Bioactivity | Ensitrelvir (S-217622) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM)[1][2]. | ||||||||||||
Invitro | 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]. | ||||||||||||
In Vivo | Ensitrelvir dose-dependently inhibits intrapulmonary replication of SARS-CoV-2 in mice[2]. | ||||||||||||
Name | Ensitrelvir | ||||||||||||
CAS | 2647530-73-0 | ||||||||||||
Formula | C22H17ClF3N9O2 | ||||||||||||
Molar Mass | 531.88 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |