Formulation: A solid
Formal Name: (1R,2S,5S)-N-[(1S)-1-cyano-2-[(3S)-2-oxo-3-pyrrolidinyl]ethyl]-3-[(2S)-3,3-dimethyl-1-oxo-2-[(2,2,2-trifluoroacetyl)amino]butyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
Purity: ≥95%
Formula Markup: C23H32F3N5O4
Formula Weight: 499,5
Shelf life (days): 1460
CAS Number: 2628280-40-8
Notes: PF-07321332 is an orally bioavailable inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), also known as 3C-like protease (3CLpro), with a Ki value of 3.11 nM.{62563} It also inhibits Mpro from other members of the Betacoronavirus genus, including SARS-CoV-1, HKU1-CoV, OC43-CoV, and MERS-CoV (Kis = 4.94, 189, 36.4, and 187 nM, respectively), as well as Mpro from NL-63-CoV and 229E CoV (Kis = 226 and 44.4 nM, respectively), which are members of the Alphacoronavirus genus. PF-07321332 is selective for these enzymes over several other proteases, including human and HIV-1 proteases (IC50s = >100 µM for all), as well as a panel of G protein-coupled receptors, kinases, and transporters (IC50s = ≥100 µM for all). It inhibits SARS-CoV-2 replication in A549 cells (EC50 = 77.9 nM) and reduces the cytopathic effect of SARS-CoV-2 in infected Vero E6 cells (EC50 = 74.5 nM) with a 50% cytotoxic concentration (CC50) value of greater than 100 µM. PF-07321332 (300 and 1,000 mg/kg) reduces lung viral titers and the severity of pulmonary lesions in mice infected with the mouse-adapted SARS-CoV-2 MA10 variant. Formulations containing PF-07321332 have been used in the treatment of COVID-19.
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