Cat. No.: HY-13315A

Montelukast

(Synonyms: MK0476 free base)

15 Cited Publications

Customer Review

Based on 15 publication(s) in Google Scholar

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.

Purity: 99.94%
CAS No.: 158966-92-8
Formula: C₃₅H₃₆ClNO₃S
Molecular Weight:586.18

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Montelukast Chemical Structure

CAS No.: 158966-92-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (15)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

CysLT₁

All Leukotriene Receptor Isoforms :

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.

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.

Chemical Information

CAS No. 158966-92-8
Appearance Solid
Molecular Weight 586.18
Formula C₃₅H₃₆ClNO₃S
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
Synonyms

MK0476 free base
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

Publications (15)

All In Vivo Efficacy StudyBio/Physico-chemical AssayFlow Cytometry

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Adv Mater

Efficient Delivery of Lomitapide using Hybrid Membrane-Coated Tetrahedral DNA Nanostructures for Glioblastoma Therapy. [Abstract]

2024 Jun;36(24):e2311760. PMID: 38569065
Nat Commun

Cholangiocarcinoma PDHA1 succinylation suppresses macrophage antigen presentation via alpha-ketoglutaric acid accumulation. [Abstract]

2025 Apr 3;16(1):3177. PMID: 40180922

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).
J Cachexia Sarcopenia Muscle

A disease-associated missense mutation in CYP4F3 affects the metabolism of leukotriene B4 via disruption of electron transfer. [Abstract]

2022 Aug;13(4):2242-2253. PMID: 35686338
Environ Pollut

Enantioselective metabolic mechanism and metabolism pathway of tetraconazole in human liver microsomes: In vitro and in silico study. [Abstract]

2026 May 1:396:127849. PMID: 41720237

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

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

2026 Jun 2;45(6):117490. PMID: 42234559
Cell Rep

Carvedilol sensitizes chemotherapy by targeting STING to boost anti-tumor immunity. [Abstract]

2025 Apr 16;44(5):115572. PMID: 40249703
Anal Chem

A Computational Integration Strategy Driven by Chemical Similarity Uncovers Comprehensive Metabolic Profiles of Small Bioactive Peptides via UHPLC-HRMS for Doping Control. [Abstract]

2025 Nov 18;97(45):25158-25167. PMID: 41202118
Eur J Pharmacol

Montelukast, cysteinyl leukotriene receptor 1 antagonist, inhibits cardiac fibrosis by activating APJ. [Abstract]

2022 May 15;923:174892. PMID: 35358494
Artif Cell Nanomed B

Montelukast promotes mitochondrial biogenesis via CREB/PGC-1α in human bronchial epithelial cells. [Abstract]

2019 Dec;47(1):4234-4239. PMID: 31722576
Naunyn Schmiedebergs Arch Pharmacol

Combined contributions of cytochrome P450s (CYPs) and non-enzymatic metabolism in the in vitro biotransformation of anaprazole, a novel proton pump inhibitor. [Abstract]

2023 Aug;396(8):1759-1771. PMID: 36847804
SSRN

2024 Oct 29.

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.
Patent

US20230404992A1.
Patent

US20230348536A1.
Patent

US20210309696A1.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7060 mL

8.5298 mL

17.0596 mL

5 mM

0.3412 mL

1.7060 mL

3.4119 mL

10 mM

0.1706 mL

0.8530 mL

1.7060 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Pu S, et, al. Montelukast Prevents Mice Against Acetaminophen-Induced Liver Injury. Front Pharmacol. 2019 Sep 18; 10:1070. [Content Brief]

[2]. William RHJ, et, al. A role for cysteinyl leukotrienes in airway remodeling in a mouse asthma model. Am J Respir Crit Care Med. 2002 Jan 1; 165(1): 108-16. [Content Brief]

[3]. Langlois A, et al. Montelukast regulates eosinophil protease activity through a leukotriene-independent mechanism. J Allergy Clin Immunol. 2006;118(1):113-119. [Content Brief]

[4]. Khan AR, et al. Montelukast in hospitalized patients diagnosed with COVID-19. J Asthma. 2022 Apr;59(4):780-786. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Publications Citing Use of MedChemExpress (MCE) Montelukast

All Leukotriene Receptor Isoforms

Biological Activity

Chemical Information

Publications (15)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Montelukast Related Classifications

HY-13315A Related Classifications