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

Montelukast  (Synonyms: MK0476 free base)

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

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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.

Montelukast Chemical Structure

Montelukast Chemical Structure

CAS No. : 158966-92-8

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

Based on 8 publication(s) in Google Scholar

Other Forms of Montelukast:

Montelukast Related Antibodies

Top Publications Citing Use of Products

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

 

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.
Clinical Trial
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.

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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.

  • Protocol 2

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

    Solubility: 2.08 mg/mL (3.55 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
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%

COA (252 KB) HNMR (282 KB) LCMS (93 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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