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

Chemical Structure : Montelukast

CAS No.: 158966-92-8

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Montelukast (MK0476, MK-0476)

货号: PC-23319Not For Human Use, Lab Use Only.

Montelukast (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1) with Ki of 0.18 nM, 4 nM and 0.52 nM in guinea pig lung, sheep lung and U937 cell plasma membrane preparations respectively.

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

生物&药学活性

Montelukast (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1) with Ki of 0.18 nM, 4 nM and 0.52 nM in guinea pig lung, sheep lung and U937 cell plasma membrane preparations respectively.
Montelukast (MK0476) is inactive versus [3H]leukotriene C4 specific binding in dimethylsulfoxide-differentiated U937 cell membranes (IC50 10 microM) and [3H]leukotriene B4 specific binding in THP-1 cell membranes (IC50 40 microM).
Montelukast (MK0476) inhibited specific binding of [3H]leukotriene D4 to guinea pig lung in the presence of human serum albumin, human plasma, and squirrel monkey plasma with Ki values of 0.21, 0.19, and 0.26 nM, respectively.
Montelukast (MK0476) antagonized contractions of guinea pig trachea induced by leukotriene D4 (pA2 value 9.3; slope 0.8).
Montelukast (MK0476) blocked leukotriene D4 induced bronchoconstriction in conscious squirrel monkeys, ovalbumin-induced bronchoconstriction in conscious sensitized rats (ED50 0.03 mg/kg; 4 h pretreatment), and also ascaris-induced early and late phase bronchoconstriction in conscious squirrel monkeys (0.03-0.1 mg/kg; 4 h pretreatment).

物理化学性质&存储条件

分子量 586.19
分子式 C35H36ClNO3S
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

(R,E)-2-(1-(((1-(3-(2-(7-Chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propyl)thio)methyl)cyclopropyl)acetic acid

参考文献

1. Reiss TF, et al. Thorax. 1997 Jan;52(1):45-8.

2. Reiss TF, et al. Allergy Clin Immunol. 1996 Sep;98(3):528-34.

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