Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PSI-6206 (RO 2433) 是 PSI-6130 的脱氨衍生物,PSI-6206 是一种选择性 HCV RNA 聚合酶抑制剂,低效抑制HCV 复制,EC90为 <100 μM。PSI-6130 是一种有效的选择性 HCV NS5B 聚合酶抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 113 | 现货 | ||
5 mg | ¥ 228 | 现货 | ||
10 mg | ¥ 328 | 现货 | ||
25 mg | ¥ 547 | 现货 | ||
50 mg | ¥ 793 | 现货 | ||
100 mg | ¥ 1,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 293 | 现货 |
产品描述 | PSI-6206 (RO 2433) (RO2433) is a selective HCV RNA polymerase inhibitor. |
体外活性 | PSI-6206 (RO2433) is tested for anti-HCV activity in both a cell-based quantitative real-time RT-PCR assay and surrogate bovine viral diarrhea virus (BVDV) assays and demonstrates no activity or cytoxicity in any assay[1]. The formation of the 5′-triphosphate (TP) of PSI-6130 (PSI-6130-TP) and RO2433 (RO2433-TP) increases with time and reached steady state levels at 48 h. RO2433-TP also inhibits RNA synthesis by the native HCV replicase isolated from HCV replicon cells and the recombinant HCV polymerase NS5B[2]. PSI-6206 (RO2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase[3]. |
激酶实验 | Protein Kinase Assays: The in vitro kinase assays are performed in 96-well plates (30 μL) at ambient temperature for 15–45 min using the recombinant glutathione S-transferase-fused kinase domains (4-100 ng, depending on specific activity). [γ33P]ATP is used as phosphate donor and polyGluTyr-(4:1) peptide as acceptor. With the exception of protein kinase C-α, cyclin-dependent kinase 1/cycB and protein kinase A are protamine sulfate (200 μg/mL), histone H1 (100 μg/mL), and the heptapeptide Leu-Arg-Arg-Ala-Ser-Leu-Gly (known as Kemptide Bachem) respectively and are used as peptide substrates. Assays are optimized for each kinase using the following ATP concentrations: 1.0 μM (c-Kit, c-Met, c-Fms, c-Raf-1, and RET), 2.0 μM (EGFR, erbB2, ErbB3, and ErbB4), 5.0 μM (c-abl), 8.0 μM (Flt-1, Flt-3, Flt-4, Flk, KDR, FGFR-1, and Tek), 10.0 μM (PDGFR-β, protein kinase C-α, and cyclin-dependent kinase 1), and 20.0 μM (c-Src and protein kinase A). The reaction is terminated by the addition of 20 μL 125 mM EDTA. Thirty μL (c-abl, c-Src, insulin-like growth factor-1R, RET-Men2A, and RET-Men2B) or 40 μL (all other kinases) of the reaction mixture is transferred onto Immobilon-polyvinylidene difluoride membrane, presoaked with 0.5% H3PO4 and mounted on a vacuum manifold. Vacuum is then applied and each well rinsed with 200 μL 0.5% H3PO4. Membranes are removed and washed four times with 1.0% H3PO4 and once with ethanol. Dried membranes are counted after mounting in a Packard TopCount 96-well frame and with the addition of 10 μL/well of Microscint. IC50 values (±SE) are calculated by linear regression analysis of the percentage inhibition and are averages of at least three determinations. |
别名 | 2'-deoxy-2'-fluoro-2'-C-methyluridine, RO 2433, GS-331007 |
分子量 | 260.22 |
分子式 | C10H13FN2O5 |
CAS No. | 863329-66-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (230.57 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.8429 mL | 19.2145 mL | 38.429 mL | 96.0726 mL |
5 mM | 0.7686 mL | 3.8429 mL | 7.6858 mL | 19.2145 mL | |
10 mM | 0.3843 mL | 1.9215 mL | 3.8429 mL | 9.6073 mL | |
20 mM | 0.1921 mL | 0.9607 mL | 1.9215 mL | 4.8036 mL | |
50 mM | 0.0769 mL | 0.3843 mL | 0.7686 mL | 1.9215 mL | |
100 mM | 0.0384 mL | 0.1921 mL | 0.3843 mL | 0.9607 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。
PSI-6206 863329-66-2 Microbiology/Virology Proteases/Proteasome HCV Protease Inhibitor Hepatitis C virus PSI 6206 RO-2433 inhibit RO2433 PSI6206 GS 331007 HCV 2'-deoxy-2'-fluoro-2'-C-methyluridine GS331007 RO 2433 GS-331007 inhibitor