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Montelukast dicyclohexylamine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Montelukast dicyclohexylamine图片
CAS NO:577953-88-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
MK0476 dicyclohexylamine
产品介绍
Montelukast (MK0476) dicyclohexylamine 是一种有效的、选择性和具有口服活性的半胱氨酸白三烯受体 1 (CysLT1) 拮抗剂。Montelukast dicyclohexylamine 可用于研究预防哮喘和肝损伤。Montelukast dicyclohexylamine 在肠缺血-再灌注损伤中也具有抗氧化作用,还可以减少心脏损伤。Montelukast dicyclohexylamine 减少嗜酸性粒细胞浸润到哮喘气道。Montelukast dicyclohexylamine 也可用于 COVID-19 的研究。
生物活性

Montelukast (MK0476) dicyclohexylamine is a potent, selective and orally active antagonist ofcysteinylleukotriene receptor1 (CysLT1). Montelukast dicyclohexylamine can be used for the reseach of asthma and liver injury. Montelukast dicyclohexylamine also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast dicyclohexylamine decreases eosinophil infiltration into the asthmatic airways. Montelukast dicyclohexylamine can also be used for COVID-19 research[1][2][3][4].

IC50& Target

CysLT1

 

体外研究
(In Vitro)

Montelukast (5 μM; 1 h) inhibits APAP (Acetaminophen) (HY-66005)-induced cell damage[1].
Montelukast (0.01-10 μM; 30 min) diminishes the 5-oxo-ETE–induced cell migration and modulates the activation of the plasmin-plasminogen system[3].
Montelukast (10 μM; 18 h) modulates the activation of MMP-9[3].

Cell Migration Assay[3]

Cell Line:Eosinophils
Concentration:0.01-10 μM
Incubation Time:30 min
Result:Diminished the 5-oxo-ETE–induced cell migration.

Western Blot Analysis[3]

Cell Line:Eosinophils
Concentration:10 μM
Incubation Time:18 h
Result:Reduced the 5-oxo-ETE–boosted MMP-9 secretion.
体内研究
(In Vivo)

Montelukast (3 mg/kg; oral gavage) protects against APAP-induced hepatotoxicity in mice[1].
Montelukast (1 mg/kg; miniosmotic pump administration) reduces the airway remodeling changes observed in OVA-treated mice and blocks the actions of cysteinyl leukotrienes (LT) C4, D4, and E4 mediated by the CysLT1 receptor[2].
Montelukast (1 mg/kg; miniosmotic pump administration) reduces the elevated levels of IL-4 and IL-13 found in the BAL fluid of OVA-treated mice[2].

Animal Model:C57BL/6J mice (8-week-old; 22-25 g) are induced acute hepatic injury[1]
Dosage:3 mg/kg
Administration:Oral gavage 1 h after saline or APAP administration
Result:Decreased serum levels of alanine transaminase (ALT) and aspartate aminotransferase (AST), and alleviated liver damage.
Clinical Trial
分子量

767.50

Formula

C47H59ClN2O3S

CAS 号

577953-88-9

中文名称

孟鲁司特二环己基胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.