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首页-小分子抑制剂&激动剂-GPCR-Leukotriene Receptor-Zafirlukast
Zafirlukast

Chemical Structure : Zafirlukast

CAS No.: 107753-78-6

Zafirlukast (ICI-204219, ICI 204219)

货号: PC-45294Not For Human Use, Lab Use Only.

Zafirlukast (ICI-204219) is a potent, selective, orally active cysteinyl leukotriene 1 (CysLT1) receptor antagonist with IC50 of 14 nM in cell-based calcium mobilization assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Zafirlukast (ICI-204219) is a potent, selective, orally active cysteinyl leukotriene 1 (CysLT1) receptor antagonist with IC50 of 14 nM in cell-based calcium mobilization assays.
Zafirlukast is selective for CysLT1 over CysLT2 receptors (IC50=58 uM).
Zafirlukast inhibits mucus secretion induced by leukotriene D4 (LTD4) in isolated guinea pig trachea (IC50=0.6 μM).
Zafirlukast (5 μM) inhibits ovalbumin-induced increases in tracheal mucus secretion in ovalbumin-sensitized guinea pigs by 65%.
Zafirlukast inhibits LTD4-induced bronchoconstriction in anesthetized guinea pigs (ED50 = 61 nmol/kg, i.v.).

物理化学性质&存储条件

分子量 575.6752
分子式 C31H33N3O6S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Carbamic acid, N-[3-[[2-methoxy-4-[[[(2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]-, cyclopentyl ester

参考文献

1. Buckner CK, et al. J Pharmacol Exp Ther. 1990 Jan;252(1):77-85.

2. Spector SL, et al. Am J Respir Crit Care Med. 1994 Sep;150(3):618-23.

3. Kidney JC, et al. Am Rev Respir Dis. 1993 Jan;147(1):215-7.

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