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Zafirlukast (ICI-204219)

Name: Zafirlukast (ICI-204219)
Brand: Selleck Chemicals
SKU: S1633
Rating: 5 (5 reviews)

Catalog No.S1633

For research use only.

Zafirlukast (ICI-204219) is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms.

Zafirlukast (ICI-204219) Chemical Structure

CAS No. 107753-78-6

Selleck's Zafirlukast (ICI-204219) has been cited by 5 Publications

Purity & Quality Control

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Biological Activity

Description

Zafirlukast (ICI-204219) 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 (from reference)

References

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. Click to purchase: PEG300 Tween 80	20mg/mL

Chemical Information

Molecular Weight	575.68
Formula	C₃₁H₃₃N₃O₆S
CAS No.	107753-78-6
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
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

Download Zafirlukast (ICI-204219) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02950480	Terminated	Drug: zafirlukast\|Other: Standard of Care (no intervention)	Breast Cancer	University of California San Francisco	March 13 2017	Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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