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Montelukast Sodium

Catalog No.: GC11006Purity:>98%Synonyms: MK-476
몬테루카스트 나트륨(MK0476)은 시스테닐 류코트리엔 수용체 1(CysLT1)의 강력하고 선택적이며 경구 활성 길항제입니다.

제품은 연구용으로만 사용됩니다. 인체에 사용할 수 없으며 환자에게 판매하지 않습니다.


Montelukast Sodium
Cas No.: 151767-02-1
10mM (in 1mL Water)In Stock
$47.00
1
50mgIn Stock
$43.00
1
100mgIn Stock
$79.00
1
500mgIn Stock
$252.00
1

인용 문헌 (Citations)

현재 이 제품에 대한 인용 문헌이 없습니다. 아래는 GlpBio 제품을 인용한 주요 논문입니다.
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    632, 686–694 (2024)
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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    388(6745) (2025)
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제품 설명 (Description)

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.

실험 프로토콜 (Protocol)

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].

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].

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.

화학적 특성 (Chemical Properties)

CAS 번호
151767-02-1
동의어
MK-476
화학명
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
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+]
분자식
C35H35ClNNaO3S
분자량
608.17
용해도
≥ 28.7mg/mL in DMSO
보관
Store at -20°C, sealed storage, away from moisture
일반 주의사항
제품의 용해도 데이터에 따라 적절한 용매를 선택하십시오. 조제 후에는 반복적인 동결·해동을 피할 수 있도록 저장 용액을 소분하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
배송 조건
평가용 샘플은 아이스팩과 함께 배송됩니다. 그 외 용량은 실온 배송되며, 요청 시 아이스팩과 함께 배송할 수 있습니다.

계산 도구 (Calculators)몰 농도 / 희석 / 분자량 / 단위 변환 / 생체 내 제형 / 용해도

g/mol

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