL 10mM 0.2240mL 1.1198mL 2.2397mL   生物活性 产品描述 一种非核苷抑制剂,抑制丙型肝炎病毒非结构蛋白聚合酶。 靶点/IC50 NS3V170A EC50: 9nM NS3V170A 13nM NS3K583T 15nM NS5BI424V 13nM   体外研究 Replicon cells are treated with 1 mg/mL G418 and combinations of the two compounds. Nesbuvir (HCV-796) is added to 40 or 80nM (approximately 10 and 20 times the EC50 in a 3-day replicon inhibition assay, respectively) and Boceprevir is added to 400 or 800nM (approximately 2 and 4 times the EC50, respectively). The EC50s for Nesbuvir and Boceprevir for the parental replicon in the transient expression assay are comparable to those obtained in the 3-day inhibition assay with the stable replicon cells; the EC50 for Nesbuvir in the transient expression assay is 14nM, whereas it is 5nM for the stable replicon; and the EC50 for Boceprevir in the transient expression assay is 608nM, whereas it is 201nM for the stable replicon.   体内研究 Among a huge variety of yet characterized nucleoside and non-nucleoside inhibitors (NNI), the benzofurane derivative NNI Nesbuvir (HCV-796) is demonstrated to yield significant antiviral effects in mice with chimeric human livers and in patients infected with HCV. HCV-796 binds to a hydrophobic binding pocket at the “palm” domain of NS5B; however, its mode of inhibition remains to be defined.   推荐实验方法(仅供参考) 细胞实验:   Cell Assay Huh7-BB7 cells are seeded at a density of 20,000 cells per 100 mm dish in DMEM supplemented with 2% FBS, 1 mg/mL G418,and various concentrations of Nesbuvir and/or Boceprevir with DMSO at a final concentration of 0.5% (vol/vol). The medium is removed and is replaced with fresh medium with the appropriate compound concentrations every 3 or 4 days. After 7 days, the cells are split 1 to 10, placed into fresh 100 mm dishes, and incubated with medium with the appropriate compound concentrations. After 20 days, the medium is removed and the cells are fixed with 7% (wt/vol) formaldehyde and stained with 1% (wt/vol) crystal violet in 50% (vol/vol) ethanol.
保存条件:-20℃