Lufotrelvir (PF-07304814)

Catalog No.S9858

For research use only.

PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174 nM.

Lufotrelvir (PF-07304814) Chemical Structure

CAS No. 2468015-78-1

Purity & Quality Control

Choose Selective SARS-CoV Inhibitors

Biological Activity


PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174 nM.

SARS-CoV-2 3CLpro [1]
174 nM(Ki)
In vitro

Lufotrelvir (PF-07304814) is a phosphate prodrug of PF-00835231, and there is no statistical difference in antiviral potency of Lufotrelvir in vero cells expressing high levels of the efflux transporter P-glycoprotein, showing strong antiviral activity by inhibiting coronavirus family 3CL protease activity.<sup><a class="sref" href="#s_ref">[1]</a></sup>

In vivo

PF-07304814 exhibits high conversion to PF-00835231, systemic clearance and short half-life across species in rats, dogs, and monkey, respectively, also shows unbound CL<sub>int</sub> values of 51, 84, 168 and 428 µL/min/mg in rat, dog, monkey and human respectively. <sup><a class="sref" href="#s_ref">[1]</a></sup>

Protocol (from reference)

Cell Research:

<sup><a class="sref" href="#s_ref">[1]</a></sup>

  • Cell lines: VeroE6-ACE2 (Kideney), VeroE6-egfp (Kidney), A549-ACE2 (Lung) and MRC5 (Lung, h229E virus)
  • Concentrations: 0.01-1000 µM
  • Incubation Time: --
  • Method:

    These cell lines were infected with the SARS-CoV-2 Washington strain 1 (WA1-EPI_ISL_404895) or the Belgium/GHB-03021/2020 strain (GHB-03021-EPI_ISL_407976), respectively, which have identical 3CL<sup>pro</sup> amino acid sequences and conducted with a cytopathic effect (CPE) assay.

Animal Research:

<sup><a class="sref" href="#s_ref">[1]</a></sup>

  • Animal Models: Rat, dog, monkey and human
  • Dosages: 1.17 mg/kg for animals, 500 mg/day for human
  • Administration: i.v.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 552.51


CAS No. 2468015-78-1
Storage 3 years -20°C powder
2 years -80°C in solvent

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05050682 Completed Drug: PF-07304814 Healthy Pfizer October 7 2021 Phase 1
NCT04627532 Completed Drug: PF-07304814|Drug: Placebo Healthy Pfizer October 23 2020 Phase 1
NCT04535167 Completed Drug: PF-07304814|Drug: Placebo Viral Disease Pfizer September 9 2020 Phase 1

(data from, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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