CAS Number151767-02-1
SynonymsMontelukast SodiuM Hydrate; Montelukast sodium; Montelukast sodium salt; Montelukast monosodium salt; Singulair; Montelukast (sodium)
Molecular FormulaC35H35ClNNaO3S
Molecular Weight608.17
Purity98%
Boiling Point750.5ºC at 760mmHg
Melting Point115 °C(dec.)
Appearancewhite to tan
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 151767-02-1 |
| Catalog No. | 2A-9011498 |
| Chinese Name | 孟鲁司特钠 |
| Synonyms | Montelukast SodiuM Hydrate; Montelukast sodium; Montelukast sodium salt; Montelukast monosodium salt; Singulair; Montelukast (sodium) |
| Molecular Formula | C35H35ClNNaO3S |
| Molecular Weight | 608.17 |
| Purity | 98 |
| Boiling Point | 750.5ºC at 760mmHg |
| Melting Point | 115 °C(dec.) |
| Appearance | white to tan |
| Water Solubility | DMSO: ≥8mg/mL at 60°C |
| Storage Condition | -20°C Freezer, Under Inert Atmosphere |
| Application | Montelukast sodium is a potent, selective leukotriene receptor antagonist. |
| HTC | 2933499090 |
| SMILES | [Na+].S([C@H](CCc5c(cccc5)C(O)(C)C)c2cc(ccc2)\C=C\c3nc4c(cc3)ccc(c4)Cl)CC1(CC1)CC(=O)[O-] |
| InChI | 1S/C35H36ClNO3S.Na/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29;/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39);/q;+1/p-1/b15-10+;/t32-;/m1./s1 |
| InChI Key | LBFBRXGCXUHRJY-HKHDRNBDSA-M |
| NACRES Code | NA.24 |
| UNSPSC | 41116107 |
| MSDS | msds/11498_1_151767_02_1.pdf |
| Bioactivity | Montelukast sodium is a potent, selective CysLT1 receptor antagonist. Related Catalog Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor Research Areas >> Inflammation/Immunology Target CysLT1 Autophagy In Vitro Montelukast may contribute to the reduction of eosinophilic inflammation in upper-airway inflammatory diseases such as rhinitis and nasal polyposis. Montelukast has a significant inhibitory effect on FBS-induced GM-CSF, IL-6, and IL-8 secretion, but not sICAM-1, in nasal mucosa and polyp epithelial cells. Montelukast also shows an inhibitory effect (p<0.05) on ECM-induced eosinophil survival from both nasal mucosa and polyp epithelial cells[1]. In Vivo Montelukast significantly reduces mild, moderate, and part of severe exacerbations in chronic mild to moderate asthma, 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 during airway remodeling[3]. Blockade of CysLT1R by repeated treatment with montelukast (1 or 2 mg/kg, ig, 4 weeks) reduces Aβ1-42-induced CysLT1R expression and also suppresses Aβ1-42-induced increments of NF-κB p65, TNF-α, IL-1β and caspase-3 activation, and Bcl-2 downregulation in the hippocampus and cortex. Correspondingly, montelukast treatment significantly improves Aβ1-42-induced memory impairment in mice, but has little effect on normal mice[4]. Cell Assay Nasal mucosa and polyp epithelial cells are stimulated with fetal bovine serum (FBS) with or without MK for 24 hours, and cytokine concentrations in epithelial secretions are measured by ELISA. After incubating peripheral blood eosinophils with epithelial cell-conditioned media (ECM) with or without montelukast up to 3 days, eosinophil survival is assessed by Trypan blue dye exclusion[1]. Animal Admin Rats: Twenty four Sprague Dawley rats are randomLy divided into control group, asthma, and montelukast group. A rat model of asthma is induced by ovalbumin (OVA) inhalation. Normal saline is used instead of sensitizing solution and 1% OVA in the control group. Each rat in the montelukast group is given montelukast (15mg/kg) by gavage 2h before OVA inhalation. All rats are treated for 8 weeks[3]. Mice: Montelukast is dissolved in 0.5% sodium carboxymethyl cellulose (CMC-Na). Mice are randomLy assigned to 4 groups: (1) vehicle plus vehicle,(2) Aβ1-42 plus vehicle, (3) Aβ1-42 plus montelukast (1.0 mg/kg), (4) Aβ1-42 plus montelukast (2.0 mg/kg). The solutions are injected bilaterally into the cerebroventricles through the micropipette[4]. References [1]. Mullol J, 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 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, et al. Effect of montelukast on the expression of neurokinin-1 receptor in young asthmatic rats with airway remodeling. Zhongguo Dang Dai Er Ke Za Zhi. 2013 Apr;15(4):298-301. [4]. Lai J, et al. Montelukast targeting the cysteinyl leukotriene receptor 1 ameliorates Aβ1-42-induced memory impairment and neuroinflammatory and apoptotic responses in mice. Neuropharmacology. 2014 Apr;79:707-14. Chemical & Physical Properties Boiling Point 750.5ºC at 760mmHg Melting Point 115 °C(dec.) Molecular Formula C35H35ClNNaO3S Molecular Weight 608.165 Flash Point 407.7ºC Exact Mass 607.192383 PSA 98.55000 LogP 7.61330 Appearance of Characters white to tan InChIKey LBFBRXGCXUHRJY-HKHDRNBDSA-M SMILES CC(C)(O)c1ccccc1CCC(SCC1(CC(=O)[O-])CC1)c1cccc(C=Cc2ccc3ccc(Cl)cc3n2)c1.[Na+] Storage condition -20°C Freezer, Under Inert Atmosphere Water Solubility DMSO: ≥8mg/mL at 60°C |
| Use of | Montelukast sodium is a potent, selective CysLT1 receptor antagonist. Properties Articles38 Name Montelukast sodium Synonym More Synonyms Montelukast sodium Biological Activity Description Montelukast sodium is a potent, selective CysLT1 receptor antagonist. Related Catalog Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor Research Areas >> Inflammation/Immunology In Vitro Montelukast may contribute to the reduction of eosinophilic inflammation in upper-airway inflammatory diseases such as rhinitis and nasal polyposis. Montelukast has a significant inhibitory effect on FBS-induced GM-CSF, IL-6, and IL-8 secretion, but not sICAM-1, in nasal mucosa and polyp epithelial cells. Montelukast also shows an inhibitory effect (p<0.05) on ECM-induced eosinophil survival from both nasal mucosa and polyp epithelial cells[1]. Cell Assay Nasal mucosa and polyp epithelial cells are stimulated with fetal bovine serum (FBS) with or without MK for 24 hours, and cytokine concentrations in epithelial secretions are measured by ELISA. After incubating peripheral blood eosinophils with epithelial cell-conditioned media (ECM) with or without montelukast up to 3 days, eosinophil survival is assessed by Trypan blue dye exclusion[1]. References [1]. Mullol J, 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 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, et al. Effect of montelukast on the expression of neurokinin-1 receptor in young asthmatic rats with airway remodeling. Zhongguo Dang Dai Er Ke Za Zhi. 2013 Apr;15(4):298-301. [4]. Lai J, et al. Montelukast targeting the cysteinyl leukotriene receptor 1 ameliorates Aβ1-42-induced memory impairment and neuroinflammatory and apoptotic responses in mice. Neuropharmacology. 2014 Apr;79:707-14. Chemical & Physical Properties Exact Mass 607.192383 PSA 98.55000 LogP 7.61330 Appearance of Characters white to tan InChIKey LBFBRXGCXUHRJY-HKHDRNBDSA-M |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Summary 2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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