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Pranlukast

Cayman Chemical Item Number 10008319

Ultair; ONO-1078 (CAS 103177-37-3)

Pranlukast (CAS 103177-37-3)

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Description

The cysteinyl leukotrienes (CysLT) 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 Pranlukast (ONO-1078) is a potent, selective and orally active CysLT1 receptor antagonist.4 Sold under the trade name Ultair, it was the first cysteinyl (peptidyl) leukotriene receptor antagonist (LTRA) marketed for the treatment of asthma.5 Clinical studies in Japan, Europe, and North America all show that pranlukast significantly attenuates bronchoconstriction in response to a variety of allergen challenges as well as to inhaled LTD4.5 Pranlukast binds to the human CysLT1 and CysLT2 receptors with IC50 values of approximately 4-7 nM and 3,600 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 Taniguchi, Y., Tamura, G., Honma, M., et al. The effect of an oral leukotriene antagonist ONO-1078, on allergen-induced immediate bronchoconstriction. J Allergy Clin Immunol 92 507-512 (1993).

5 Barnes, N.C., de Jong, B., and Miyamoto, T. Worldwide clinical experience with the first marketed leukotriene receptor antagonist. Chest 111 52-60 (1997).

Synonyms
  • Ultair
  • ONO-1078
Formal Name N-​[4-​oxo-​2-​(1H-​tetrazol-​5-​yl)-​4H-​1-​benzopyran-​8-​yl]-​4-​(4-​phenylbutoxy)-​benzamide
CAS Number 103177-37-3
Molecular Formula C27H23N5O4
Formula Weight 481.5
Formulation A crystalline solid
Purity ≥98%
λmax 255, 315 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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O=C(Nc1cccc2c(=O)​cc(oc12)​c1[nH]​nnn1)​c1ccc(OCCCCc2ccccc2)​cc1

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).

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).

Taniguchi, Y., Tamura, G., Honma, M., et al. The effect of an oral leukotriene antagonist ONO-1078, on allergen-induced immediate bronchoconstriction. J Allergy Clin Immunol 92 507-512 (1993).

Barnes, N.C., de Jong, B., and Miyamoto, T. Worldwide clinical experience with the first marketed leukotriene receptor antagonist. Chest 111 52-60 (1997).

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Pranlukast 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
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 2012-05-25. 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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