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

Montelukast sodium  (Synonyms: MK0476)

Cat. No.: HY-13315 Purity: 99.84%
SDS COA Handling Instructions

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.

Montelukast sodium Chemical Structure

Montelukast sodium Chemical Structure

CAS No. : 151767-02-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
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100 mg USD 80 In-stock
500 mg USD 160 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Montelukast sodium:

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  • Biological Activity

  • 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)

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:

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

Purity: 99.84%

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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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.

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Montelukast sodium
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