Zafirlukast

Catalog No.S1633 Synonyms: ICI-204219

Zafirlukast  Chemical Structure

Molecular Weight(MW): 575.68

Zafirlukast is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 97 In stock
USD 970 In stock
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Biological Activity

Description Zafirlukast is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms.
Targets
leukotriene receptor [1]
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]

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 individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
Synonyms ICI-204219

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02950480 Not yet recruiting Breast Cancer University of California, San Francisco November 2016 Phase 2
NCT01283061 Completed Healthy Dr. Reddys Laboratories Limited December 2007 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID