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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

Montelukast (sodium salt)

Cayman Chemical Item Number 10008318

Singulair® (CAS 151767-02-1)

Montelukast (sodium salt) (CAS 151767-02-1)

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Description

The cysteinyl leukotrienes (CysLTs), LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of G protein-coupled receptors, CysLT1 and CysLT2.1,2,3 Montelukast (sodium salt) is a potent, selective CysLT1 receptor antagonist sold under the trade name Singulair for the treatment of asthma as well as for the symptoms associated with allergic rhinitis.4,5,6,7 It binds to the human CysLT1 receptor with an IC50 of less than 5 nM with no appreciable binding to the CysLT2 receptor.1,2,3

1 Lynch, K.R., O'Neill, G.P., Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature 399 789-793 (1999).

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

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

4 Leff, J.A., Busse, W.W., Pearlman, D., et al. Montelukast, a leukotriene-receptor antagonist, for the treatment of mild asthma and exercise-induced brochoconstriction. N Engl J Med 339 147-152 (1998).

5 Reiss, T.F., Chervinsky, P., Dockhorn, R.J., et al. Montelukast, a once-daily leukotriene receptor antagonist, in the treatment of chronic asthma. A multicenter, randomized, double-blind trial. Arch Intern Med 158 1213-1220 (1998).

6 Reiss, T.F., Altman, L.C., Chervinsky, P., et al. Effects of montelukast (MK-0476), a new potent cysteinyl leukotriene (LTD4) receptor antagonist, in patients with chronic asthma. J Allergy Clin Immunol 98 528-534 (1996).

7 Peters-Golden, M., and Henderson, W.R. The role of leukotrienes in allergic rhinitis. Ann Allergy Asthma Immunol 94 609-618 (2005).

Synonyms
  • Singulair®
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
Molecular Formula C35H35ClNO3S · Na
Formula Weight 608.2
Formulation A crystalline solid
Purity >98%
λmax 212, 284, 328, 345, 359 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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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+]​

Background Reading

Lynch, K.R., O'Neill, G.P., Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature 399 789-793 (1999).

Leff, J.A., Busse, W.W., Pearlman, D., et al. Montelukast, a leukotriene-receptor antagonist, for the treatment of mild asthma and exercise-induced brochoconstriction. N Engl J Med 339 147-152 (1998).

Reiss, T.F., Altman, L.C., Chervinsky, P., et al. Effects of montelukast (MK-0476), a new potent cysteinyl leukotriene (LTD4) receptor antagonist, in patients with chronic asthma. J Allergy Clin Immunol 98 528-534 (1996).

Peters-Golden, M., and Henderson, W.R. The role of leukotrienes in allergic rhinitis. Ann Allergy Asthma Immunol 94 609-618 (2005).

Reiss, T.F., Chervinsky, P., Dockhorn, R.J., et al. Montelukast, a once-daily leukotriene receptor antagonist, in the treatment of chronic asthma. A multicenter, randomized, double-blind trial. Arch Intern Med 158 1213-1220 (1998).

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

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

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Montelukast (sodium salt) is available in the following screening library:

Size Price Quantity Subtotal
10 mg $14.00 $0.00
50 mg $63.00 $0.00
100 mg $112.00 $0.00
500 mg $490.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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