Synonyms: 1-O-Octadecyl-2-O-benzyl-sn-glyceryl-3-phospho-GS-441524 | compound 5c [PMID: 34310217] | example 67 [WO2022081973A1] | ODBG-P-RVn
Compound class:
Synthetic organic
Comment: V2043 is an orally bioavailable phospholipid analogue of remdesivir nucleoside (RVn; GS-441524) [1,3]. It is a prodrug that is metabolised first to RVn monophosphate (by sphingomyelin phosphodiesterase I), and then to the active metabolite RVn triphosphate. Mechanistically, RVn triphosphate inhibits the viral RNA-dependent RNA polymerase (RdRP). Antiviral activity against SARS-CoV-2 has been demonstrated in vitro and in a mouse model of SARS-CoV-2 infection. Structural modifications of V2043 have been reported to improve its antiviral activity [1].
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Bioactivity Comments |
In vitro antiviral activity against several SARS-CoV-2 variants has been demonstrated: B.1.1.7 (Alpha; EC50 146 nM), B.1.351 (Beta; EC50 146 nM), P.1 (Gamma; EC50 167 nM), B.1.617.2 (Delta; EC50 85 nM), BA.1 (Omicron; EC50 44 nM) [1]. Evidence of anti-RSV activity was contained in Gilead Sciences' patent WO2022081973A1 [2]. As a prodrug, target potency will be associated with the active metabolite RVn triphosphate. |
Selectivity at other protein targets | ||||||||||||||||||||||||||||||||||
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