Montelukast
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.94%
- CAS No.: 158966-92-8
- 화학식: C35H36ClNO3S
- 분자량:586.18
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Montelukast
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Adv Mater. 2024 Jun;36(24):e2311760. [Abstract]
- Nat Commun. 2025 Apr 3;16(1):3177. [Abstract]
- J Cachexia Sarcopenia Muscle. 2022 Aug;13(4):2242-2253. [Abstract]
- Cell Rep. 2026 Jun 2;45(6):117490. [Abstract]
- Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]
- Anal Chem. 2025 Nov 18;97(45):25158-25167. [Abstract]
- Environ Pollut. 2026 May 1:396:127849. [Abstract]
- Eur J Pharmacol. 2022 May 15;923:174892. [Abstract]
- Artif Cell Nanomed B. 2019 Dec;47(1):4234-4239. [Abstract]
- Naunyn Schmiedebergs Arch Pharmacol. 2023 Aug;396(8):1759-1771. [Abstract]
- SSRN. 2024 Oct 29.
- Patent. US20230404992A1.
- Patent. US20230348536A1.
- Patent. US20210309696A1.
Customer Validation & Images
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Flow Cytometry
All Leukotriene Receptor Isoforms
More
Biological Activity
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CysLT1 |
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | IC50 |
>10000 nM
Compound: montelukast
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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
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[PMID: 26200813] |
| J774.A1 | IC50 |
8.7 μM
Compound: Montelukast
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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
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[PMID: 37683361] |
| U-937 | IC50 |
0.78 nM
Compound: 1 (Singulair)
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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
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[PMID: 9871597] |
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.
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Cell Line:Eosinophils
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Concentration:0.01-10 μM
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Incubation Time:30 min
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Result:Diminished the 5-oxo-ETE–induced cell migration.
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Cell Line:Eosinophils
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Concentration:10 μM
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Incubation Time:18 h
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Result:Reduced the 5-oxo-ETE–boosted MMP-9 secretion.
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.
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Animal Model:C57BL/6J mice (8-week-old; 22-25 g) are induced acute hepatic injury[1]
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Dosage:3 mg/kg
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Administration:Oral gavage 1 h after saline or APAP administration
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Result:Decreased serum levels of alanine transaminase (ALT) and aspartate aminotransferase (AST), and alleviated liver damage.
Chemical Information
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CAS No. 158966-92-8
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Appearance Solid
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분자량 586.18
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화학식 C35H36ClNO3S
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Color Off-white to yellow
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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
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Synonyms
MK0476 free base
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (15)
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Journal Impact Factor
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Most Recent
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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).
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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 -
Cell Rep
HSPA6 maintains IMPDH2 phosphorylation to regulate GTP synthesis for driving radioresistance of glioblastoma stem cells. [Abstract]2026 Jun 2;45(6):117490. PMID: 42234559 -
Cell Rep
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 -
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.
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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 -
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.
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용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (280 KB)
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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)
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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]
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 |
Montelukast Related Classifications
HY-13315A Related Classifications
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