1. Anti-infection
  2. SARS-CoV
  3. Nirmatrelvir

Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CLPRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research.

For research use only. We do not sell to patients.

CAS No. : 2628280-40-8

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Customer Review

Based on 103 publication(s) in Google Scholar

Other Forms of Nirmatrelvir:

Top Publications Citing Use of Products

103 Publications Citing Use of MCE Nirmatrelvir

Bio/Physico-chemical Assay
In Vivo Efficacy Study
Histological Imaging/Staining
In Vivo Imaging
Cell Proliferation/Viability Assay

    Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 3;16(1):2900.  [Abstract]

    Mice were treated at 6 h, 24 h and 48 h with euthanasia performed at 72 h post-infection. WT 7-9 week-old mice were infected with SARS-CoV-2 P21 and treated with either vehicle, PLT (Paxlovid-like treatment: 56 mg/kg Nirmatrelvir, 19 mg/kg Ritonavir), or WEHI-P8 (100 mg/kg or 150 mg/kg). Three days post-infection, mice were monitored for d viral load and percentage change in body weight compared to initial body weight.

    Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 3;16(1):2900.  [Abstract]

    H&E staining showed that mice in the PLT treatment group (Paxlovid-like treatment: 56 mg/kg Nirmatrelvir, 19 mg/kg Ritonavir) exhibited mild to moderate multifocal inflammation, mainly confined to the peribronchial and perivascular areas of the lungs, with occasional alveolar collapse and mild hemorrhages.

    Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Nature. 2022 Jul;607(7917):119-127.  [Abstract]

    Syrian hamsters were intranasally inoculated with 103 PFU of BA.2 (NCD1288). One day after infection, hamsters were treated with: 500 mg kg−1 molnupiravir, 1,000 mg kg−1 nirmatrelvir or 60 mg kg−1 S-217622 orally twice daily for 3 days. Methylcellulose served as a control for oral treatment. Eight hamsters per group were euthanized at 4 dpi for virus titration. Viral titres in the nasal turbinates and lungs were determined by plaque assay.

    Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Sci Immunol. 2023 Apr 14;8(82):eadf0348.  [Abstract]

    DIO mice were infected with SARS-CoV-2 MA10 virus and treated with vehicle, Nirmatrelvir, or Nirmatrelvir plus MSDC. Host mortality was monitored and survival rate is shown.

    Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Sci Immunol. 2023 Apr 14;8(82):eadf0348.  [Abstract]

    DIO mice were infected with SARS-CoV-2 MA10 virus and treated with vehicle, Nirmatrelvir, or Nirmatrelvir plus MSDC. H&E staining of lung section (n = 5) and quantification of pathological lesions at 21 d.p.i. Scale bar, 200 μm. HM, hyaline membranes.

    Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Vet Sci. 2023 Aug 9;10(8):513.

    The CC50, EC50, and SI for six compounds against FIPV. The half-maximal cytotoxic concentration (CC50) values are from four measurements of diluted drugs using MTT assay, in CRFK cells treated with drugs for 48 h. The half-maximal effective concentration (EC50) values are from six measurements of diluted drugs against FIPV replication in CRFK cells for 48 h. Based on the SI value (mean CC50)/(mean EC50), GS-441524 was found highly selective (SI 165.5) against FIPV among the drugs tested and showed high efficacy (EC50 1.6 µM) against FIPV with a less deleterious effect (CC50 260.0 µM) on the cells. Nirmatrelvir also showed promising efficacy (EC50 2.5 µM) and selectivity (SI 113.7) against FIPV. Ritonavir showed the highest toxicity level in the cells (CC50 39.9).

    Nirmatrelvir purchased from MedChemExpress. Usage Cited in: N Engl J Med. 2023 Jan 5;388(1):89-91.  [Abstract]

    Remdesivir, Molnupiravir, and Nirmatrelvir are efficacious against both BQ.1.1 and XBB in vitro.

    Nirmatrelvir purchased from MedChemExpress. Usage Cited in: N Engl J Med. 2023 Jan 5;388(1):89-91.  [Abstract]

    Representative echocardiographic images (M-mode) from sham, TAC and Tipifarnib (10 mg/kg body weight/three times a week, IP injection) treated TAC mouse heart at 8 weeks.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CLPRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research[1].

