An active metabolite of camostat
FOY-251 is an active metabolite of the antiviral protease inhibitor camostat .1 It inhibits transmembrane serine protease 2 (TMPRSS2; IC50 = 33.3 nM).2 FOY-251 inhibits entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) pseudotyped particles in Calu-3 cells (EC50 = 178 nM) and reduces viral titers in SARS-CoV-2-infected Calu-3 cells when used at concentrations ranging from 1 to 10 ?M.1
1.Hoffmann, M., Hofmann-Winkler, H., Smith, J.C., et al.Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activityEBioMedicine65103255(2021) 2.Shrimp, J.H., Kales, S.C., Sanderson, P.E., et al.An enzymatic TMPRSS2 assay for assessment of clinical candidates and discovery of inhibitors as potential treatment of COVID-19bioRxiv167544(2020)
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