PF-07304814 is a non-cytotoxic, aqueous soluble phosphate ester prodrug of the potent and selective corona virus inhibitor PF-00835231 (pro-/active drug SARS CoV-2 Ki = 174/0.27 nM). PF-07304814 is rapidly converted to PF-00835231, exhibiting anti-viral efficacy in cultures (PF-07304814/PF-00835231 IC50 with 2 μM P-pg efflux inhibitor CP-100356 = 3.8/0.24 μM (SARS2 Washington 1 & Vero E6-enACE2), 830/760 nM (SARS2 BetaCov GHB-03021/2020 & Vero E6-EGFP); PF-07304814/PF-00835231 IC50 with 0.5 μM CP-100356 = 58/80 nM (HCoV-229E & MRC-5)) without affecting P450 enzymes (>100 μM) or a range of transporters (>130 μM).
bioRxiv : the preprint server for biology (2020-09-17)
COVID-19 caused by the SARS-CoV-2 virus has become a global pandemic. 3CL protease is a virally encoded protein that is essential across a broad spectrum of coronaviruses with no close human analogs. The designed phosphate prodrug PF-07304814 is metabolized to
Questions
Reviews
★★★★★ No rating value
Active Filters
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.