GS-621763

GS-621763 is an orally bioavailable prodrug form of the antiviral nucleotide analog GS-443902, which is also an active metabolite of remdesivir (Cay-30354). Upon intestinal absorption, GS-621763 is metabolized into the intermediate metabolite GS-441524 (Cay-30469), which is then further metabolized to the active nucleotide triphosphate GS-443902 in cells where it induces RNA chain termination and inhibits viral polymerases. It reduces the cytopathic effect of respiratory syncytial virus (RSV) in infected HEp-2 cells (EC50 = 0.26 µM), as well as reduces viral titers in Vero E6 cells infected with various clinical isolates of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2, EC50s = 0.11-0.73 µM). GS-621763 (10 mg/kg) inhibits viral transmission in ferrets infected with the SARS-CoV-2 variant of concern (VOC) P.1, also known as the gamma variant.Formal Name: 6-((1E,3Z,6Z,9Z)-pentadeca-1,3,6,9-tetraen-1-yl)tetrahydro-2H-pyran-2-one. CAS Number: 2563617-99-0. Synonyms: GS-441524 tris-isobutyryl ester. Molecular Formula: C24H31N5O7. Formula Weight: 501.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml. lambdamax: 246 nm. SMILES: O=C(C(C)C)OC[C@@H]1[C@@H](OC(C(C)C)=O)[C@@H](OC(C(C)C)=O)[C@@](C#N)(C2=CC=C3N2N=CN=C3N)O1. InChi Key: RVSSLHFYCSUAHY-VEBYGKHWSA-N.