Montelukast Sodium

別名: MK0476 中文名稱：孟魯司特鈉

目錄號(hào)：S4211 Purity: 99.86%

Montelukast Sodium選擇性拮抗leukotriene D₄ (LTD₄)，通過結(jié)合到Cysteinyl leukotriene受體CysLT1，從而抑制Leukotriene D4。Montelukast 可促進(jìn)大自噬 macroautophagy 而非伴侶分子介導(dǎo)的自噬途徑。在溶液中不穩(wěn)定，請現(xiàn)配現(xiàn)用！

Montelukast Sodium Chemical Structure

CAS: 151767-02-1

規(guī)格	價(jià)格	庫存
50mg	799.28	現(xiàn)貨
1g	5487.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.86%

99.86

Montelukast Sodium相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	LTB4	點(diǎn)擊展開
相關(guān)產(chǎn)品	MK571 MK-571 sodium salt	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫 FDA藥物庫天然產(chǎn)物庫已知活性藥物庫-I 高選擇性抑制劑庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)信息
HEK293	Function assay	10 mins	Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay, IC50=0.31μM	26985325
HEK293	Function assay	10 mins	Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay, IC50=27μM	26985325
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生物活性

產(chǎn)品描述

靶點(diǎn)

CysLT1 ^[1]

體外研究(In Vitro)
體外研究活性	Montelukast是一種白三烯受體拮抗劑（LTRA），用于哮喘的持續(xù)治療以及緩解季節(jié)性過敏癥狀。Montelukast通過與肺部和支氣管中半胱氨酰白三烯受體CysLT1結(jié)合而阻斷白三烯D4的作用，防止氣道水腫，平滑肌收縮，以及分泌液粘稠。這減少了由白三烯引起的支氣管收縮，并且使炎癥較少發(fā)生。 ^[1]

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Montelukast (6 mg/kg, 每天一次，服用20天)顯著抑制OVA激發(fā)的小鼠體內(nèi)BAL液和肺組織中增多的嗜酸細(xì)胞，并且增加BAL液中IL-5水平。 OVA激發(fā)會(huì)增加CysLT1S受體但會(huì)減少CysLT2受體的mRNA表達(dá)。OVA激發(fā)后，Montelukast抑制增加的CysLT1但不降低CysLT2表達(dá)。 ^[2]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06340984	Not yet recruiting	Acne Vulgaris	South Valley University	June 2024	Phase 3
NCT04351698	Recruiting	Anemia Sickle Cell\|Sleep-Disordered Breathing	Great Ormond Street Hospital for Children NHS Foundation Trust\|Guy''s and St Thomas'' NHS Foundation Trust\|University College London Hospitals\|North Middlesex University Hospital\|King''s College Hospital NHS Trust\|The Whittington Hospital NHS Trust	October 16 2023	Phase 2\|Phase 3
NCT05651750	Unknown status	To Evaluate PSQ as Clinical Tool in the Decision Between Medical and Surgical Treatment for Adenotonsillar Hypertrophy\|To Determine Clinical Response to Montelukast or Nasal Steroids Based on PSQ Results	Assaf-Harofeh Medical Center	November 15 2022	Phase 4
NCT05064631	Recruiting	Respiratory Tract Infections\|Pediatric Respiratory Diseases\|Wheezing	Queen Mary University of London\|Queensland University of Technology	January 12 2022	Phase 2
NCT05710081	Recruiting	Wheezing\|Bronchiolitis\|Asthma in Children	Barts & The London NHS Trust\|University of Aberdeen\|University of Edinburgh\|King''s College London\|University of Southampton\|Menzies School of Health Research	November 30 2021	Phase 3

參考文獻(xiàn)
[1] Montelukast [2] Zhang YJ, et al. Acta Pharmacol Sin, 2004, 25(10), 1341-1346

參考文獻(xiàn)

[1] Montelukast
[2] Zhang YJ, et al. Acta Pharmacol Sin, 2004, 25(10), 1341-1346