Montelukast Sodium

Catalog No.S4211 Synonyms: MK-0476

Montelukast Sodium Chemical Structure

Molecular Weight(MW): 608.17

Montelukast selectively antagonizes leukotriene D 4 (LTD4) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1.

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Biological Activity

Description Montelukast selectively antagonizes leukotriene D 4 (LTD4) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1.
Targets
CysLT1 [1]
In vitro

Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. [1]

In vivo Montelukast (6 mg/kg, once per day for 20 d) significantly suppresses the increased eosinophils in BAL fluid and lung tissue, and increases IL-5 level in BAL fluid in OVA challenged mice. OVA challenge increases CysLT1 but decreases CysLT2 receptor mRNA expression. Montelukast inhibits the increased CysLT1 but not the reduces CysLT2 expression after OVA challenge. [2]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (164.42 mM)
Water 100 mg/mL (164.42 mM)
Ethanol 100 mg/mL (164.42 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 608.17
Formula

C35H36ClNO3S.Na

CAS No. 151767-02-1
Storage powder
Synonyms MK-0476

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02889809 Recruiting Asthma GlaxoSmithKline October 2016 Phase 4
NCT02793375 Not yet recruiting Pain Childrens Hospital Medical Center, Cincinnati July 2016 Phase 3
NCT02762123 Completed Rheumatoid Arthritis Bristol-Myers Squibb May 2016 Phase 1
NCT02720081 Recruiting Asthma Merck Sharp & Dohme Corp. May 2016 Phase 2
NCT02761252 Completed Seasonal Allergic Rhinoconjunctivitis|Asthma Menarini International Operations Luxembourg SA April 2016 Phase 4
NCT02655562 Recruiting Coughing Beijing Chao Yang Hospital April 2016 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID