Home Microbiology SARS-CoV inhibitor - COVID-19 inhibitor Nirmatrelvir (PF-07321332) For research use only.

Nirmatrelvir (PF-07321332)

Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme.

Nirmatrelvir (PF-07321332) Chemical Structure

Nirmatrelvir (PF-07321332) Chemical Structure

CAS: 2628280-40-8

Selleck's Nirmatrelvir (PF-07321332) has been cited by 7 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

Description

Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme.
Targets
SARS-CoV-2 Mpro [1]
3.11 nM(ki)
In vitro
In vitro
Nirmatrelvir (PF-07321332) is a reversible covalent inhibitor of SARS-CoV-2 main protease (M<sup>pro</sup>, also known as 3CL protease), and ki is 3.11 nM. 
PF- 07321332 directly binds to the catalytic cysteine (Cys145) residue of the enzyme.<sup><a class="sref" href="#s_ref">[1]</a></sup>
Kinase Assay Enzyme kinetics assay
Test compounds and SARS-CoV-2 Mpro enzyme were incubated at a 1:1 molar ratio of 2 μM compound and 2 μM enzyme in assay buffer for 20 minutes. The mixture was then diluted 50-fold into assay buffer followed by a transfer of 5 μl to wells of a black low volume 384-well assay plate. Enzyme activity was monitored on a BMG Pherastar at Ex/Em of 340 nm/460 nm after addition of 5 μl 60 μM peptide substrate. Final reaction conditions were 20 nM enzyme with 20 nM compound and 30 μM peptide substrate.
Cell Research Cell lines HCoV-229E in Huh-7 cells
Concentrations 0.62 µM
Incubation Time 2 days
Method

hCoV-229E experiments were performed on Huh-7 cells at an MOI of 0.002 and infection determined by in-cell ELISA 2 days later
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05487040 Terminated COVID-19 Pfizer September 7 2022 Phase 1
NCT05339334 Completed Healthy Participants Pfizer March 10 2022 Phase 1
NCT05263921 Completed Bioavailability Pfizer March 10 2022 Phase 1
NCT05129475 Completed Healthy Participants Pfizer November 12 2021 Phase 1

Chemical lnformation & Solubility

Molecular Weight 499.53 Formula

C23H32F3N5O4
CAS No. 2628280-40-8 SDF --
Smiles CC(C)(C)C(NC(=O)C(F)(F)F)C(=O)N1CC2C(C1C(=O)NC(CC3CCNC3=O)C#N)C2(C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (200.18 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : 2 mg/mL


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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. )

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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.

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