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Zafirlukast

Catalog No.GC15839

oral leukotriene receptor antagonist

Products are for research use only. Not for human use. We do not sell to patients.

Zafirlukast Chemical Structure

Cas No.: 107753-78-6

Size Price Stock Qty
10mM (in 1mL DMSO)
$91.00
In stock
100mg
$83.00
In stock
500mg
$297.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Antibacterial experiment [1]:

Bacteria

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

Applications

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

Applications

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.

References:

[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.

Background

Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist.

Zafirlukast is a peptidyl leukotriene antagonist and inhibitor of LTD4. After 13 weeks of exposure, the yield of lung tumors is significantly decreased by both dose levels of Zafirlukast (270 and 540 mg/kg), the high dose of Zileuton (1200 mg/kg), and the combinations containing 600 mg/kg Zileuton with either Zafirlukast or MK-866. The efficacy of the combination containing Zileuton and Zafirlukast to prevent lung tumors is not significantly different from the efficacy of either inhibitor administered alone. Although when administered alone at the dose level in their combination, neither Zileuton or MK-886 prevents lung tumors; the combination containing them does significantly prevent tumors. In contrast, the combination containing Zafirlukast and MK-886 does not reduce the yield of tumors, whereas Zafirlukast administered alone does significantly reduce the yield of tumors[2].

References:
[1]. Finnerty JP, et al. Role of leukotrienes in exercise-induced asthma. Inhibitory effect of ICI 204219, a potent leukotriene D4 receptor antagonist. Am Rev Respir Dis. 1992 Apr;145(4 Pt 1):746-9.
[2]. Gunning WT, et al. Chemoprevention by lipoxygenase and leukotriene pathway inhibitors of vinyl carbamate-induced lung tumors in mice. Cancer Res. 2002 Aug 1;62(15):4199-201.

Chemical Properties

Cas No. 107753-78-6 SDF
Chemical Name cyclopentyl N-[3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methylindol-5-yl]carbamate
Canonical 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
Formula C31H33N3O6S M.Wt 575.68
Solubility ≥ 23.9mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.7371 mL 8.6854 mL 17.3708 mL
5 mM 0.3474 mL 1.7371 mL 3.4742 mL
10 mM 0.1737 mL 0.8685 mL 1.7371 mL
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 8 reference(s) in Google Scholar.)

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