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Catalog No.
oral leukotriene receptor antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
In stock

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Email: [email protected]

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Zafirlukast is a leukotriene receptor antagonist (LTRA). (IC50=0.6 uM, IC50=7.0 uM for CYP2C9)

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.107753-78-6
Solubility≥23.9 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Namecyclopentyl N-[3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methylindol-5-yl]carbamate
SDFDownload SDF
Canonical SMILESCC1=CC=CC=C1S(=O)(=O)NC(=O)C2=CC(=C(C=C2)CC3=CN(C4=C3C=C(C=C4)NC(=O)OC5CCCC5)C)OC
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.


Antibacterial experiment [1]:


Gram-positive and Gram-negative bacteria

Preparation method

The solubility of this compound in DMSO is > 23.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

12.5 ~ > 100 μM


Zafirlukast exhibited antibacterial and antibiofilm activities against Gram-positive bacteria (including the cariogenic pathogen S. mutans) whilst showed no significant activity against Gram-negative bacteria (except for the oral pathogen P. gingivalis). Additional tests showed that Zafirlukast did not cause resistance in S. mutans.

Animal experiment [2]:

Animal models

A rat model of colitis

Dosage form

40 or 80 mg/kg; orally or rectally; for 3 consecutive days


In a rat model of colitis, pretreatment with Zafirlukast (80 mg/kg, orally) significantly decreased tissue malondialdehyde and myeloperoxidase, and meanwhile, increased the reduced glutathione and catalase levels, whilst there was no significant change when it was given rectally. At the dose of 40 mg/kg dose (orally and rectally), no significant protective effect was observed.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1]. Kassahun K, Skordos K, McIntosh I, Slaughter D, Doss GA, Baillie TA, Yost GS. Zafirlukast metabolism by cytochrome P450 3A4 produces an electrophilic alpha,beta-unsaturated iminium species that results in the selective mechanism-based inactivation of the enzyme. Chem Res Toxicol. 2005 Sep;18(9):1427-37.

[2]. Mahgoub AA, El-Medany AA, Hager HH, Mustafa AA, El-Sabah DM. Evaluating the prophylactic potential of zafirlukast against the toxic effects of acetic acid on the rat colon. Toxicol Lett. 2003 Nov 1;145(1):79-87.

Quality Control

Chemical structure