Catalog No.S1633 Synonyms: ICI-204219
Molecular Weight(MW): 575.68
Zafirlukast is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms.
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|Description||Zafirlukast is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms.|
Zafirlukast is similar to 3-methylindole because it contains an N-methylindole moiety that has a 3-alkyl substituent on the indole ring. Zafirlukast readily forms (10% conversion in 60 min) a GSH adduct with molecular mass of 880 Da upon incubation with horseradish peroxidase. Zafirlukast produces time-, concentration-, and NADP(H)-dependent inactivation of CYP3A4. Zafirlukast is shown to inhibit CYP3A enzyme activity in vitro (nonpreincubation inhibition) with a Ki of 2 μM in one report, but higher values have been published, and our KI for the inactivation process is 13.4 μM. Zafirlukast has high plasma protein binding (>99%), which would lower the free-drug concentration. Zafirlukast undergoes two successive one-electron oxidations to afford a highly electrophilic α,β-unsaturated iminium species, which reacts spontaneously with GSH to yield the observed adduct. 
|In vivo||Zafirlukast is a potent and selective cysteinyl leukotriene receptor antagonist which is used mainly in the prophylaxis of bronchial asthma. Zafirlukast in a dose of 80 mg/kg orally produces a significant decrease in tissue malondialdehyde, myeloperoxidase, and an increase in both reduced glutathione and catalase levels, while there is no significant changes with the rectal route. |
|In vitro||DMSO||100 mg/mL (173.7 mM)|
|In vivo||Add solvents individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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