Lufotrelvir

Research use only, not for human use.

Lufotrelvir (PF-07304814) is a small molecule inhibitor of the SARS CoV-2 3CL protease for the treatment of COVID-19 with broad-spectrum anti-SARS activity for the study of novel coronavirus infections.

Lufotrelvir (PF-07304814), a phosphate proagent 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.

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Once administered through intravenous infusion, Lufotrelvir is cleaved into PF-00835231 to exert its anti-viral effects. Lufotrelvir exhibits a favorable cardiovascular safety profile.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.

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Others

Other Targets

SARS-CoV

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2468015-78-1

552.51

C24H33N4O9P

>98% (HPLC)

In Vitro:?DMSO : 130 mg/mL (235.29 mM; Ultrasonic ) H2O : 50 mg/mL (90.50 mM; Ultrasonic)

O(C)C1=C2C(NC(C(N[C@H](C(N[C@@H](C[C@H]3C(=O)NCC3)C(COP(=O)(O)O)=O)=O)CC(C)C)=O)=C2)=CC=C1

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(-20℃)

With Ice Pack

≥ 2 years