Name | PSI-7409 |
Synonyms | PSI7409 PSI 7409 PSI-7409 Uridine 5'-(tetrahydrogen triphosphate), 2'-deoxy-2'-fluoro-2'-methyl-, (2'R)- (2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate |
CAS | 1015073-42-3 |
Molecular Formula | C10H16FN2O14P3 |
Molar Mass | 500.16 |
Solubility | DMSO |
Storage Condition | -20℃ |
In vitro study | PSI-7409 inhibits the enzymatic activities of these NS5BΔ21 polymerases in a dose-dependent manner. The IC 50 s 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 (IC 50 =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%. 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. |
biological activity | PSI-7409 is the 5 '-triphosphate active metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active inhibitor of HCV nucleotide analogs. |