Home Microbiology SARS-CoV inhibitor - COVID-19 inhibitor Lufotrelvir (PF-07304814) For research use only.

Lufotrelvir (PF-07304814)

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

Lufotrelvir (PF-07304814) Chemical Structure

CAS No. 2468015-78-1

Purity & Quality Control

Batch: S985801 DMSO]100 mg/mL]false]Water]50 mg/mL]false]Ethanol]Insoluble]false Purity: 99.93%
99.93

Lufotrelvir (PF-07304814) Related Products

Biological Activity

Description

PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174 nM.
Targets
SARS-CoV-2 3CLpro [1]
174 nM(Ki)
In vitro
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>
Cell Research 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.
In Vivo
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>
Animal Research Animal Models Rat, dog, monkey and human
Dosages 1.17 mg/kg for animals, 500 mg/day for human
Administration i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05050682 Completed
Healthy
Pfizer
 October 7 2021 Phase 1
NCT04627532 Completed
Healthy
Pfizer
 October 23 2020 Phase 1
NCT04535167 Completed
Viral Disease
Pfizer
 September 9 2020 Phase 1

Chemical Information & Solubility

Molecular Weight 552.51 Formula

C24H33N4O9P
CAS No. 2468015-78-1 SDF --
Smiles COC1=CC=CC2=C1C=C([NH]2)C(=O)NC(CC(C)C)C(=O)NC(CC3CCNC3=O)C(=O)CO[P](O)(O)=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (180.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 50 mg/mL

Ethanol : Insoluble


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In vivo
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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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