Biological Activity
S-217622 is the first oral non-covalent, non-peptidic SARS-CoV-2 3CL protease inhibitor with IC50 of 0.096 μM. S-217622 displays antiviral activity in vitro towards a range of SARS-CoV-2 variants and coronavirus families, favorable drug metabolism and pharmacokinetic (DMPK) profiles.
In Vitro
In a cytopathic effect (cpe)-inhibition assay of SARS-CoV-2 infected VeroE6/TMPRSS2 cells, Ensitrelvir 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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ensitrelvir dose-dependently inhibits intrapulmonary replication of SARS-CoV-2 in mice[2].
References & source
[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-Covale
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.