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Zafirlukast

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Chemical Structure| 107753-78-6 同义名 : 扎鲁司特 ;ICI 204219
CAS号 : 107753-78-6
货号 : A769198
分子式 : C31H33N3O6S
纯度 : 99%
分子量 : 575.675
MDL号 : MFCD00864775
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(182.39 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 3 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

生物活性
靶点

  • LTR
描述 Cysteinyl leukotrienes (CysLTs, including LTC4, LTD4, and LTE4) are important inflammatory mediators implicated in pathogenesisi of asthma. Zafirlukast (Accolate) is the first-approved LTD4 and LTE4 receptor antagonist which is used clinically to treat mild to moderate asthma. A single oral 40 mg dose of Zafirlukast treatment before subjects were challenged with aerosolized allergen significantly attentuated the early and late phase bronchoconstriction to inhaled allergen and suppressed the allergen-induced increase in non-specific bronchial reactivity[3]. MIN6 cells treated with zafirlukast for 1 h showed increased insulin secretion in a concentration-dependent manner in both low and high glucose conditions[4]. The glucose-lowering effect of zafirlukast (0.1 mg/g) was also observed in mice at 90 and 120 min during an intraperitoneal glucose tolerance test, with 29.3 ± 7.9% reduction for 90 min and 46.7 ± 6.6% reduction for 120 min, respectively[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01125748 Allergic Asthma Phase 4 Completed - -
NCT01125748 - Completed - -
NCT01283061 Healthy Phase 1 Completed - India ... 展开 >> BA Research India Ltd. Ahmedabad, Bodakdev, India, 380 054 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.69mL

1.74mL

0.87mL

17.37mL

3.47mL

1.74mL
参考文献

[1]Kassahun K, Skordos K, et al. 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]Senter DA, Scott DW, et al. Treatment of canine atopic dermatitis with zafirlukast, a leukotriene-receptor antagonist: a single-blinded, placebo-controlled study. Can Vet J. 2002 Mar;43(3):203-6.

[3]Taylor IK, O'Shaughnessy KM, Fuller RW, Dollery CT. Effect of cysteinyl-leukotriene receptor antagonist ICI 204.219 on allergen-induced bronchoconstriction and airway hyperreactivity in atopic subjects. Lancet. 1991 Mar 23;337(8743):690-4. doi: 10.1016/0140-6736(91)90277-v. PMID: 1672176.

[4]Hwang HJ, Park KS, Choi JH, Cocco L, Jang HJ, Suh PG. Zafirlukast promotes insulin secretion by increasing calcium influx through L-type calcium channels. J Cell Physiol. 2018 Nov;233(11):8701-8710. doi: 10.1002/jcp.26750. Epub 2018 May 24. PMID: 29797580.