Montelukast sodium (MK0476) 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 sodium 可用于研究预防哮喘和肝损伤。Montelukast sodium 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 sodium 减少嗜酸性粒细胞浸润到哮喘气道。Montelukast sodium 也可用于 COVID-19 的研究。
| 生物活性 | Montelukast sodium (MK0476) is a potent, selective and orally active antagonist ofcysteinylleukotriene receptor1 (CysLT1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast sodium decreases eosinophil infiltration into the asthmatic airways. Montelukast sodium 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 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(82.21 mM;Need ultrasonic) H2O : ≥ 50 mg/mL(82.21 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.6443 mL | 8.2214 mL | 16.4428 mL | | 5 mM | 0.3289 mL | 1.6443 mL | 3.2886 mL | | 10 mM | 0.1644 mL | 0.8221 mL | 1.6443 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 1.25 mg/mL (2.06 mM); Suspended solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
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