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Cat. No. Name Size Price Add Cart
KI0799Zafirlukast50 mg$154

Chemical Characteristic

Product NameZafirlukast
SynonymsAccolate
CAS No.107753-78-6
Molecular Weight 575.68
FormulaC31H33N3O6S
Chemical NameCyclopentyl N-[3-{[2-methoxy-4-[(2-methylphenyl) sulfonylcarbamoyl]phenyl]methyl}-1-methyl-indol-5-yl]carbamate
SmilesC(=O)(Nc1cc2c(cn(c2cc1)C)Cc1c(cc(cc1)C(=O)NS(=O)(=O)c1c(cccc1)C)OC)OC1CCCC1
Chemical Structure

Biological activities

Zafirlukast is a cysteinyl leukotriene receptor antagonist. Zafirlukast has high affinity for the leukotriene D4 (LTD4) receptor in a competitive manner. Zafirlukast is effective in both the prophylaxis and the chronic treatment of allergic and exercise-induced asthma and can reduce the constriction of the human airway and the pulmonary vascular smooth muscle. Zafirlukast inhibits the hydroxylation of tolbutamide (CYP2C9), triazolam (CYP3A) and S-mephenytoin (CYP2C19) with IC50 of 7.0, 20.9 and 32.7µM, respectively. Besides, zafirlukast is a less potent inhibitor of phenacetin O-deethylation (CYP1A2) and dextromethorphan O-demethylation (CYP2D6) with IC50 of 56 and 116µM, respectively.[1] Zafirlukast inhibits the elimination of pioglitazone in human liver microsomes (HLM) with an IC50 of 1.0µM.[2] In vivo, a total of five glutathione (GSH) conjugates are detected in the bile of rats dosed with zafirlukast at 5 mg/kg iv or 20 mg/kg po. The enzyme inhibitory property of zafirlukast is selective, and the inactivation is characterized by a Kι of 13.4µM and Kinact of 0.026 min-1.[3]

Protocols

Zafirlukast is dissolved in DMSO.[3]

References

[1] Shader RI, et al. Inhibition of human cytochrome P450 isoforms in vitro by zafirlukast. Biopharm Drug Dispos. 1999, 20 (8): 385-388.
[2] Jaakkola T, et al. Montelukast and zafirlukast do not affect the pharmacokinetics of the CYP2C8 substrate pioglitazone. Eur J Clin Pharmacol. 2006, 62(7): 503-509.
[3] Kassahun K, et al. Zafirlukast metabolism by cytochrome P450 3A4 produces an electrophilic , -unsaturated iminium species that results in the selective mechanism-based inactivation of the enzyme. Chem Res Toxicol. 2005, 18 (9): 1427- 1437.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

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