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Zafirlukast

Chemical Structure : Zafirlukast

CAS No.: 107753-78-6

Zafirlukast (ICI-204219)

Catalog No.: PC-45294Not For Human Use, Lab Use Only.

Zafirlukast (ICI-204219) is a potent, selective, orally active cysteinyl leukotriene 1 (CysLT1) receptor antagonist with IC50 of 14 nM in cell-based calcium mobilization assays.

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Biological Activity

Zafirlukast (ICI-204219) is a potent, selective, orally active cysteinyl leukotriene 1 (CysLT1) receptor antagonist with IC50 of 14 nM in cell-based calcium mobilization assays.
Zafirlukast is selective for CysLT1 over CysLT2 receptors (IC50=58 uM).
Zafirlukast inhibits mucus secretion induced by leukotriene D4 (LTD4) in isolated guinea pig trachea (IC50=0.6 μM).
Zafirlukast (5 μM) inhibits ovalbumin-induced increases in tracheal mucus secretion in ovalbumin-sensitized guinea pigs by 65%.
Zafirlukast inhibits LTD4-induced bronchoconstriction in anesthetized guinea pigs (ED50 = 61 nmol/kg, i.v.).

Physicochemical Properties

M.Wt 575.6752
Formula C31H33N3O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Carbamic acid, N-[3-[[2-methoxy-4-[[[(2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]-, cyclopentyl ester

References

1. Buckner CK, et al. J Pharmacol Exp Ther. 1990 Jan;252(1):77-85.

2. Spector SL, et al. Am J Respir Crit Care Med. 1994 Sep;150(3):618-23.

3. Kidney JC, et al. Am Rev Respir Dis. 1993 Jan;147(1):215-7.

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