    IC50 & Target

    IC50: 3CLPRO[1]

    Cellular Effect
    Cell Line Type Value Description References
    CCRF-CEM CC50
    > 100 μM
    Compound: Nirmatrelvir
    Cytotoxicity against human CEM cells assessed as reduction in cell viability
    Cytotoxicity against human CEM cells assessed as reduction in cell viability
    [PMID: 38432056]
    Caco-2 CC50
    > 100 μM
    Compound: Nirmatrelvir
    Cytotoxicity against human Caco-2 cells assessed as reduction in cell viability
    Cytotoxicity against human Caco-2 cells assessed as reduction in cell viability
    [PMID: 38432056]
    Calu-3 CC50
    > 100 μM
    Compound: Nirmatrelvir
    Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability
    Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability
    [PMID: 38432056]
    Epithelial cell EC50
    25.3 nM
    Compound: PF-07321332
    Antiviral activity against SARS-CoV-2 infected in human Primary bronchial epithelial cell assessed as inhibition of viral growth
    Antiviral activity against SARS-CoV-2 infected in human Primary bronchial epithelial cell assessed as inhibition of viral growth
    [PMID: 38335279]
    HCT-8 CC50
    > 30 μM
    Compound: PF-07321332
    Cytotoxicity against human HCT-8 cells incubated for 120 hrs by Cell-Titer Glo assay
    Cytotoxicity against human HCT-8 cells incubated for 120 hrs by Cell-Titer Glo assay
    [PMID: 38335279]
    HEK-293T CC50
    > 50000 nM
    Compound: PF-07321332
    Cytotoxicity against HEK293T cells transfected with ACE2 and TMPRSS2 assessed as reduction in cell viability
    Cytotoxicity against HEK293T cells transfected with ACE2 and TMPRSS2 assessed as reduction in cell viability
    [PMID: 36229406]
    HeLa CC50
    > 40 μM
    Compound: PF-07321332
    Cytotoxicity against human HeLa cells expressing ACE2 incubated for 120 hrs by Cell-Titer Glo assay
    Cytotoxicity against human HeLa cells expressing ACE2 incubated for 120 hrs by Cell-Titer Glo assay
    [PMID: 38335279]
    Huh-7 CC50
    > 100 μM
    Compound: Nirmatrelvir
    Cytotoxicity against human Huh-7 cells overexpressing human ACE2 assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against human Huh-7 cells overexpressing human ACE2 assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    [PMID: 36549112]
    Huh-7 CC50
    > 100 μM
    Compound: Nirmatrelvir
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability
    [PMID: 38432056]
    Huh-7 CC50
    > 50000 nM
    Compound: 4
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 7 days by Celltiter -Glo assay
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 7 days by Celltiter -Glo assay
    [PMID: 38518735]
    MRC5 CC50
    > 30 μM
    Compound: PF-07321332
    Cytotoxicity against human MRC5 cells incubated for 120 hrs by Cell-Titer Glo assay
    Cytotoxicity against human MRC5 cells incubated for 120 hrs by Cell-Titer Glo assay
    [PMID: 38335279]
    MRC5 CC50
    > 50000 nM
    Compound: 4
    Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 7 days by Celltiter -Glo assay
    Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 7 days by Celltiter -Glo assay
    [PMID: 38518735]
    MRC5 EC50
    0.212 μM
    Compound: Nirmatrelvir
    Antiviral activity against against Human coronavirus 229E infected in human MRC5 cells assessed as reduction in cell viability measured after 4 days by CellTiter-Glo luminescence assay
    Antiviral activity against against Human coronavirus 229E infected in human MRC5 cells assessed as reduction in cell viability measured after 4 days by CellTiter-Glo luminescence assay
    [PMID: 35971455]
    PBMC CC50
    > 100 μM
    Compound: Nirmatrelvir
    Cytotoxicity against human PBMC cells assessed as reduction in cell viability
    Cytotoxicity against human PBMC cells assessed as reduction in cell viability
    [PMID: 38432056]
    Vero CC50
    > 100 μM
    Compound: Nirmatrelvir
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
    [PMID: 38432056]
    Vero CC50
    > 25 μM
    Compound: Nirmatrevir
    Cytotoxicity against african green monkey Vero cells
    Cytotoxicity against african green monkey Vero cells
    [PMID: 36870624]
    Vero C1008 CC50
    > 100 μM
    Compound: 1
    Cytotoxicity against African green monkey Vero E6 cells incubated for 3 days by WST-8 assay
    Cytotoxicity against African green monkey Vero E6 cells incubated for 3 days by WST-8 assay
    [PMID: 37756225]
    Vero C1008 CC50
    > 100 μM
    Compound: 1
    Cytotoxicity in African green monkey Vero E6 cells measured after 25 days by Neutral red release assay
    Cytotoxicity in African green monkey Vero E6 cells measured after 25 days by Neutral red release assay
    [PMID: 37992202]
    Vero C1008 CC50
    > 100 μM
    Compound: Nirmatrelvir
    Cytotoxicity against african green monkey Vero E6 cells assessed as reduction in cell viability after 26 hrs by MTS assay
    Cytotoxicity against african green monkey Vero E6 cells assessed as reduction in cell viability after 26 hrs by MTS assay
    [PMID: 36475694]
    Vero C1008 CC50
    > 500 μM
    Compound: 1
    Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    [PMID: 37594952]
    Vero C1008 CC50
    > 500 μM
    Compound: Nirmatrelvir
    Cytotoxicity against African green monkey Vero E6 cells incubated for 48 hrs by Luminescent cell viability assay
    Cytotoxicity against African green monkey Vero E6 cells incubated for 48 hrs by Luminescent cell viability assay
    [PMID: 37253309]
    Vero C1008 CC50
    > 50000 nM
    Compound: PF-07321332
    Cytotoxicity against African green monkey Vero E6 cells transfected with TMPRSS2 assessed as reduction in cell viability
    Cytotoxicity against African green monkey Vero E6 cells transfected with TMPRSS2 assessed as reduction in cell viability
    [PMID: 36229406]
    Vero C1008 EC50
    0.074 μM
    Compound: 1; PF-07321332
    Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in viral growth incubated for 24 hrs by fluorescence based analysis
    Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in viral growth incubated for 24 hrs by fluorescence based analysis
    [PMID: 37244162]
    Vero C1008 EC50
    0.075 μM
    Compound: Nirmatrelvir
    Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in virus induced cytopathic effect incubated for 3 days
    Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in virus induced cytopathic effect incubated for 3 days
    [PMID: 36475694]
    Vero C1008 EC50
    0.729 μM
    Compound: 1
    Antiviral activity against SARS-CoV-2 B1.617.2 (Delta) infected in african green monkey Vero E6 cells assessed as reduction in viral replication incubated for 24 hrs by qRT-PCR analysis
    Antiviral activity against SARS-CoV-2 B1.617.2 (Delta) infected in african green monkey Vero E6 cells assessed as reduction in viral replication incubated for 24 hrs by qRT-PCR analysis
    [PMID: 37594952]
    Vero C1008 EC50
    21.7 nM
    Compound: PF-07321332
    Antiviral activity against SARS-CoV-2 variant Omicron BA.2 infected in African green monkey Vero E6 cells assessed as reduction in virus-induced cytopathic effect
    Antiviral activity against SARS-CoV-2 variant Omicron BA.2 infected in African green monkey Vero E6 cells assessed as reduction in virus-induced cytopathic effect
    [PMID: 37229831]
    Vero C1008 EC50
    75 nM
    Compound: 13
    Antiviral activity against SARS Cov-2 infected in Vero E6 cells expressing hACE2 assessed as virus induced cytopathic effect incubated for 3 day by Cell Titer-Glo assay
    Antiviral activity against SARS Cov-2 infected in Vero E6 cells expressing hACE2 assessed as virus induced cytopathic effect incubated for 3 day by Cell Titer-Glo assay
    [PMID: 35291756]
    In Vitro

