PSI-7409

PSI-7409是 Sofosbuvir (PSI-7977) 的5'-三磷酸活性代谢物。Sofosbuvir (PSI-7977) 是选择性和高活性的 HCV 核苷酸类似物抑制剂。

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库存: 现货

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1mg

￥2825.00

2260.00

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5mg

￥8412.00

6730.00

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10mg

￥0.00

0.00

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50mg

￥0.00

0.00

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货号: ajce58304
CAS: 1015073-42-3
别名:
分子式: C10H16FN2O14P3
分子量: 500.16
纯度: >98%
溶解度: Water: 50 mg/mL (99.97 mM); DMF: < 1 mg/mL (insoluble); DMSO: < 1 mg/mL (insoluble or slightly soluble)
储存: Store at -20°C
库存: 现货

Background

PSI-7409 is the active 5'-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV.

PSI-7409 inhibits the enzymatic activities of these NS5Bδ21 polymerases in a dose-dependent manner. The IC50s for PSI-7409 against GT 1b, 2a, 3a, and 4a NS5B polymerases are 1.6 μM, 2.8 μM, 0.7 μM, and 2.6 μM, respectively. PSI-7409 is a weak inhibitor of DNA Pol α (IC50=550 μM). DNA Pol β and γ are not inhibited by 1 mM PSI-7409. A significant amount of RNA product is made in the presence of 500 μM PSI-7409, about 85%[1]. In clone A cells, the levels of PSI-7409 gradually increases to a maximum concentration of about 25 μm over a period of 48 h. PSI-7409 forms at a much faster rate in primary human hepatocytes, achieving a maximum intracellular concentration of ～100 μM at 4 h and remains at that concentration for 48 h[2].

[1]. Lam AM, et al. PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. Antimicrob Agents Chemother. 2010 Aug;54(8):3187-96. [2]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.