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扎鲁斯特 /Zafirlukast {[allProObj[0].p_purity_real_show]}

货号:A769198 同义名: 扎鲁司特 / ICI 204219

Zafirlukast is the first-approved LTR antagonist with anti-asthmatic and potential capsular contracture-preventing activities.

Zafirlukast 化学结构 CAS号:107753-78-6
Zafirlukast 化学结构
CAS号:107753-78-6
Zafirlukast 3D分子结构
CAS号:107753-78-6
Zafirlukast 化学结构 CAS号:107753-78-6
Zafirlukast 3D分子结构 CAS号:107753-78-6
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Zafirlukast 纯度/质量文件 产品仅供科研

货号:A769198 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 LTR 其他靶点 纯度
Montelukast Sodium 98%
MK571 98%
Zafirlukast 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Zafirlukast 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].

Zafirlukast 动物研究

Dose Rat: 40 mg/kg, 80 mg/kg[3] (p.o.)
Administration p.o.

Zafirlukast 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 <<

Zafirlukast 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.

Zafirlukast 实验方案

计算器
存储液制备 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

Zafirlukast 技术信息

CAS号107753-78-6
分子式C31H33N3O6S
分子量 575.675
别名 扎鲁司特 ;ICI 204219
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

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

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