PF-00835231

For research use only.

Catalog No.S9731

PF-00835231 Chemical Structure

CAS No. 870153-29-0

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

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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

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]

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 95 mg/mL (201.04 mM)
Water Insoluble
Ethanol ''''95 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 472.53
Formula

C24H32N4O6

CAS No. 870153-29-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID