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.
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产品名称 | LTR ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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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。 |
靶点 |
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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]. |
Dose | Rat: 40 mg/kg, 80 mg/kg[3] (p.o.) |
Administration | 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 ... 展开 >> BA Research India Ltd. Ahmedabad, Bodakdev, India, 380 054 收起 << |
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 |
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 |