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GS-443902 trisodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GS-443902 trisodium图片
CAS NO:1355050-21-3
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议

产品名称
瑞德西韦代谢物三钠盐
GS-441524triphosphatetrisodium
Remdesivirmetabolitetrisodium
产品介绍

产品描述

GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC 50 s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734).

体外活性

In a continuous 72 h incubation of 1 μM Remdesivir (GS-5734), the GS-443902 trisodium (GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium) level is measured at 2, 24, 48 and 72 h, and reaches a C max of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively[1]. GS-443902 trisodium (compound 8a) is a triphosphates (TP) derivative[2]. GS-443902 trisodium (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 sodium[3].

体内活性

Remdesivir (GS-5734; 10?mg?kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 trisodium (Remdesivir metabolite trisodium; NTP) is apparent within 2?h of dose administration in rhesus monkeys. In PBMCs, GS-443902 trisodium represents the predominant metabolite and is persistent with a t 1/2 of 14?h and levels required for >50% virus inhibition for 24?hours[3].

Cas No.

1355050-21-3

别名

瑞德西韦代谢物三钠盐;GS-441524triphosphatetrisodium;Remdesivirmetabolitetrisodium

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years