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Sofosbuvir

产品编号 T6676Cas号 1190307-88-0
别名 GS 7977, PSI-7977, 索非布韦

Sofosbuvir (GS 7977) 是一种丙型肝炎病毒聚合酶 NS5B 的尿苷单磷酸类似物抑制剂,用作治疗慢性丙型肝炎的抗病毒剂。

Sofosbuvir

Sofosbuvir

纯度: 99.93%
产品编号 T6676 别名 GS 7977, PSI-7977, 索非布韦Cas号 1190307-88-0

Sofosbuvir (GS 7977) 是一种丙型肝炎病毒聚合酶 NS5B 的尿苷单磷酸类似物抑制剂,用作治疗慢性丙型肝炎的抗病毒剂。

规格价格库存数量
1 mg¥ 152现货
5 mg¥ 297现货
10 mg¥ 413现货
50 mg¥ 529现货
100 mg¥ 637现货
500 mg¥ 892现货
1 g¥ 1,160现货
1 mL x 10 mM (in DMSO)¥ 356现货
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纯度:99.93%
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产品介绍

生物活性
产品描述
Sofosbuvir (GS 7977) is a uridine monophosphate analog inhibitor of hepatitis C virus (HCV) polymerase NS5B that is used as an antiviral agent in the treatment of chronic hepatitis C.
靶点活性
HCV RNA:92 nM(EC50)
体外活性
As HCV NS5B polymerase inhibitor, PSI-7977 displays more potent inhibitory activity against HCV RNA replication than PSI-7976 with EC50 of 92 nM versus 1.07 μM and EC90 of 0.29 μM versus 2.99 μM, consistent with that incubating clone A cells with PSI-7977 leads to a higher concentration of PSI-7409 than clone A cells incubated with PSI-7976. PSI-7977 is an effective substrate for CatA to form PSI-352707 with 18-30 fold more potency as compared with PSI-7976. Unlike GS-7976, however, the CES1-mediated hydrolysis of PSI-7977 does not progress in a time-dependent manner. [1] The S282T NS5B polymerase mutation but not S96T mutation confers resistance to PSI-7977 with EC90 increases from 0.42 μM to 7.8 μM. When assessed in an 8-day cytotoxicity assay, PSI-7977 displays no cytotoxicity against Huh7, HepG2, BxPC3, and CEM cells even at concentrations up to 100 μM. PSI-7977 treatment for 14 days shows a IC90 of 72.1 μM and 68.6 μM for the inhibition of mtDNA and rDNA, respectively, in HepG2 cells. [2] PSI-7977 exhibits potent activity against genotype (GT) 1a, 1b, and 2a (strain JFH-1) replicons and chimeric replicons containing GT 2a (strain J6), 2b, and 3a NS5B polymerase. Sequence analysis of the JFH-1 NS5B region indicates that additional amino acid changes including T179A, M289L, I293L, M434T, and H479P are selected both prior to and after the emergence of S282T, which are required to confer resistance to PSI-7977. [3]
激酶实验
PTEN Inhibition Assay: To determine the dose response of potential PTEN inhibitors, doses of test compounds ranging from 1 nM to 250 uM (final reaction mix concentrations) are evaluated in the general PTEN inhibition assay. To obtain performed IC50 data, two separate rounds of the dose response assay are performed. In the first round, PTEN activity is tested in the presence of inhibitor at 10 fold serial dilutions ranging from 1 nM to 250 uM. Once the concentration range is determined, at which PTEN activity changes dramatically, two additional concentration data points within this range are added and the PTEN inhibition assay is then rerun for the second round. The PTEN inhibition IC50 is presented as the inhibitor concentration at which 50% of the PTEN activity. When the assay was run on multiple occasions and gave slightly different IC50 then those are reported as a range of IC50 found.
细胞实验
Cells are exposed to various concentrations of PSI-7977 for 8 days. At the end of the growth period, MTS dye from the CellTiter 96 AQueous One Solution Cell Proliferation Assay kit is added to each well, and the plate is incubated for an additional 2 hours. The absorbance at 490 nm is read with a Victor3 plate reader using themedium only controlwells as blanks. The 50% inhibition value (IC50) is determined by comparing the absorbance in wells containing cells and PSI-7977 to untreated cell control wells.(Only for Reference)
别名GS 7977, PSI-7977, 索非布韦
化学信息
分子量529.45
分子式C22H29FN3O9P
CAS No.1190307-88-0
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 93 mg/mL (175.7 mM)
DMSO: 60 mg/mL (113.33 mM)
H2O: 9 mg/mL (17 mM)
溶液配制表
H2O/DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.8888 mL9.4438 mL18.8875 mL94.4376 mL
5 mM0.3778 mL1.8888 mL3.7775 mL18.8875 mL
10 mM0.1889 mL0.9444 mL1.8888 mL9.4438 mL
DMSO/Ethanol
1mg5mg10mg50mg
20 mM0.0944 mL0.4722 mL0.9444 mL4.7219 mL
50 mM0.0378 mL0.1889 mL0.3778 mL1.8888 mL
100 mM0.0189 mL0.0944 mL0.1889 mL0.9444 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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