DC Chemicals Limited
China
Product Name: GS-443902
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Purity: 98.0%
Stocking Period: 2 Day
Contact: Tony Cao

1355149-45-9

1355149-45-9 structure

Name: GS-443902
Chemical Name: GS 441524 triphosphate
CAS Number: 1355149-45-9
Molecular Formula: C₁₂H₁₆N₅O₁₃P₃
Molecular Weight: 531.202
Catalog: Signaling Pathways Anti-infection HCV
Create Date: 2019-04-05 09:41:54
Modify Date: 2024-01-12 16:09:50
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].

Name	GS 441524 triphosphate
Synonyms	((2R,3S,4R,5R)-5-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methyl tetrahydrogen triphosphate GS-441524

Description	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].
Related Catalog	Signaling Pathways >> Anti-infection >> HCV Research Areas >> Infection Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis Signaling Pathways >> Anti-infection >> RSV
Target	IC50: 5.6 µM (TP RdRp), 1.1 µM (RSV RdRp) and 5 µM (HCV RdRp)[1][2]
In Vitro	GS-443902 (compound 8a), a triphosphates (TP) derivative, is a potent inhibitory activity against the enzyme TP RdRp (IC50=5.6 µM)[1]. In a continuous 72 h incubation of 1 µM GS-5734, the GS-443902 (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[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].
In Vivo	GS-5734 (10 mg kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 (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[3].
References	[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.

Density	2.4±0.1 g/cm3
Molecular Formula	C₁₂H₁₆N₅O₁₃P₃
Molecular Weight	531.202
Exact Mass	530.995728
LogP	-5.92
Index of Refraction	1.841
Storage condition	-20°C

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