PSI-7409

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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。

PSI-7409

PSI-7409 Chemical Structure

CAS No. : 1015073-42-3

规格 价格 是否有货 数量
1 mg ¥2600 In-stock
5 mg ¥7800 In-stock
10 mg   询价  
50 mg   询价  

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生物活性

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.

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

500.16

Formula

C10H16FN2O14P3

CAS 号

1015073-42-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 50 mg/mL (99.97 mM; Need ultrasonic)

DMF : < 1 mg/mL (insoluble)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9994 mL 9.9968 mL 19.9936 mL
5 mM 0.3999 mL 1.9994 mL 3.9987 mL
10 mM 0.1999 mL 0.9997 mL 1.9994 mL

*

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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [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.

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