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Lufotrelvir (PF-07304814)

Catalog No.S9858 Purity: 99.93%

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

Lufotrelvir (PF-07304814) Chemical Structure

CAS: 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

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Biological Activity

Description

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

Targets

SARS-CoV-2 3CL^pro ^[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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References
[1] Britton Boras, et al. Nat Commun . 2021 Oct 18;12(1):6055.

References

[1] Britton Boras, et al. Nat Commun . 2021 Oct 18;12(1):6055.

Chemical lnformation & 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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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
Batch:

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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