Montelukast Sodium
(Synonyms: 孟鲁司特钠; MK0476) 目录号 : GC11006
A CysLT1 receptor antagonist
Cas No.:151767-02-1
Sample solution is provided at 25 µL, 10mM.
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Montelukast Sodium (MK-0476) is a selective, reversible antagonist of leukotriene receptor with the Ki values of 0.52nM in U937 cell [1].
Montelukast Sodium has been reported to inhibit leukotriene D4 receptor specific binding in U937 cell, guinea pig lung and sheep lung with the Ki values of 0.52nM, 0.18nM and 4nM, respectively. In addition, Montelukast Sodium has also shown the inhibitory effect with the IC50 of 10mM for leukotriene C3 in U937 cell membranes and 40mM for leukotriene B4 in THP-1 cell membranes. Apart from these, after oral treatment of Montelukast Sodium, it has been revealed to suppress leukotriene D4 receptor induced bronchoconstriction in conscious squirrel monkeys with ED50 value of 0.03±0.001mg/kg [1].
References:
[1] Jones TR1, Labelle M, Belley M, Champion E, Charette L, Evans J, Ford-Hutchinson AW, Gauthier JY, Lord A, Masson P, et al. Pharmacology of montelukast sodium (Singulair), a potent and selective leukotriene D4 receptor antagonist. Can J Physiol Pharmacol. 1995 Feb;73(2):191-201.
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Cell experiment: |
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]. |
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Animal experiment: |
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]. |
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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. |
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| Cas No. | 151767-02-1 | SDF | |
| 别名 | 孟鲁司特钠; MK0476 | ||
| 化学名 | sodium;2-[1-[[(1R)-1-[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl]sulfanylmethyl]cyclopropyl]acetate | ||
| Canonical SMILES | CC(C)(C1=CC=CC=C1CCC(C2=CC=CC(=C2)C=CC3=NC4=C(C=CC(=C4)Cl)C=C3)SCC5(CC5)CC(=O)[O-])O.[Na+] | ||
| 分子式 | C35H35ClNNaO3S | 分子量 | 608.17 |
| 溶解度 | ≥ 28.7mg/mL in DMSO | 储存条件 | Store at -20°C, sealed storage, away from moisture |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet