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Zafirlukast (CAS 107753-78-6) LS-H16

CysLT1 receptor antagonist
LS-H16-10 / 10 mg / $175
LS-H16-100 / 100 mg / $235
LS-H16-500 / 500 mg / $515
LS-H16-1000 / 1000 mg / $875
USA Shipment Only
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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. Zafirlukast is a potent, selective cysteinyl-leukotrienes 1 (CysLT1) receptor antagonist sold under the trade name Accolate for the treatment of asthma as well as for the symptoms associated with allergic rhinitis. It binds to the human CysLT1 and CysLT2 receptors with IC50 values of approximately 5 and 7,400 nM, respectively. H16_ChemicalStructureImage.png
[3-[[2-methoxy-4-[[[(2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]-carbamic acid, cyclopentyl ester
Accolate
biochemical, chemical, antagonist
LS-H16
107753-78-6
C31H33N3O6S
≥97%
A crystalline solid
 
COc1cc(ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12)C(=O)NS(=O)(=O)c1ccccc1C
InChI=1S/C31H33N3O6S/c1-20-8-4-7-11-29(20)41(37,38)33-30(35)22-13-12-21(28(17-22)39-3)16-23-19-34(2)27-15-14-24(18-26(23)27)32-31(36)40-25-9-5-6-10-25/h4,7-8,11-15,17-19,25H,5-6,9-10,16H2,1-3H3,(H,32,36)(H,33,35)
YEEZWCHGZNKEEK-UHFFFAOYSA-N
Shipped at 4°C, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: CYSLTR1 / CYSLT1 related products

Usage Information

Zafirlukast is supplied as a crystalline solid. A stock solution may be made by dissolving the zafirlukast in an organic solvent purged with an inert gas. Zafirlukast is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of zafirlukast in these solvents is approximately 0.25, 20, and 30 mg/ml, respectively. Zafirlukast is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, zafirlukast should first be dissolved in DMF and then diluted with the aqueous buffer of choice. Zafirlukast has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Lynch, K.R., O’Neill, G.P., Liu, Q., et al. Nature 399, 789-793 (1999).
  2. Heise, C.E., O’Dowd, B.F., Figueroa, D.J., et al. J. Biol. Chem. 275, 30531-30536 (2000).
  3. Sarau, H.M., Ames, R.S., Chambers, J., et al. Mol. Pharmacol. 56, 657-663 (1999).
  4. Matassa, V.G., Maduskuie, T.P., Jr., Shapiro, H.S., et al. J. Med. Chem. 33, 1781-1790 (1990).
  5. Silverman, R.A., Nowak, R.M., Korenblat, P.E., et al. Chest 126, 1480-1489 (2004).

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