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Montelukast Sodium.

白三烯受体拮抗剂,Montelukast sodium是有效，选择性的白三烯受体受体拮抗剂。

目录号: PC10743 纯度: ≥98%

CAS No. :151767-02-1

商品编号	规格	价格	会员价
PC10743-100mg	100mg	¥1136.80	请登录
PC10743-250mg	250mg	¥1675.80	请登录
PC10743-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥490.00	请登录

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中文名称	Montelukast Sodium.
中文别名	孟鲁司特钠;马尼地平;马尼地平盐酸盐;孟鲁斯特钠;孟鲁司特钠水合物;Montelukast Sodium Hydrate 孟鲁司特钠水合物;夫西地酸;孟鲁司特-D6钠;孟鲁司特峰鉴别 EP标准品;孟鲁司特钠 EP标准品;孟鲁司特钠 USP标准品;孟鲁司特钠标准品;孟鲁司特钠技术转让;孟鲁司特钠(治哮喘);孟鲁司特钠盐;孟鲁司特钠原药;孟鲁司特钠杂质对照品;孟鲁斯特纳;孟鲁斯特钠标准品;[R-(E)]-1-[[[1-[3-[2-(7-氯-2-喹啉)乙烯基]苯基-3-[2-(1-羟基-1-甲基乙基)苯基]丙基]硫]甲基]环丙烷乙酸钠;孟鲁司特钠对照品;孟鲁斯特钠,用于鉴定;孟钠;盂鲁司特钠;孟鲁司特纳;孟卤司特钠;孟鲁司特D6;孟鲁司特杂质K
英文名称	Montelukast Sodium
英文别名	Montelukast Sodium;2-[1-[[1-[3-[2-[(7-chloro-2-quinolyl)]vinyl]phenyl]-3-[2-(1-hydroxy-1-methyl-ethyl)phenyl]-propyl]sulfanylmethyl]cyclopropyl]acetic acid sodium salt;singulair;mk-476;Montelukast Sodium Hydrate;Montelukast (sodium salt);Montelukast Sodium S;Montelukast Sodium Salt;Sodium (R,E)-2-(1-(((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propyl)thio)methyl)cyclopropyl)acetate;sodium (R,S)-2-(1-(((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propyl)thio)methyl)cyclopropyl)acetate;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;MK-0476;MK-476-d6;MONTELUKAST NA;montelucast-d6;MK-476, Singulair;Motelukast SodiuM;MONTELUKST SODIUM
Cas No.	151767-02-1
分子式	C₃₅H₃₅ClNNaO₃S
分子量	608.17
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Montelukast sodium (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (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.

性状

Solid

IC50 & Target[1][2]

CysLT₁

体外研究(In Vitro)

Montelukast (5 μM; 1 h) inhibits APAP (Acetaminophen) (HY-66005)-induced cell damage.
Montelukast (0.01-10 μM; 30 min) diminishes the 5-oxo-ETE–induced cell migration and modulates the activation of the plasmin-plasminogen system.
Montelukast (10 μM; 18 h) modulates the activation of MMP-9.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay

Cell Line:	Eosinophils
Concentration:	0.01-10 μM
Incubation Time:	30 min
Result:	Diminished the 5-oxo-ETE–induced cell migration.

Western Blot Analysis

Cell Line:	Eosinophils
Concentration:	10 μM
Incubation Time:	18 h
Result:	Reduced the 5-oxo-ETE–boosted MMP-9 secretion.

体内研究(In Vivo)

Montelukast (3 mg/kg; oral gavage) protects against APAP-induced hepatotoxicity in mice.
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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6J mice (8-week-old; 22-25 g) are induced acute hepatic injury
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.

运输条件

Room temperature or refrigerated transportation.

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)

ClinicalTrial

参考文献

[1]. Pu S, et, al. Montelukast Prevents Mice Against Acetaminophen-Induced Liver Injury. Front Pharmacol. 2019 Sep 18; 10:1070. [Information]

[2]. William RHJ, et, al. A role for cysteinyl leukotrienes in airway remodeling in a mouse asthma model. Am J Respir Crit Care Med. 2002 Jan 1; 165(1): 108-16. [Information]

[3]. Langlois A, et al. Montelukast regulates eosinophil protease activity through a leukotriene-independent mechanism. J Allergy Clin Immunol. 2006;118(1):113-119. [Information]

[4]. Khan AR, et al. Montelukast in hospitalized patients diagnosed with COVID-19. J Asthma. 2022 Apr;59(4):780-786. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (82.21 mM; Need ultrasonic)

H₂O : ≥ 50 mg/mL (82.21 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 1.25 mg/mL (2.06 mM); Suspended solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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