Montelukast sodium

SKU: orb1226160

Description

Montelukast sodium (MK0476, MK-0476) is a potent, selective, orally active leukotriene D4 receptor (LTD4) antagonist with Ki of 0.18 nM for guinea pig lung LTD4; shows no significant affinity for leukotriene C4 and leukotriene B4 receptors; Montelukast sodium is a potent and competitive antagonist of leukotriene D4-induced contractions of non-tonal guinea-pig trachea with pA2 of 9.3; antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v. leukotriene D4, blocksleukotriene D4 induced bronchoconstriction in vivo.Allergy Approved(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: 151767-02-1
• MW: 608.2
• Purity: >98% (HPLC)
• Formula: C₃₅H₃₅ClNNaO₃S
• SMILES: CC(C)(C1=CC=CC=C1CC[C@H](C2=CC=CC(=C2)/C=C/C3=NC4=C(C=CC(=C4)Cl)C=C3)SCC5(CC5)CC(=O)[O-])O.[Na+]
• Target: Leukotriene Receptor
• Solubility: H2O: ≥ 70 mg/mL

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

MK0476 | MK-0476

Quick Database Links

Gene Symbol

Leukotriene Receptor