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Zafirlukast

Cayman Chemical Item Number 10008282

Accolate® (CAS 107753-78-6)

Zafirlukast (CAS 107753-78-6)

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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 Zafirlukast is a potent, selective CysLT1 receptor antagonist sold under the trade name Accolate for the treatment of asthma as well as for the symptoms associated with allergic rhinitis.4,5,6 It binds to the human CysLT1 and CysLT2 receptors with IC50 values of approximately 5 and 7,400 nM, respectively.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 Matassa, V.G., Maduskuie, T.P., Shapiro, H.S., et al. Evolution of a series of peptidoleukotriene antagonists: Synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles. J Med Chem 33 1781-1790 (1990).

5 Silverman, R.A., Nowak, R.M., Korenblat, P.E., et al. Zafirlukast treatment for acute asthma. Evaluation in a randomized, double-blind, multicenter trail. Chest 126 1480-1489 (2004).

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

Synonyms
  • Accolate®
Formal Name [3-​[[2-​methoxy-​4-​[[[(2-​methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-​1-​methyl-​1H-​indol-​5-​yl]-​carbamic acid,​ cyclopentyl ester
CAS Number 107753-78-6
Molecular Formula C31H33N3O6S
Formula Weight 575.7
Formulation A crystalline solid
Purity ≥97%
λmax 203, 215, 241, 299 nm
Stability 2 years
Storage -20°C
Shipping Wet ice in continental US; may vary elsewhere
SMILES
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COc1cc(ccc1Cc1cn(C)​c2ccc(NC(=O)​OC3CCCC3)​cc12)​C(=O)​NS(=O)​(=O)​c1ccccc1C

Background Reading

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).

Matassa, V.G., Maduskuie, T.P., Shapiro, H.S., et al. Evolution of a series of peptidoleukotriene antagonists: Synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles. J Med Chem 33 1781-1790 (1990).

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

Silverman, R.A., Nowak, R.M., Korenblat, P.E., et al. Zafirlukast treatment for acute asthma. Evaluation in a randomized, double-blind, multicenter trail. Chest 126 1480-1489 (2004).

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

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).

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Zafirlukast is available in the following screening library:

Size Price Quantity Subtotal
10 mg $14.00 $0.00
100 mg $112.00 $0.00
500 mg $490.00 $0.00
1 g $840.00 $0.00
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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 2012-05-26. 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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