产品
编 号：F135701
分子式：C12H16N5O13P3
分子量：531.2
分子式：C12H16N5O13P3
分子量：531.2
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CAS No: 1355149-45-9
产品详情
生物活性：
GS-443902 (GS-441524 triphosphate) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 is the active triphosphate metabolite of Remdesivir.
体内研究：
Remdesivir (GS-5734; 10?mg?kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 (GS-441524 triphosphate; Remdesivir metabolite; NTP) is apparent within 2?h of dose administration in rhesus monkeys. In PBMCs, GS-443902 represents the predominant metabolite and is persistent with a t1/2 of 14?h and levels required for >50% virus inhibition for 24?hours.
体外研究：
In a continuous 72 h incubation of 1 μM Remdesivir (GS-5734), the GS-443902 (GS-441524 triphosphate; Remdesivir metabolite; compound 4tp) level is measured at 2, 24, 48 and 72 h, and reaches a Cmax of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively. GS-443902 (compound 8a) is a triphosphates (TP) derivative. GS-443902 (NTP; 0.01, 0.1, 1, 10, 100 μM) inhibits RSV RdRp-catalysed RNA synthesis by incorporating into the nascent viral RNA transcript and causing its premature termination. GS-5734 selectively inhibits EBOV replication by targeting its RdRp and inhibiting viral RNA synthesis following efficient intracellular conversion to GS-443902.
GS-443902 (GS-441524 triphosphate) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 is the active triphosphate metabolite of Remdesivir.
体内研究：
Remdesivir (GS-5734; 10?mg?kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 (GS-441524 triphosphate; Remdesivir metabolite; NTP) is apparent within 2?h of dose administration in rhesus monkeys. In PBMCs, GS-443902 represents the predominant metabolite and is persistent with a t1/2 of 14?h and levels required for >50% virus inhibition for 24?hours.
体外研究：
In a continuous 72 h incubation of 1 μM Remdesivir (GS-5734), the GS-443902 (GS-441524 triphosphate; Remdesivir metabolite; compound 4tp) level is measured at 2, 24, 48 and 72 h, and reaches a Cmax of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively. GS-443902 (compound 8a) is a triphosphates (TP) derivative. GS-443902 (NTP; 0.01, 0.1, 1, 10, 100 μM) inhibits RSV RdRp-catalysed RNA synthesis by incorporating into the nascent viral RNA transcript and causing its premature termination. GS-5734 selectively inhibits EBOV replication by targeting its RdRp and inhibiting viral RNA synthesis following efficient intracellular conversion to GS-443902.
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