| Bioactivity | Lufotrelvir (PF-07304814), a phosphate prodrug of PF-00835231, acts as a potent 3CLpro protease (Mpro) inhibitor with SARS-CoV-2 antiviral activity. Lufotrelvir binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174nM. Lufotrelvir is promising single antiviral agent and also can be used for the research of combination with other antivirals that target other critical stages of the coronavirus life cycle[1]. | ||||||||||||
| In Vivo | Once administered through intravenous infusion, Lufotrelvir is cleaved into PF-00835231 to exert its anti-viral effects. Lufotrelvir exhibits a favorable cardiovascular safety profile[1].Lufotrelvir is administered intravenously to rats, dogs and monkeys. It exhibits high systemic clearance and short half-life across species forming 68, 81, 76% PF-00835231 in rats, dogs and monkey respectively in comparison to the systemic exposure achieved with IV administration of PF00835231[1]. | ||||||||||||
| Name | Lufotrelvir | ||||||||||||
| CAS | 2468015-78-1 | ||||||||||||
| Formula | C24H33N4O9P | ||||||||||||
| Molar Mass | 552.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Koen Vandyck, et al. Considerations for the discovery and development of 3-chymotrypsin-like cysteine protease inhibitors targeting SARS-CoV-2 infection. Curr Opin Virol. 2021 Apr 27;49:36-40. [2]. Britton Boras, et al. Title: Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19 Short Title: Novel 3CL Protease Inhibitor for COVID-19 |
Lufotrelvir
CAS: 2468015-78-1 F: C24H33N4O9P W: 552.51
Lufotrelvir (PF-07304814), a phosphate prodrug of PF-00835231, acts as a potent 3CLpro protease (Mpro) inhibitor with S
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