| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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Montelukast (also known as MK-476; MK 476; MK0476; trade names Singulair; Monteflo; Lukotas; Lumona) is a novel, potent, selective CysLT1 (leukotriene receptor) receptor antagonist used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. Montelukast blocks the action of leukotriene D4 (and secondary ligands LTC4 and LTE4) on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene and results in less inflammation.
| Targets |
CysLT1
|
|---|---|
| ln Vitro |
Montelukast (5 μM; 1 hour) prevents cell damage caused by acetaminophen (APAP) [1]. The 30-minute administration of montelukast (0.01-10 μM) inhibits the migration of cells produced by 5-oxo-ETE and modifies the activation of the plasmin-plasminogen system [3]. The 18-hour duration of 10 μM montelukast modifies MMP-9 activity [3].
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| ln Vivo |
Montelukast (3 mg/kg; orally administered) shields mice from hepatotoxicity caused by APAP [1]. When administered via a micro-osmotic pump, montelukast (1 mg/kg) inhibits the production of cysteinyl leukotriene (LT) via the CysLT1 receptor and lessens the alterations in airway remodeling that occur in mice treated with OVA. C4, D4, and E4's roles[2]. Increased levels of IL-4 and IL-13 in the BAL fluid of mice treated with OVA can be decreased by administering 1 mg/kg of montelukast using a micro-osmotic pump [2].
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| Cell Assay |
Cell migration assay [3]
Cell Types: Eosinophils Tested Concentrations: 0.01-10 μM Incubation Duration: 30 minutes Experimental Results: diminished 5-oxo-ETE-induced cell migration. Western Blot Analysis[3] Cell Types: Eosinophils Tested Concentrations: 10 μM Incubation Duration: 18 hrs (hours) Experimental Results: diminished 5-oxo-ETE-promoted MMP-9 secretion. |
| Animal Protocol |
Animal/Disease Models: C57BL/6J mice (8 weeks old; 22-25 g) induced acute liver injury [1]
Doses: 3 mg/kg Route of Administration: po (oral gavage) 1 hour after administration of normal saline or APAP Experimental Results: Serum moderate alanine aminotransferase (ALT) and aspartate aminotransferase (AST), and reduce liver damage. |
| References |
[1]. Pu S, et, al. Montelukast Prevents Mice Against Acetaminophen-Induced Liver Injury. Front Pharmacol. 2019 Sep 18; 10:1070.
[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. [3]. Langlois A, et al. Montelukast regulates eosinophil protease activity through a leukotriene-independent mechanism. J Allergy Clin Immunol. 2006;118(1):113-119. [4]. Khan AR, et al. Montelukast in hospitalized patients diagnosed with COVID-19. J Asthma. 2022 Apr;59(4):780-786. |
| Molecular Formula |
C35H36CLNO3S
|
|---|---|
| Molecular Weight |
586.18
|
| Exact Mass |
585.210442
|
| Elemental Analysis |
C, 71.72; H, 6.19; Cl, 6.05; N, 2.39; O, 8.19; S, 5.47
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| CAS # |
158966-92-8
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| Related CAS # |
Montelukast sodium;151767-02-1;Montelukast dicyclohexylamine;577953-88-9;Montelukast-d6;1093746-29-2
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| Appearance |
Light yellow to yellow solid
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| LogP |
7.7
|
| tPSA |
95.7Ų
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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
|
| InChi Key |
UCHDWCPVSPXUMX-TZIWLTJVSA-N
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| InChi Code |
InChI=1S/C35H36ClNO3S/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39)/b15-10+/t32-/m1/s1
|
| Chemical Name |
Cyclopropaneacetic acid, 1-((((1R)-1-(3-((1E)-2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)-
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| Synonyms |
MK-476; MK 476; MK0476; trade names Singulair; Monteflo; Lukotas; Lumona
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~426.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (3.55 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1706 mL | 0.8530 mL | 1.7060 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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