Montelukast (MK0476 free base) 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 可用于研究预防哮喘和肝损伤。Montelukast 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 减少嗜酸性粒细胞浸润到哮喘气道。Montelukast 也可用于 COVID-19 的研究。
| 生物活性 | Montelukast (MK0476 free base) is a potent, selective and orally active antagonist ofcysteinylleukotriene receptor1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast decreases eosinophil infiltration into the asthmatic airways. Montelukast can also be used for COVID-19 research[1][2][3][4]. |
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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. |
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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. |
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| 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. |
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