Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 369 | 现货 | ||
10 mg | ¥ 497 | 现货 | ||
50 mg | ¥ 637 | 现货 | ||
100 mg | ¥ 764 | 现货 | ||
500 mg | ¥ 1,098 | 现货 | ||
1 g | ¥ 1,297 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 423 | 现货 |
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 | 索非布韦, GS 7977, PSI-7977 |
分子量 | 529.45 |
分子式 | C22H29FN3O9P |
CAS No. | 1190307-88-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 93 mg/mL (175.7 mM)
DMSO: 93 mg/mL (175.7 mM)
H2O: 9 mg/mL (17 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO / H2O | 1 mM | 1.8888 mL | 9.4438 mL | 18.8875 mL | 47.2188 mL |
5 mM | 0.3778 mL | 1.8888 mL | 3.7775 mL | 9.4438 mL | |
10 mM | 0.1889 mL | 0.9444 mL | 1.8888 mL | 4.7219 mL | |
Ethanol / DMSO | 20 mM | 0.0944 mL | 0.4722 mL | 0.9444 mL | 2.3609 mL |
50 mM | 0.0378 mL | 0.1889 mL | 0.3778 mL | 0.9444 mL | |
100 mM | 0.0189 mL | 0.0944 mL | 0.1889 mL | 0.4722 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Sofosbuvir 1190307-88-0 Microbiology/Virology Proteases/Proteasome HCV Protease 索非布韦 inhibit Inhibitor HCV GS7977 GS 7977 PSI7977 PSI-7977 Hepatitis C virus GS-7977 PSI 7977 inhibitor