2. GPCR/G Protein
  3. Leukotriene Receptor
  4. Montelukast

Montelukast  (Synonyms: MK0476 free base)

Cat. No.: HY-13315A Purity: 99.94%
COA
SDS
Handling Instructions Technical Support

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

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

CAS No. : 158966-92-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Montelukast:

Montelukast Related Antibodies

Top Publications Citing Use of Products

    Montelukast 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 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 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 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 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.

    View All Leukotriene Receptor Isoform Specific Products:

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    LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1]

    CysLT1

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK-293T IC50
    > 10000 nM
    Compound: montelukast
    Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
    Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
    		[PMID: 26200813]
    J774.A1 IC50
    8.7 μM
    Compound: Montelukast
    Anti-inflammatory activity in mouse J774.A1 cells assessed as suppression of LPS-induced IL-6 production by ELISA analysis
    Anti-inflammatory activity in mouse J774.A1 cells assessed as suppression of LPS-induced IL-6 production by ELISA analysis
    		[PMID: 37683361]
    U-937 IC50
    0.78 nM
    Compound: 1 (Singulair)
    In vitro inhibition of [3H]-LTD4 binding to LTD4 receptor of DMSO differentiated human U937 cell membranes
    In vitro inhibition of [3H]-LTD4 binding to LTD4 receptor of DMSO differentiated human U937 cell membranes
    		[PMID: 9871597]
    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.

    Montelukast Related Antibodies

    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.
    Molecular Weight

    586.18

    Formula

    C35H36ClNO3S
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(O)CC1(CS[C@@H](C2=CC=CC(/C=C/C3=NC4=CC(Cl)=CC=C4C=C3)=C2)CCC5=CC=CC=C5C(C)(O)C)CC1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 233.33 mg/mL (398.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7060 mL 8.5298 mL 17.0596 mL
    5 mM 0.3412 mL 1.7060 mL 3.4119 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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

    ×
    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    90% Corn Oil

      Solubility: ≥ 5 mg/mL (8.53 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 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 (50.0 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: 99.94%

    SDS (393 KB)

    COA (252 KB) HNMR (275 KB) LCMS (104 KB)

    Handling Instructions (2659 KB)
    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
    DMSO 1 mM 1.7060 mL 8.5298 mL 17.0596 mL 42.6490 mL
    5 mM 0.3412 mL 1.7060 mL 3.4119 mL 8.5298 mL
    10 mM 0.1706 mL 0.8530 mL 1.7060 mL 4.2649 mL
    15 mM 0.1137 mL 0.5687 mL 1.1373 mL 2.8433 mL
    20 mM 0.0853 mL 0.4265 mL 0.8530 mL 2.1325 mL
    25 mM 0.0682 mL 0.3412 mL 0.6824 mL 1.7060 mL
    30 mM 0.0569 mL 0.2843 mL 0.5687 mL 1.4216 mL
    40 mM 0.0426 mL 0.2132 mL 0.4265 mL 1.0662 mL
    50 mM 0.0341 mL 0.1706 mL 0.3412 mL 0.8530 mL
    60 mM 0.0284 mL 0.1422 mL 0.2843 mL 0.7108 mL
    80 mM 0.0213 mL 0.1066 mL 0.2132 mL 0.5331 mL
    100 mM 0.0171 mL 0.0853 mL 0.1706 mL 0.4265 mL
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    Montelukast 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:

    Montelukast158966-92-8MK0476MK 0476MK-0476Leukotriene ReceptorcysteinylleukotrieneCysltr1asthmaliverinjuryantioxidantintestinalischemia–reperfusionicardiacdamageCOVID-19Inhibitorinhibitorinhibit

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