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Nesbuvir

Nesbuvir

产品编号 TQ0090   CAS 691852-58-1
别名: HCV-796

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。

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Nesbuvir Chemical Structure
Nesbuvir, CAS 691852-58-1
规格 价格/CNY 货期 数量
1 mg ¥ 736 现货
5 mg ¥ 1,820 现货
10 mg ¥ 2,570 现货
25 mg ¥ 4,190 现货
50 mg ¥ 5,970 现货
100 mg ¥ 8,190 现货
500 mg ¥ 16,300 现货
1 mL * 10 mM (in DMSO) ¥ 1,960 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: Nesbuvir (TQ0090)
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纯度: 98.72%
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生物活性
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存储 & 溶解度
参考文献
产品描述 Nesbuvir is a selective hepatitis C virus (HCV) nonstructural protein 5B (NS5B) RNA-dependent polymerase inhibitor.Nesbuvir has an IC50 of 9 nM against hepatocellular carcinoma cells containing 1b HCV replicons.
靶点活性 NS3V170A:13 nM (EC50), NS3V170A:9 nM (EC50), NS5BI424V:13 nM (EC50), NS3K583T:15 nM (EC50), NS5B:5 nM
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]
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].
别名 HCV-796
分子量 446.49
分子式 C22H23FN2O5S
CAS No. 691852-58-1

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 45.0 mg/mL (100.8 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2397 mL 11.1985 mL 22.3969 mL 55.9923 mL
5 mM 0.4479 mL 2.2397 mL 4.4794 mL 11.1985 mL
10 mM 0.224 mL 1.1198 mL 2.2397 mL 5.5992 mL
20 mM 0.112 mL 0.5599 mL 1.1198 mL 2.7996 mL
50 mM 0.0448 mL 0.224 mL 0.4479 mL 1.1198 mL
100 mM 0.0224 mL 0.112 mL 0.224 mL 0.5599 mL

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TargetMol Library Books参考文献

1. Flint M, et al. Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034). Antimicrob Agents Chemother. 2009;53(2):401-411. 2. Reich S, et al. Mechanisms of activity and inhibition of the hepatitis C virus RNA-dependent RNA polymerase. J Biol Chem. 2010;285(18):13685-13693. 3. Howe AY, et al. Molecular mechanism of hepatitis C virus replicon variants with reduced susceptibility to a benzofuran inhibitor, HCV-796. Antimicrob Agents Chemother. 2008;52(9):3327-3338. 4. Meshram RJ, et al. Effective epitope identification employing phylogenetic, mutational variability, sequence entropy, and correlated mutation analysis targeting NS5B protein of hepatitis C virus: from bioinformatics to therapeutics. J Mol Recognit. 2015;28(8):492-505. 5. Kneteman NM, et al. HCV796: A selective nonstructural protein 5B polymerase inhibitor with potent anti-hepatitis C virus activity in vitro, in mice with chimeric human livers, and in humans infected with hepatitis C virus. Hepatology. 2009;49(3):745-752.
Sofosbuvir impurity N Boceprevir 2'-C-Methyladenosine Inarigivir soproxil Lycorine hydrochloride U18666A Paritaprevir Deferiprone

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 药物功能重定位化合物库 已知活性化合物库 经典已知活性库 临床期小分子药物库

TargetMol Calculator剂量换算

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Nesbuvir 691852-58-1 Microbiology/Virology Proteases/Proteasome HCV Protease HCV-796 HCV 796 HCV796 Inhibitor inhibitor inhibit

 

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