Ensitrelvir fumarate

Names

[ Name ]:
Ensitrelvir fumarate

[Synonym ]:
S-217622

Biological Activity

[Description]:

Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM)[1][2].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> SARS-CoV

[In Vitro]

In a cytopathic effect (cpe)-inhibition assay of SARS-CoV-2 infected VeroE6/TMPRSS2 cells, Ensitrelvir fumarate shows the EC50 values are approximately 0.4 μM for both wild-type virus and Alpha, Beta, Gamma and Delta variants. EC50 values for SARS-CoV and MERS-CoV were 0.21 and 1.4 μM respectively[1].

[In Vivo]

Ensitrelvir fumarate dose-dependently inhibits intrapulmonary replication of SARS-CoV-2 in mice[2].

[References]

[1]. McKimm-Breschkin JL, et al. COVID-19, Influenza and RSV: Surveillance-informed prevention and treatment - Meeting report from an isirv-WHO virtual conference. Antiviral Res. 2022;197:105227.

[2]. Yuto Unoh, et al. Discovery of S-217622, a Non-Covalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19. bioRxiv 2022.01.26.477782.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₆H₂₁ClF₃N₉O₆

[ Molecular Weight ]:
647.95

Ensitrelvir fumarate

Names

Biological Activity

Chemical & Physical Properties

Related Compounds