Nirmatrelvir (PF-07321332)

Catalog No.S9866 Batch:S986602

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Technical Data

Formula

C23H32F3N5O4

Molecular Weight 499.53 CAS No. 2628280-40-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (200.18 mM)
Ethanol 100 mg/mL (200.18 mM)
Water 2 mg/mL (4.0 mM)
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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
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>

Protocol (from reference)

Kinase Assay:

[1]

  • 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 Assay:

[2]

  • 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

Animal Study:

[3]

  • Animal Models

    Female C57BL/6 Cg-Tg2Prlmn/J mice 

  • Dosages

    20 mg/kg

  • Administration

    Oral

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

Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int J Mol Sci, 2023, 24(7)6062] PubMed: 37047038
Immunodetection assays for the quantification of seasonal common cold coronaviruses OC43, NL63, or 229E infection confirm nirmatrelvir as broad coronavirus inhibitor [ Antiviral Res, 2022, 203:105343] PubMed: 35598779
Autoprocessing and oxyanion loop reorganization upon GC373 and nirmatrelvir binding of monomeric SARS-CoV-2 main protease catalytic domain [ Commun Biol, 2022, 5(1):976] PubMed: 36114420
The MEK1/2 Inhibitor ATR-002 (Zapnometinib) Synergistically Potentiates the Antiviral Effect of Direct-Acting Anti-SARS-CoV-2 Drugs [ Pharmaceutics, 2022, 14(9)1776] PubMed: 36145524
Use of Human Lung Tissue Models for Screening of Drugs against SARS-CoV-2 Infection [ Viruses, 2022, 14(11)2417] PubMed: 36366514
PF-07321332 (Nirmatrelvir) Does Not Interact with Human ENT1 or ENT2: Implications for COVID-19 Patients [ Clin Transl Sci, 2022, 10.1111/cts.13292] PubMed: 35505633
Virologic and Immunologic Characterization of COVID-19 Recrudescence after Nirmatrelvir/Ritonavir Treatment [ Res Sq, 2022, rs.3.rs-1662783] PubMed: 35611335

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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