    3CLPRO is responsible for cleaving polyproteins 1a and 1ab of SARS-CoV-2.1. Without the activity of the SARS-CoV-2 3CLPRO, nonstructural proteins (including proteases) cannot be released to perform their functions, inhibiting viral replication[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    499.53

    Formula

    C23H32F3N5O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NCC1)[C@@H]1C[C@@H](C#N)NC([C@@H]2[C@]3([H])[C@@](CN2C([C@H](C(C)(C)C)NC(C(F)(F)F)=O)=O)([H])C3(C)C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 140 mg/mL (280.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 50 mg/mL (100.09 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0019 mL 10.0094 mL 20.0188 mL
    5 mM 0.4004 mL 2.0019 mL 4.0038 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.74%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.0019 mL 10.0094 mL 20.0188 mL 50.0470 mL
    5 mM 0.4004 mL 2.0019 mL 4.0038 mL 10.0094 mL
    10 mM 0.2002 mL 1.0009 mL 2.0019 mL 5.0047 mL
    15 mM 0.1335 mL 0.6673 mL 1.3346 mL 3.3365 mL
    20 mM 0.1001 mL 0.5005 mL 1.0009 mL 2.5024 mL
    25 mM 0.0801 mL 0.4004 mL 0.8008 mL 2.0019 mL
    30 mM 0.0667 mL 0.3336 mL 0.6673 mL 1.6682 mL
    40 mM 0.0500 mL 0.2502 mL 0.5005 mL 1.2512 mL
    50 mM 0.0400 mL 0.2002 mL 0.4004 mL 1.0009 mL
    60 mM 0.0334 mL 0.1668 mL 0.3336 mL 0.8341 mL
    80 mM 0.0250 mL 0.1251 mL 0.2502 mL 0.6256 mL
    100 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5005 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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