GS-443902 是一种有效的病毒 RNA 依赖的 RNA 聚合酶 (RdRp) 抑制剂，对 TP RdRp，RSV RdRp 和 HCV RdRp 的 IC50 分别为 5.6 µM，1.1 µM 和 5 µM。GS-443902 是 Remdesivir 的活性三磷酸盐代谢产物。
GS-443902 (Remdesivir metabolite) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 5.6 µM, 1.1 µM, 5 µM for TP RdRp, RSV RdRp and HCV RdRp, respectively. GS-443902 is the active triphosphate metabolite of Remdesivir[1][2].
[1]. Siegel D, et al. Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses. Med Chem. 2017 Mar 9;60(5):1648-1661. [2]. Cho A, et al. Synthesis and antiviral activity of a series of 1’-substituted 4-aza-7,9-dideazaadenosine C-nucleosides. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2705-7. [3]. Warren TK, et al. Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature. 2016 Mar 17;531(7594):381-5.
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