化合物Nesbuvir TQ0090

Product Introduction
Bioactivity


英文名: Nesbuvir

描述: Nesbuvir 是一种选择性丙型肝炎病毒（HCV）非结构蛋白5B（NS5B）RNA 依赖性聚合酶抑制剂。Nesbuvir 对含1b HCV 复制子的肝癌细胞的 IC50为9nM。

细胞实验: 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 a 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 [1].

体外活性: Nesbuvir (40 or 80 nM) (approximately 10 and 20 times the EC50 in a 3-day replicon inhibition assay, respectively). The EC50 for Nesbuvir in the transient expression assay is 14 nM, whereas it is 5 nM for the stable replicon.[1]Nesbuvir (0.1 and 1 μM; Huh-7 cells; for 16 days) reduced about 3.6 log10 and 4.2 log10 HCV RNA levels, respectively.[3]

体内活性: Nesbuvir is demonstrated to yield significant antiviral effects in mice with chimeric human livers and in patients infected with HCV.[2] Nesbuvir (chimeric mouse model) treatment resulted in a 2.02 +/- 0.55 log reduction in HCV titer, whereas in combination with interferon using a suboptimal dose of 30 mg/kg three times per day showed a 2.44 log reduction and were better than interferon treatment only.[5]

存储条件: keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45.0 mg/mL (100.8 mM)


关键字: Nesbuvir | HCV 796 | HCV796

相关产品: U18666A | Deapioplatycodin D | Gentiopicroside | Tris(4-aminophenyl)methane | Boceprevir | 2′-O-Methylcytidine | Velpatasvir | JTK-109 | Trachelogenin | 2',5-Difluoro-2'-deoxycytidine

相关库: Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Bioactive Compound Library

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