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PSI-7409 tetrasodium  ≥95%

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包装规格：1mg in glass bottle
产品描述：基本信息 产品编号：P10623 产品名称：PSI-7409 tetrasodium CAS: 1621884-22-7   储存条件 粉末 -20℃ 四年 分子式： C10H12FN2Na4O14P3 溶于液体 -80℃ 两年 分子量 588.09 -20℃ i个月 化学名：  [[[(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl]   Solubility (25°C)   体外 DMSO   Ethanol   Water ≥125mg/mL (212.55mM) 体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.7004mL 8.5021mL 17.0042mL 5mM 0.3401mL 1.7004mL 3.4008mL 10mM 0.1700mL 0.8502mL 1.7004mL   生物活性 产品描述 一种 sofosbuvir (PSI-7977) 的 5'-三磷酸活性代谢物，能够抑制 HCV NS5B polymerases，对 GT 1b_Con1，GT 2a_JFH1，GT 3a和 GT 4a NS5B 聚合酶的 IC50 值分别为 1.6，2.8，0.7 和 2.6μM。 靶点/IC50 GT 1b_Con1 IC50: 1.6μM GT 2a_JFH1 2.8μM GT 3a 0.7μM GT 4a 2.6μM   体外研究 PSI-7409 tetrasodium is an active 5'-triphosphate metabolite, inhibiting HCV NS5B polymerases, with IC50s of 1.6, 2.8, 0.7 and 2.6μM for GT 1b_Con1, GT 2a_JFH1, GT 3a, and GT 4a NS5B polymerases, respectively. PSI-7409 also weakly inhibits human DNA polymerase α, with an IC50 of 550μM, but shows no inhibition on DNA Pol β and γ. In clone A cells, the levels of PSI-7409 gradually increases to a maximum concentration of about 25μM over a period of 48 h. PSI-7409 forms at a much faster rate in primary human hepatocytes, achieving a maximum intracellular concentration of -100μM at 4 h and remains at that concentration for 48h.   推荐实验方法(仅供参考) 激酶实验：   Kinase Assay Human DNA polymerase α, β, or γ is assayed in a 10-μL reaction mixture containing 50mM Tris (pH 7.5), 50mM NaCl, 3mU/μL activated calf thymus DNA, a 20μM concentration of all four natural deoxynucleoside triphosphates, 4μCi [α-32P]dCTP, 5mM MgCl2, and increasing concentrations of PSI-7409 (up to 1mM), D-ddFCTP, or aphidicolin. DNA polymerase α, β, or γ is added to the reaction mixture to give final concentrations of 20, 18, and, 50μg/mL, respectively. All reactions are run at 37°C and quenched at 30 min by mixing with 1 μL of 0.5 M EDTA. The radiolabeled products are quantified. A nonlinear fit is performed to determine the IC50. The activity of RNA polymerase II is determined in a 25-μL in vitro transcription reaction mixture containing 100ng of cytomegalovirus (CMV) immediate-early promoter DNA, 400μM ATP, CTP, and UTP, 16μM GTP,10μCi [α-32P]GTP, 3mM MgCl2, and various concentrations of PSI-7409 (up to 1mM), 3'-dCTP, or α-amanitin in transcription buffer (20mM HEPES [pH 7.9], 100mM KCl, 0.2mM EDTA, 0.5mM DTT, and 20% glycerol). All reactions are run at 30°C and quenched at 60 min by mixing with 125μL of stop solution (0.3 M Tris-HCl [pH 7.4], 0.3 M sodium acetate, 0.5% SDS, 2mM EDTA, and 3μg/mL tRNA). The RNA product is purified. The resulting samples contains 12μL and the same volume of gel loading dye (98% formamide, 10mM EDTA, 0.1% xylene cyanol, and 0.1% bromophenol blue) is added. The samples are heated at 90°C for 5 min and loaded onto a 6% polyacrylamide sequencing gel. After running, the gel is exposed to a phosphorscreen, and the product is visualized and quantified by using a phosphorimager.
保存条件：-20℃

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