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GS-621763

Chemical Structure : GS-621763

CAS No.: 2647442-13-3

GS-621763 (GS621763)

Catalog No.: PC-38459Not For Human Use, Lab Use Only.

GS-621763 is an oral prodrug of remdesivir parent nucleoside GS-441524, inhibits SARS-CoV-2, including variants of concern in cell culture (EC50=0.11 to 0.73 uM) and human airway epithelium organoids.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GS-621763 is an oral prodrug of remdesivir parent nucleoside GS-441524, inhibits SARS-CoV-2, including variants of concern in cell culture (EC50=0.11 to 0.73 uM) and human airway epithelium organoids.
Oral GS-621763 is efficiently converted to plasma metabolite GS-441524, and in lungs to the triphosphate metabolite identical to that generated by remdesivir, demonstrating a consistent mechanism of activity.
Twice-daily oral administration of 10 mg/kg GS-621763 reduces SARS-CoV-2 burden to near-undetectable levels in ferrets. GS-621763 blocks virus replication and prevents transmission to untreated contact animals SARS-CoV-2 strain P.1 gamma γ.
GS-621763 administration reduced viral load and lung pathology, improved pulmonary function in COVID-19 mouse model.

Physicochemical Properties

M.Wt 501.540
Formula C24H31N5O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2R,3R,4R,5R)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2-cyano-5-((isobutyryloxy)methyl)tetrahydrofuran-3,4-diyl bis(2-methylpropanoate)

References

1. Cox RM, et al. Nat Commun. 2021 Nov 5;12(1):6415.

2. Schäfer A, et al. Sci Transl Med. 2022 Mar 22:eabm3410.

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