2017年11月27日星期一

PSI-7409|cas 1015073-42-3

PSI-7409|cas 1015073-42-3

DC Chemicals, Website: www.dcchemicals.com

Product Name: PSI-7409|Cas Number: 1015073-42-3| Catalog Number: DC10162|Other Nmaes: PSI 7409; PSI7409

PSI-7409 is the active 5′-triphosphate metabolite of PSI-7851. PSI-7851 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].

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