Home Microbiology COVID-19 inhibitor - SARS-CoV inhibitor PF-00835231 For research use only.

PF-00835231

PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19.

PF-00835231 Chemical Structure

PF-00835231 Chemical Structure

CAS: 870153-29-0

Selleck's PF-00835231 has been cited by 4 publications

Purity & Quality Control

Batch: S973101 DMSO] 95 mg/mL] false] Ethanol] 95 mg/mL] false] Water] Insoluble] false Purity: 99.08%
99.08

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Biological Activity

Description PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19.
Targets
3CLpro [1]
In vitro
In vitro

A time-of-drug-addition approach delineates the timing of early SARS-CoV-2 life cycle steps in A549+ACE2 cells and validates PF-00835231's early time of action. In a model of the human polarized airway epithelium, PF-00835231 potently inhibits SARS-CoV-2 at low micromolar concentrations. PF-00835231 exhibits the potential as an effective SARS-CoV-2 antiviral.[1]
Cell Research Cell lines A549 cells, human airway epithelial cultures (HAEC)
Concentrations 1 nM-10 μM
Incubation Time 0-4 h
Method

A549+ACE2 cells are seeded into black wall 96-well plates at 70% confluency. The next day, media is removed and replaced with complete media containing compound (PF-00835231)/carrier two hours prior to infection. Cells are then infected at 0.425 multiplicity of infection (MOI), based on Vero E6 titer, at 37°C. 1 hour post virus addition, virus is removed, and media containing compound/carrier is added. At 24 and 48 hours post infection, cells are fixed by submerging in 10% formalin solution for 30-45 min. After fixation, cells are washed once with H2O to remove excess formalin.
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 lnformation & Solubility

Molecular Weight 472.53 Formula

C24H32N4O6
CAS No. 870153-29-0 SDF --
Smiles COC1=CC=CC2=C1C=C([NH]2)C(=O)NC(CC(C)C)C(=O)NC(CC3CCNC3=O)C(=O)CO
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 95 mg/mL ( (201.04 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble


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In vivo
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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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