A CysLT1 receptor antagonist
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Alternative(s)
10008318Montelukast (sodium salt)
Labeled Version(s)
22180Montelukast-d6 (sodium salt)
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Montelukast

Item No. 35779

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
CAS Number
158966-92-8
Synonyms
  • MK-476
Molecular Formula
C35H36ClNO3S
Formula Weight
586.2
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/ml
λmax
245, 284, 327, 359 nm
SMILES
CC(C)(O)C(C=CC=C1)=C1CC[C@H](C2=CC(/C=C/C3=NC4=C(C=CC(Cl)=C4)C=C3)=CC=C2)SCC5(CC5)CC(O)=O
InChi Code
InChI=1S/C35H36ClNO3S/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)/b15-10+/t32-/m1/s1
InChi Key
UCHDWCPVSPXUMX-TZIWLTJVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    50 mg

    $75

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    100 mg

    $156

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    250 mg

    $283

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    500 mg

    $530

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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).