产品说明书

Montelukast Sodium

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Chemical Structure| 151767-02-1 同义名 : 孟鲁司特钠 水合物 ;MK0476;Montelukast (sodium salt);MK-476
CAS号 : 151767-02-1
货号 : A232574
分子式 : C35H35ClNNaO3S
纯度 : 98%
分子量 : 608.165
MDL号 : MFCD00931431
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(82.21 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(82.21 mM)
动物实验配方：

PO 0.5% CMC-Na 17 mg/mL suspension

生物活性
靶点

  • LTR
描述 Cysteinyl leukotrienes (CysLTs, including LTC4, LTD4, and LTE4), mainly produced by eosinophils, mast cells, and macrophages in response to a variety of stimuli activating arachidonate 5-lipoxygenase pathway, are important inflammatory mediators. CysLT1 receptor (LTR1) expresses in human lung smooth muscle cells, lung macrophages, most peripheral blood eosinophils and pregranulocytic CD34+ cells, and in subsets of monocytes and B lymphocytes. Montelukast Sodium is a potent, selective and competitive LTR1 antagonist with IC50 value < 5 nM and are currently used in the treatment of asthma. Nonsmoking patients with asthma treated with Montelukast Sodium(200mg, three times daily for 10 1/3 days) showed improvements in FEV1, compared with placebo-treated patients[5]. In C57BL/6 mice with asthma induced by chronic exposure to ovalbumin, Montelukast (6 mg/kg, once daily for 20 days) treatment significantly suppressed the increased eosinophils in bronchoalveolar lavage (BAL) fluid and lung tissue, and increased IL-5 level in BAL fluid in models[6]. It was also proved that Montelukast inhibited the diabetes-induced capillary and neuronal degeneration in streptozotocin-induced diabetes mouse model[7].
作用机制 Montelukast Sodium is a potent competing ligand for high affinity [3H]LTD4 specific binding.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02110654 Sinusitis Nas... 展开 >>al Polyps Asthma 收起 << Phase 4 Unknown June 2016 China, Guangdong ... 展开 >> the first affiliated hospital, Sun Yat-sen University Not yet recruiting Guangzhou, Guangdong, China, 510080 Contact: Fenghong Chen, doctor    02086013560170816    chfhong@mail.sysu.edu.cn    Principal Investigator: jianbo Shi, doctor 收起 <<
NCT00504946 Asthma Phase 3 Completed - Poland ... 展开 >> Department of Pediatrics and Allergy, Medical University of Lodz Lodz, Poland Lodz, Poland, 93-513 收起 <<
NCT00398151 Asthma Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.64mL

0.33mL

0.16mL

8.22mL

1.64mL

0.82mL

16.44mL

3.29mL

1.64mL
参考文献

[1]Mullol J, Callejas FB, et al. Montelukast reduces eosinophilic inflammation by inhibiting both epithelial cell cytokine secretion (GM-CSF, IL-6, IL-8) and eosinophil survival. J Biol Regul Homeost Agents. 2010 Oct-Dec;24(4):403-11.

[2]Zhang YJ, Zhang L, et al. Montelukast modulates lung CysLT(1) receptor expression and eosinophilic inflammation in asthmatic mice. Acta Pharmacol Sin. 2004 Oct;25(10):1341-6.

[3]Wu S, Zhu X, et al. The protective role of montelukast against intestinal ischemia-reperfusion injury in rats. Sci Rep. 2015 Oct 26;5:15787.

[4]Montelukast

[5]Reiss TF, Altman LC, Chervinsky P, Bewtra A, Stricker WE, Noonan GP, Kundu S, Zhang J. Effects of montelukast (MK-0476), a new potent cysteinyl leukotriene (LTD4) receptor antagonist, in patients with chronic asthma. J Allergy Clin Immunol. 1996 Sep;98(3):528-34. doi: 10.1016/s0091-6749(96)70086-6. PMID: 8828530.

[6]Zhang YJ, Zhang L, Wang SB, Shen HH, Wei EQ. Montelukast modulates lung CysLT(1) receptor expression and eosinophilic inflammation in asthmatic mice. Acta Pharmacol Sin. 2004 Oct;25(10):1341-6. PMID: 15456537.

[7]Bapputty R, Talahalli R, Zarini S, Samuels I, Murphy R, Gubitosi-Klug R. Montelukast Prevents Early Diabetic Retinopathy in Mice. Diabetes. 2019 Oct;68(10):2004-2015. doi: 10.2337/db19-0026. Epub 2019 Jul 26. PMID: 31350303; PMCID: PMC6754245.