Zafirlukast
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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Biological Activity
| Description | Zafirlukast is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms. | |
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| Targets |
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| In vitro |
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. [1] |
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| 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. [2] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (173.7 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 4% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing. |
20mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 575.68 |
|---|---|
| Formula | C31H33N3O6S |
| CAS No. | 107753-78-6 |
| Storage | powder |
| in solvent | |
| Synonyms | ICI-204219 |
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