2. Anti-infection Metabolic Enzyme/Protease
  3. HCV HCV Protease SARS-CoV
  4. Glecaprevir

Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM. Glecaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 4.09 μM.

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

CAS No. : 1365970-03-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Glecaprevir:

Glecaprevir Related Antibodies

Top Publications Citing Use of Products

    Glecaprevir purchased from MedChemExpress. Usage Cited in: Bioorg Chem. 2026 Apr:171:109555.  [Abstract]

    Inhibition of HCV NS3/4A protease activity and molecular docking analysis. Recombinant His/MBP-tagged NS3/4A protein from JFH-1 and J4 strains was treated with test compounds (20 μM), using DMSO as the vehicle control and Glecaprevir (10 nM; 1 h) as the positive control. Relative protease activity at endpoint measurement. The results showed that for the JFH-1 strain, Glecaprevir exhibited rapid-onset inhibition, consistent with its established mechanism as a competitive inhibitor.

    Glecaprevir purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Feb 6;26(3):1381.  [Abstract]

    Glecaprevir (48 h) showed significantly reduced MDCK cell activity at a maximum concentration of 100 μM, with median maximum cytotoxic concentrations (CC50) of 77.32 μM.

    Glecaprevir purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Feb 6;26(3):1381.  [Abstract]

    Five mice in Glecaprevir (10-40 mg/kg; p.o.) groups were randomly selected 5 days after infection, and their lungs were dissected after euthanasia for examination by H&E staining analysis (n = 5). The yellow arrow represents granulocytes, the gray arrow represents the alveolar wall, the purple arrow represents alveolar dilation, the red arrow represents bleeding around the alveoli and blood vessels, the brown arrow represents epithelial cells, and the blue arrow represents macrophages.

    Glecaprevir purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Feb 6;26(3):1381.  [Abstract]

    Western blot images showed in Glecaprevir (10-40 mg/kg; p.o.) groups the expression of viral nucleoprotein (NP), hemagglutinin (HA) and structural protein (M1) in mouse lungs.

    Glecaprevir purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2022 Nov 14;40(11):1294-1305.e4.  [Abstract]

    Cytotoxicity of ON VIPER CARexpressing primary T cells in response to different NS3 inhibitors. The results showed that Glecaprevir (0.0001–10 μM) induced cell killing at lower concentrations.

    Glecaprevir purchased from MedChemExpress. Usage Cited in: Elife. 2020 Jun 9:9:e56469.  [Abstract]

    Knockoff in neurons required further attenuation of the cleavage site. Representative anti-GFP immunoblots from rat cortical neurons expressing substrates bearing the natural NS5A/5B cleavage sequence (EDVVCC/SMSY), modified sequence (EDVVCC/QMSY), and further attenuated sequence (ADVVCC/QMSY) in the presence of inhibitors. Glecaprevir (GCV, 10 μM) was the most effective inhibitor of substrate cleavage.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM. Glecaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 4.09 μM[2].

    IC50 & Target

    IC50: 3.5~11.3 nM (HCV NS3/4A protease)[1]
    Cellular Effect
    Cell Line Type Value Description References
    Huh-7 EC50
    0.2 nM
    Compound: GLE; ABT-493
    Antiviral activity against HCV genotype 1b harboring D168A mutant infected in human Huh7 cells incubated for 96 hrs by luciferase assay
    Antiviral activity against HCV genotype 1b harboring D168A mutant infected in human Huh7 cells incubated for 96 hrs by luciferase assay
    		[PMID: 34405680]
    Huh-7 EC50
    0.2 nM
    Compound: GLE; ABT-493
    Antiviral activity against HCV genotype 1b infected in human Huh7 cells incubated for 96 hrs by luciferase assay
    Antiviral activity against HCV genotype 1b infected in human Huh7 cells incubated for 96 hrs by luciferase assay
    		[PMID: 34405680]
    Huh-7 EC50
    230 nM
    Compound: GLE; ABT-493
    Antiviral activity against HCV genotype 1b harboring A156T mutant infected in human Huh7 cells incubated for 96 hrs by luciferase assay
    Antiviral activity against HCV genotype 1b harboring A156T mutant infected in human Huh7 cells incubated for 96 hrs by luciferase assay
    		[PMID: 34405680]
    In Vitro

