Zafirlukast|107753-78-6|安捷凯

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].

参考文献:
[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.

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.

参考文献:

[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.

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信号通路

生命科学

有机化学

无机化学

材料科学

Zafirlukast

Zafirlukast详情

Background

Protocol

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