1. GPCR/G Protein
  2. Leukotriene Receptor
  3. Montelukast sodium

Montelukast sodium (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast sodium decreases eosinophil infiltration into the asthmatic airways. Montelukast sodium can also be used for COVID-19 research.

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

CAS No. : 151767-02-1

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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Montelukast sodium:

Top Publications Citing Use of Products

    Montelukast sodium purchased from MedChemExpress. Usage Cited in: Environ Pollut. 2026 May 1:396:127849.

    Effect of Montelukast (Mon) (500 μM) on the metabolic inhibition rate of tetraconazole enantiomers in the in vitro incubation mixtures with HLMs.

    Montelukast sodium purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 3;16(1):3177.  [Abstract]

    Schematic diagram of subcutaneous tumor treatment on C57BL/6 mice and representative images of Montelukast (5 mg/kg; i.p.; 7-26 d) on day 26.

    Montelukast sodium purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 3;16(1):3177.  [Abstract]

    Tumor growth of LTP-C9 with overexpression of PDHA1 WT was observed in C57BL/6 mice treated with Montelukast (5 mg/kg; i.p.; 7-26 d).

    Montelukast sodium purchased from MedChemExpress. Usage Cited in: SSRN. 2024 Oct 29.

    Montelukast (M) (2.5-5.0 mg/kg; i.p.; once daily for 19 weeks) reduced urine protein levels and concentrations of autoantibodies, including ANA and anti-dsDNA of MRL/Lpr mice.

    Montelukast sodium purchased from MedChemExpress. Usage Cited in: SSRN. 2024 Oct 29.

    Montelukast (M) (2.5-5.0 mg/kg; i.p.; once daily for 19 weeks) decreased the percentages of ASCs, plasma cells, and plasmablasts in the spleen of MRL/Lpr mice.

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    • Purity & Documentation

    • References

    • Customer Review

    Description

    Montelukast sodium (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast sodium decreases eosinophil infiltration into the asthmatic airways. Montelukast sodium can also be used for COVID-19 research[1][2][3][4].

    IC50 & Target[1]

    CysLT1

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    0.31 μM
    Compound: Singulair
    Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
    Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
    [PMID: 26985325]
    HEK293 IC50
    27 μM
    Compound: Singulair
    Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
    Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
    [PMID: 26985325]
    In Vitro

    Montelukast (5 μM; 1 h) inhibits APAP (Acetaminophen) (HY-66005)-induced cell damage[1].
    Montelukast (0.01-10 μM; 30 min) diminishes the 5-oxo-ETE–induced cell migration and modulates the activation of the plasmin-plasminogen system[3].
    Montelukast (10 μM; 18 h) modulates the activation of MMP-9[3].

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

    Cell Migration Assay [3]

    Cell Line: Eosinophils
    Concentration: 0.01-10 μM
    Incubation Time: 30 min
    Result: Diminished the 5-oxo-ETE–induced cell migration.

    Western Blot Analysis[3]

    Cell Line: Eosinophils
    Concentration: 10 μM
    Incubation Time: 18 h
    Result: Reduced the 5-oxo-ETE–boosted MMP-9 secretion.
    In Vivo

    Montelukast (3 mg/kg; oral gavage) protects against APAP-induced hepatotoxicity in mice[1].
    Montelukast (1 mg/kg; miniosmotic pump administration) reduces the airway remodeling changes observed in OVA-treated mice and blocks the actions of cysteinyl leukotrienes (LT) C4, D4, and E4 mediated by the CysLT1 receptor[2].
    Montelukast (1 mg/kg; miniosmotic pump administration) reduces the elevated levels of IL-4 and IL-13 found in the BAL fluid of OVA-treated mice[2].

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

    Animal Model: C57BL/6J mice (8-week-old; 22-25 g) are induced acute hepatic injury[1]
    Dosage: 3 mg/kg
    Administration: Oral gavage 1 h after saline or APAP administration
    Result: Decreased serum levels of alanine transaminase (ALT) and aspartate aminotransferase (AST), and alleviated liver damage.
    Clinical Trial
    Molecular Weight

    608.17

    Formula

    C35H35ClNNaO3S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CC2=C(C=C1)C=CC(/C=C/C3=CC([C@H](SCC4(CC(O[Na])=O)CC4)CCC5=CC=CC=C5C(C)(O)C)=CC=C3)=N2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 50 mg/mL (82.21 mM)

    DMSO : 50 mg/mL (82.21 mM; Need ultrasonic; 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 1.6443 mL 8.2214 mL 16.4428 mL
    5 mM 0.3289 mL 1.6443 mL 3.2886 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • 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)

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 1 mg/mL (1.64 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

    • Protocol 2

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 25 mg/mL (41.11 mM); Clear solution; Need ultrasonic

    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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation
    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 (sealed storage, away from moisture). 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
    H2O / DMSO 1 mM 1.6443 mL 8.2214 mL 16.4428 mL 41.1069 mL
    5 mM 0.3289 mL 1.6443 mL 3.2886 mL 8.2214 mL
    10 mM 0.1644 mL 0.8221 mL 1.6443 mL 4.1107 mL
    15 mM 0.1096 mL 0.5481 mL 1.0962 mL 2.7405 mL
    20 mM 0.0822 mL 0.4111 mL 0.8221 mL 2.0553 mL
    25 mM 0.0658 mL 0.3289 mL 0.6577 mL 1.6443 mL
    30 mM 0.0548 mL 0.2740 mL 0.5481 mL 1.3702 mL
    40 mM 0.0411 mL 0.2055 mL 0.4111 mL 1.0277 mL
    50 mM 0.0329 mL 0.1644 mL 0.3289 mL 0.8221 mL
    60 mM 0.0274 mL 0.1370 mL 0.2740 mL 0.6851 mL
    80 mM 0.0206 mL 0.1028 mL 0.2055 mL 0.5138 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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    Product Name:
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