A CysLT1 receptor antagonist
Related Products
Alternative(s)
35779Montelukast
Labeled Version(s)
22180Montelukast-d6 (sodium salt)
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Montelukast (sodium salt)

Item No. 10008318

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[[[(1R)-1-[3-(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]-methyl]-cyclopropaneacetic acid, monosodium salt
CAS Number
151767-02-1
Synonyms
  • MK-476
Molecular Formula
C35H35ClNO3S • Na
Formula Weight
608.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2)(1:9): .15 mg/mlWater: 10 mg/ml
λmax
212, 284, 328, 345, 359 nm
SMILES
CC(C)(O)C(C=CC=C1)=C1CC[C@@H](SCC2(CC2)CC([O-])=O)C3=CC(/C=C/C4=NC5=CC(Cl)=CC=C5C=C4)=CC=C3.[Na+]
InChi Code
InChI=1S/C35H36ClNO3S.Na/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29;/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39);/q;+1/p-1/b15-10+;/t32-;/m1./s1
InChi Key
LBFBRXGCXUHRJY-HKHDRNBDSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

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    50 mg

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    100 mg

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    500 mg

    $655

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    Product Description

    Montelukast is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50 = 4.9 nM in HEK293 cell membranes expressing the human receptor).1 It is selective for CysLT1 over CysLT2 receptors (IC50 = >10,000 nM in COS-7 cell membranes expressing the human receptor).2 Montelukast inhibits bronchoconstriction induced by leukotriene D4 (LTD4; Item No. 20310) in anesthetized guinea pigs (ED50 = 69 nmol/kg, p.o.).3 It inhibits ovalbumin-induced airway hyperresponsiveness and increases in the number of total cells and eosinophils in bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma when administered at doses of 3 and 10 mg/kg.4 Formulations containing montelukast have been used in the treatment of asthma, allergic rhinitis, and exercise-induced bronchoconstriction.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sarau, H.M., Ames, R.S., Chambers, J., et al. Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. Mol. Pharmacol. 56(3), 657-663 (1999).

    2. Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. The Journal of Biological Chemisty 275(39), 30531-30536 (2000).

    3. Cabré, F., Carabaza, A., García, A.M., et al. Pharmacological profile of MEN91507, a new CysLT1 receptor antagonist. Eur. J. Pharmacol. 451(3), 317-326 (2002).

    4. Eum, S.Y., Maghni, K., Hamid, Q., et al. Involvement of the cysteinyl-leukotrienes in allergen-induced airway eosinophilia and hyperresponsiveness in the mouse. Am. J. Respir. Cell Mol. Biol. 28(1), 25-32 (2003).

    Product Citations

    Nagai, J., Balestrieri, B., Fanning, L.B., et al. P2Y6 signaling in alveolar macrophages prevents leukotriene-dependent type 2 allergic lung inflammation. J. Clin. Invest. 129(12), 5169-5186 (2019).

    Lorrain, D.S., Bain, G., Correa, L.D., et al. Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation. Eur. J. Pharmacol. 640(1-3), 211-218 (2010).