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PSI-6130  ≥98%

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包装规格：5mg in glass bottle
溶解性：溶于DMSO（≥ 50 mg/mL)
产品描述：基本信息 产品编号：P10624 产品名称：PSI-6130 CAS: 817204-33-4   储存条件 粉末 -20℃ 四年     分子式： C10H14FN3O4 溶于液体 -80℃ 两年 分子量 259.23 -20℃ 一个月 化学名：  4-Amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyltetrahydrofuran-2-yl)pyrimidin-2(1H)-one   Solubility (25°C)   体外 DMSO ≥50mg/mL (192.88mM) Ethanol   Water   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 3.8576mL 19.2879mL 38.5758mL 5mM 0.7715mL 3.8576mL 7.7152mL 10mM 0.3858mL 1.9288mL 3.8576mL   生物活性 产品描述 高效的，有选择性的 HCV NS5B polymerase 抑制剂，能够抑制HCV复制，IC50 值为 0.6μM。 靶点/IC50 HCV replication IC50: 0.6μM   体外研究 PSI-6130 exhibits potent and specific inhibitory activity against HCV RNA replication mediated by the NS5B polymerase.Both PSI-6130 inhibit HCV GT-1b (Con1 strain) and GT-1a (H77 strain) subgenomic RNA replication, with mean EC50 values of 0.51 and 0.30μM, respectively. PSI-6130 inhibits 40% human serum with EC50 of 0.51μM. PSI-6130 inhibits HCV replication with a mean IC50 of 0.6μM, PSI-6130-TP inhibits HCV replicase with a mean IC50 of 0.34μM. PSI-6130-TP inhibits recombinant HCV Con1 NS5B on a heteropolymeric RNA template derived from the 3′-end of the negative strand of the HCV genome with an IC50 of 0.13μM and Ki of 0.023μM.   推荐实验方法(仅供参考) 激酶实验： Kinase Assay The inhibition potency of compounds with respect to the RdRp activity of recombinant NS5B570-BK, NS5B570-Con1, and NS5B570-H77 proteins is determined by measuring the incorporation of radiolabeled NMP into acid-insoluble RNA products by use of a complement strand of internal ribosomal entry site (cIRES) RNA template. Briefly, 50% inhibitory concentration(IC50) determinations are carried out using 200nM in vitro-transcribed cIRES RNA template, 1μCi of tritiated UTP (42Ci/mmol), 500μM ATP, 500μM GTP, 1μM CTP, 1× TMDN buffer (40mM Tris-HCl [pH 8.0], 4mM MgCl2, 4mM dithiothreitol, 40mM NaCl), and 200nM enzyme. The inhibition potency of compounds with respect to the RdRp activity of NS5B570-S282TCon1 is determined under GT-1b assay conditions as. NS5B570-BK and NS5B570-Con1 enzymes are used as controls. The final reaction volume is 50μL under all assay conditions. All reactions contain a final 10% dimethyl sulfoxide. Km and Ki values are measured.
保存条件：-20℃

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