Montelukast-sodium-MK0476-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMontelukast sodiumCat. No.: HY-13315CAS No.: 151767-02-1Synonyms: MK0476分式: CHClNNaOS分量: 608.17作靶点: Leukotriene Receptor; Autophagy作通路: GPCR/G Protein; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mo

2、nth溶解性数据体外实验 H2O : 70 mg/mL (115.10 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.6443 mL 8.2214 mL 16.4428 mL5 mM 0.3289 mL 1.6443 mL 3.2886 mL10 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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Mont

3、elukast (sodium) (MK0476)有效，选择性的三烯受体受体拮抗剂。IC50 & Target CysLT1 Autophagy体外研究Montelukast may contribute to the reduction of eosinophilic inflammation in upper-airway inflammatory1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEdiseases such as rhinitis and nasal polyposis. Montelukast has a significa

4、nt inhibitory effect on FBS-inducedGM-CSF, IL-6, and IL-8 secretion, but not sICAM-1, in nasal mucosa and polyp epithelial cells. Montelukastalso shows an inhibitory effect (p 1.体内研究 Montelukast significantly reduces mild, moderate, and part of severe exacerbations in chronic mild tomoderate asthma,

5、 but it has inferior efficacy to ICS or ICS plus LABA 2. Rats with induced asthma have up-regulated NK1R expression in the airway, and montelukast can down regulate NK1R expression duringairway remodeling 3. Blockade of CysLT1R by repeated treatment with montelukast (1 or 2 mg/kg, ig, 4weeks) reduce

6、s A1-42-induced CysLT1R expression and also suppresses A1-42-induced increments ofNF-B p65, TNF-, IL-1 and caspase-3 activation, and Bcl-2 downregulation in the hippocampus andcortex. Correspondingly, montelukast treatment significantly improves A1-42-induced memory impairment inmice, but has little

7、 effect on normal mice 4.PROTOCOLCell Assay 1 Nasal mucosa and polyp epithelial cells are stimulated with fetal bovine serum (FBS) with or without MK for24 hours, and cytokine concentrations in epithelial secretions are measured by ELISA. After incubatingperipheral blood eosinophils with epithelial

8、cell-conditioned media (ECM) with or without montelukast up to 3days, eosinophil survival is assessed by Trypan blue dye exclusion 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: Twenty four Sprague Dawley rats are randomLy divided into c

9、ontrol group, asthma, and montelukastAdministration 34 group. A rat model of asthma is induced by ovalbumin (OVA) inhalation. Normal saline is used instead ofsensitizing solution and 1% OVA in the control group. Each rat in the montelukast group is given montelukast(15mg/kg) by gavage 2h before OVA

10、inhalation. All rats are treated for 8 weeks 3.Mice: Montelukast is dissolved in 0.5% sodium carboxymethyl cellulose (CMC-Na). Mice are randomLyassigned to 4 groups: (1) vehicle plus vehicle,(2) A1-42 plus vehicle, (3) A1-42 plus montelukast (1.0mg/kg), (4) A1-42 plus montelukast (2.0 mg/kg). The so

11、lutions are injected bilaterally into thecerebroventricles through the micropipette 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Mullol J, et al. Montelukast?reduces eosinophilic inflammation by inhibiting both epithelial cell cytokine

12、 secretion (GM-CSF, IL-6, IL-8)and eosinophil survival. J Biol Regul Homeost Agents.?2010 Oct-Dec;24(4):403-11.2. Zhang HP, et al. Montelukast for prevention and treatment of asthma exacerbations in adults: Systematic review and meta-analysis.Allergy Asthma Proc. 2014 Jul-Aug;35(4):278-87.3. Wei B,

13、et al. Effect of montelukast on the expression of neurokinin-1 receptor in young asthmatic rats with airway remodeling. ZhongguoDang Dai Er Ke Za Zhi. 2013 Apr;15(4):298-301.4. Lai J, et al. Montelukast targeting the cysteinyl leukotriene receptor 1 ameliorates A1-42-induced memory impairment andneuroinflammatory and apoptotic responses in mice. Neuropharmacology. 2014 Apr;79:707-14.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师