Montelukast

Research use only, not for human use.

Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies.

Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally. Montelukast blocks the action of leukotriene D4 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. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific locus of operation, it does not interact with other allergy medications such as theophylline. Montelukast is marketed in United States and many other countries by Merck & Co. with the brand name Singulair. It is available as oral tablets, chewable tablets, and oral granules. In India and other countries, it is also marketed under the brand name Montair, produced by Indian company Cipla. (In Vitro):Montelukast (5 μM; 1 h) inhibits APAP (Acetaminophen) (HY-66005)-induced cell damage.Montelukast (0.01-10 μM; 30 min) diminishes the 5-oxo-ETE–induced cell migration and modulates the activation of the plasmin-plasminogen system.Montelukast (10 μM; 18 h) modulates the activation of MMP-9.(In Vivo):Montelukast (3 mg/kg; oral gavage) protects against APAP-induced hepatotoxicity in mice.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.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.

Montelukast (5 μM; 1 h) inhibits APAP (Acetaminophen) (HY-66005)-induced cell damage.Montelukast (0.01-10 μM; 30 min) diminishes the 5-oxo-ETE–induced cell migration and modulates the activation of the plasmin-plasminogen system.Montelukast (10 μM; 18 h) modulates the activation of MMP-9. Cell Migration Assay Cell Line:Eosinophils Concentration:0.01-10 μM Incubation Time:30 minResult:Diminished the 5-oxo-ETE–induced cell migration.Western Blot AnalysisCell Line:EosinophilsConcentration:10 μMIncubation Time:18 h Result:Reduced the 5-oxo-ETE–boosted MMP-9 secretion.

Montelukast (3 mg/kg; oral gavage) protects against APAP-induced hepatotoxicity in mice.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.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. Animal Model:C57BL/6J mice (8-week-old; 22-25 g) are induced acute hepatic injury 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.

Montelukast

Immunology/Inflammation

Lipoxygenase

ALOX5| CysLTR1

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158966-92-8

586.18

C35H36ClNO3S

>98% (HPLC)

sparingly soluble in Water

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

Cyclopropaneacetic acid, 1-((((1R)-1-(3-((1E)-2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)-

(-20℃)

With Ice Pack

≥ 2 years