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GS-443902 trisodium

Catalog No. T38761 CAS 1355050-21-3

Synonyms: GS-441524triphosphatetrisodium, Remdesivirmetabolitetrisodium

GS-443902 trisodium (GS-441524 triphosphate trisodium), the active triphosphate metabolite of Remdesivir (GS-5734), serves as a potent inhibitor of viral RNA-dependent RNA-polymerases (RdRp), displaying inhibitory concentrations (IC50) of 1.1 μM and 5 μM for RSV RdRp and HCV RdRp, respectively.

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GS-443902 trisodium, CAS 1355050-21-3

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Description	GS-443902 trisodium (GS-441524 triphosphate trisodium), the active triphosphate metabolite of Remdesivir (GS-5734), serves as a potent inhibitor of viral RNA-dependent RNA-polymerases (RdRp), displaying inhibitory concentrations (IC50) of 1.1 μM and 5 μM for RSV RdRp and HCV RdRp, respectively.
Targets&IC50	HCV RdRp:5 µM (IC50), RSV RdRp:1.1 µM (IC50)
In vitro	During a 72-hour incubation with 1 μM Remdesivir (GS-5734), levels of its metabolite, GS-443902 trisodium (GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium), were monitored at intervals of 2, 24, 48, and 72 hours, showing peak concentrations (C max) of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cell lines, respectively[1]. GS-443902 trisodium (compound 8a), a triphosphate (TP) derivative[2], impairs RSV RdRp-catalyzed RNA synthesis through integration into the nascent viral RNA, resulting in its premature termination. It is effectively transformed within cells to GS-443902 sodium, which selectively disrupts Ebola virus (EBOV) replication by targeting and inhibiting the viral RNA-dependent RNA polymerase (RdRp), thus blocking viral RNA synthesis[3].
In vivo	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].

Synonyms	GS-441524triphosphatetrisodium, Remdesivirmetabolitetrisodium
Molecular Weight	N/A
CAS No.	1355050-21-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 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. 3. 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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GS-443902 trisodium 1355050-21-3 GS-441524triphosphatetrisodium Remdesivirmetabolitetrisodium GS 443902 GS-443902 GS 443902 trisodium GS443902 trisodium GS443902 inhibitor inhibit

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