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CAS No.: 107753-78-6

扎鲁斯特 Catalog No. CSN12622

Synonyms: ICI 204219;ICI-204,219;brand names Accolate

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

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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].
动物研究
剂量
Rat: 40 mg/kg, 80 mg/kg^[3] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Rat: 40 mg/kg, 80 mg/kg^[3] (p.o.)
给药途径	p.o.

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 ... more >> BA Research India Ltd. Ahmedabad, Bodakdev, India, 380 054 Collapse <<

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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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7371 mL
- 8.6855 mL
- 17.3709 mL
- 5 mM
- 0.3474 mL
- 1.7371 mL
- 3.4742 mL
- 10 mM
- 0.1737 mL
- 0.8685 mL
- 1.7371 mL

技术信息

CAS号

107753-78-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H33N3O6S

运输

蓝冰

分子量

575.68

别名

ICI 204219;ICI-204,219;brand names Accolate;Accoleit;and Vanticon;扎鲁司特

溶解度

DMSO	430.0 mg/mL (746.9 mM) warming
Water	insoluble

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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NCT01125748	Allergic Asthma	Phase 4	Completed	-	-
NCT01125748	-	-	Completed	-	-
NCT01283061	Healthy	Phase 1	Completed	-	India ... more >> BA Research India Ltd. Ahmedabad, Bodakdev, India, 380 054 Collapse <<
NCT02950480	Breast Cancer	Phase 2	Recruiting	January 2020	United States, California ... more >> UCSF Helen Diller Family Comprehensive Cancer Center Recruiting San Francisco, California, United States, 94143-1711 Contact: Pamela N. Munster, MD 877-827-3222 cancertrials@ucsf.edu Collapse <<

扎鲁斯特 Catalog No. CSN12622

靶点选择性

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