Lufotrelvir (PF-07304814) | SARS-CoV inhibitor | CAS 2468015-78-1

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Quality Control

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

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COA
NMR
SDS
Datasheet

99.93

Related Targets	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV
Other SARS-CoV Inhibitors	Molnupiravir (EIDD-2801) Nirmatrelvir (PF-07321332) EIDD-1931 (NHC) Paquinimod (ABR-215757) Ensitrelvir fumarate Simnotrelvir Ensitrelvir ML188 XP-59 GS-621763

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (180.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 50 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight	552.51	Formula	C₂₄H₃₃N₄O₉P	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2468015-78-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	SARS-CoV-2 3CL^pro 174 nM(Ki)
In vitro	As a phosphate prodrug of PF-00835231, Lufotrelvir (PF-07304814) shows strong antiviral activity by inhibiting coronavirus family 3CL protease activity, with no statistical difference in its antiviral potency in vero cells expressing high levels of the efflux transporter P-glycoprotein.<sup><a class="sref" href="#s_ref">[1]</a></sup>
In vivo	Lufotrelvir (PF-07304814) exhibits high conversion to PF-00835231, systemic clearance and short half-life across species in rats, dogs, and monkey, respectively. It also shows unbound CL_int values of 51, 84, 168 and 428 µL/min/mg in rat, dog, monkey and human respectively.
References	[1] https://pubmed.ncbi.nlm.nih.gov/34663813/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Lufotrelvir (PF-07304814) SARS-CoV inhibitor

Chemical Structure

Molecular Weight: 552.51