Home Immunology & Inflammation LTR antagonist Zafirlukast For research use only.

Zafirlukast

Synonyms: ICI-204219

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

Zafirlukast Chemical Structure

Zafirlukast Chemical Structure

CAS No. 107753-78-6

Purity & Quality Control

Zafirlukast Related Products

Biological Activity

Description Zafirlukast is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms.
Targets
leukotriene receptor [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02950480 Terminated
Breast Cancer
University of California San Francisco
 March 13 2017 Phase 2

Chemical Information & Solubility

Molecular Weight 575.68 Formula

C31H33N3O6S
CAS No. 107753-78-6 SDF Download Zafirlukast SDF
Smiles CC1=CC=CC=C1S(=O)(=O)NC(=O)C2=CC(=C(C=C2)CC3=CN(C4=C3C=C(C=C4)NC(=O)OC5CCCC5)C)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (173.7 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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