Montelukast

SKU: orb1226080

Description

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.\n(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.

Key Properties

• CAS Number: 158966-92-8
• MW: 586.18
• Purity: >98% (HPLC)
• Formula: C₃₅H₃₆ClNO₃S
• 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
• Target: Lipoxygenase
• Solubility: sparingly soluble in Water

Bioactivity

• 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. 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.
• 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. Cell Migration Assay Cell line: Eosinophils. Concentration: 0.01-10 μM Incubation time: 30 min. Result: Diminished the 5-oxo-ETE-induced cell migration. Western blot analysis. Cell line: Eosinophils. Concentration: 10 μM. Incubation time: 18 h. Result: Reduced the 5-oxo-ETE-boosted MMP-9 secretion.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Montelukast

Quick Database Links

Gene Symbol

Lipoxygenase