Basic information Safety Supplier Related

GS-441524 sodium

Basic information Safety Supplier Related

GS-441524 sodium Basic information

Product Name:
GS-441524 sodium
Synonyms:
  • GS-441524 sodium
  • GS-443902 trisodium
  • Remdesivir Impurity 11(GS-441524 sodium)
  • GS-441524triphosphatetrisodium
  • Remdesivirmetabolitetrisodium
CAS:
1355050-21-3
MF:
C12H17N5NaO13P3
MW:
555.2
Mol File:
1355050-21-3.mol
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GS-441524 sodium Chemical Properties

form 
Solid
color 
White to light yellow
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GS-441524 sodium Usage And Synthesis

Uses

GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s 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)[1][2].

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 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. DOI:10.1021/acs.jmedchem.6b01594
[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. DOI:10.1038/nature17180
[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. DOI:10.1016/j.bmcl.2012.02.105

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