Montelukast

- Overview
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    Background
    
    Montelukast is a potent, selective and orally-active antagonist of the cysteinyl leukotriene 1 (CysLT1) receptor, with an IC50 value of 4.9 nM in HEK293 cell membranes expressing human CysLT1 receptors. The CysLT1 receptor is a receptor for cysteinyl leukotrienes (e.g. LTC4, LTD4, and LTE4) which mediate allergic and hypersensitivity reactions in a variety of inflammatory disorders, in particular asthma. Montelukast has been introduced clinically for the treatment of asthma, allergic rhinitis, and exercise-induced bronchoconstriction.
    
    1. Sarau HM, Ames RS, Chambers J, et al. Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. Molecular Pharmacology, 1999, 56(3): 657-663.
    2. Storms W. Update on montelukast and its role in the treatment of asthma, allergic rhinitis and exercise-induced bronchoconstriction. Expert Opinion on Pharmacotherapy, 2007, 8(13): 2173-2187.
    3. Eum SY, Maghni K, Hamid Q, et al. Involvement of the cysteinyl-leukotrienes in allergen-induced airway eosinophilia and hyperresponsiveness in the mouse. American Journal of Respiratory Cell and Molecular Biology, 2003, 28(1): 25-32.
- Properties
  - Categories
    
    A potent, selective and orally-active CysLT1 receptor antagonist
    
    Alternative Name
    
    (R,E)-2-(1-(((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propyl)thio)methyl)cyclopropyl)acetic acid
    
    CAS Number
    
    158966-92-8
    
    Molecular Formula
    
    C35H36ClNO3S
    
    Molecular Weight
    
    586.18
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥100mg/mL in DMSO; ≥10mg/mL in Ethanol; Insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC(C)(O)C1=CC=CC=C1CC[[email protected]@H](SCC2(CC2)CC(O)=O)C3=CC=CC(/C=C/C4=CC=C5C(C=C(Cl)C=C5)=N4)=C3
    
    * For Research Use Only