GS-443902 (GS-441524 triphosphate) is a potent viralRNA-dependent RNA-polymerases (RdRp)inhibitor withIC₅₀s of 1.1 μM, 5 μM forRSVRdRp andHCVRdRp, respectively. GS-443902 is the active triphosphate metabolite of Remdesivir^[1][2].

IC50: 1.1 μM (RSV RdRp) and 5 μM (HCV RdRp)^[1][2]

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 C_maxof 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively^[1].
GS-443902 (compound 8a) is a triphosphates (TP) derivative^[2].
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^[3].

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 t_1/2of 14 h and levels required for >50% virus inhibition for 24 hours^[3].

531.20

Solid

C₁₂H₁₆N₅O₁₃P₃

1355149-45-9

瑞德西韦代谢物

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

H₂O : 100 mg/mL(188.25 mM;Need ultrasonic)

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