    Glecaprevir inhibits the enzymatic activity of HCV genotype 1-6 NS3/4A proteases with half maximal inhibitory concentration (IC50) values ranging from 3.5 to 11.3 nM in a biochemical assay. Glecaprevir inhibites HCV subgenomic stable replicons containing proteases from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, 6a and 6e in Huh-7 cells with 50% effective concentration (EC50) values ranging from 0.21 to 4.6 nM. Glecaprevir is active against a replicon containing protease from genotype 3, the most difficult-to-treat HCV genotype, with an EC50 value of 1.9 nM, which is 10- and 44-fold lower than those for paritaprevir and grazoprevir, respectively. The median Glecaprevir EC50 values against replicons containing these genotype 1a, 1b, 2a, 2b, 3a, 4a, 4d, and 5a clinical samples are 0.08, 0.29, 1.6, 2.2, 2.3, 0.41, 0.17, and 0.12 nM, respectively, with an overall median EC50 value of 0.30 nM (range=0.05~3.8 nM)[1].

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

    Glecaprevir Related Antibodies
    Clinical Trial
    Molecular Weight

    838.87

    Formula

    C38H46F4N6O9S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@H]1N(C([C@@H](NC(O[C@@]2([H])[C@@]3([H])CCC2)=O)C(C)(C)C)=O)C[C@@](OC4=NC5=CC=CC=C5N=C4C(F)(/C=C/CO3)F)([H])C1)N[C@]6([C@H](C(F)F)C6)C(NS(=O)(C7(CC7)C)=O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 83.3 mg/mL (99.30 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1921 mL 5.9604 mL 11.9208 mL
    5 mM 0.2384 mL 1.1921 mL 2.3842 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    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 (2.48 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (2.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    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: 99.93%

    SDS (393 KB)

    COA (259 KB) LCMS (111 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    The activity of Glecaprevir, paritaprevir or grazoprevir is determined against nine cell lines each stably transfected with an HCV subgenomic replicon containing NS3 protease from a different HCV genotype using a luciferase reporter assay as described previously. All replicon constructs are bicistronic subgenomic replicons, and the replicon cell lines are generated by introducing these constructs into a Huh-7 human hepatoma-derived cell line. The inhibitory effect of Glecaprevir on HCV replication in replicon cells is determined in Dulbecco's modified eagle medium containing 5% fetal bovine serum with or without 40% human plasma. The EC50 values are determined using nonlinear regression curve[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.1921 mL 5.9604 mL 11.9208 mL 29.8020 mL
    5 mM 0.2384 mL 1.1921 mL 2.3842 mL 5.9604 mL
    10 mM 0.1192 mL 0.5960 mL 1.1921 mL 2.9802 mL
    15 mM 0.0795 mL 0.3974 mL 0.7947 mL 1.9868 mL
    20 mM 0.0596 mL 0.2980 mL 0.5960 mL 1.4901 mL
    25 mM 0.0477 mL 0.2384 mL 0.4768 mL 1.1921 mL
    30 mM 0.0397 mL 0.1987 mL 0.3974 mL 0.9934 mL
    40 mM 0.0298 mL 0.1490 mL 0.2980 mL 0.7450 mL
    50 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.5960 mL
    60 mM 0.0199 mL 0.0993 mL 0.1987 mL 0.4967 mL
    80 mM 0.0149 mL 0.0745 mL 0.1490 mL 0.3725 mL
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    Glecaprevir Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    Glecaprevir1365970-03-1ABT-493ABT493ABT 493HCVHCV ProteaseSARS-CoVHepatitis C virusSARS coronavirusInhibitorinhibitorinhibit

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