Montelukast sodium

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Montelukastodium (MK0476, MK-0476) 是一种有效的、选择性的、口服活性的白三烯 D4 受体 (LTD4) 拮抗剂，对豚鼠肺 LTD4 的 Ki 值为 0.18 nM。

Montelukast sodium (MK0476, MK-0476) is a potent, selective, orally active leukotriene D4 receptor (LTD4) antagonist with Ki of 0.18 nM for guinea pig lung LTD4; shows no significant affinity for leukotriene C4 and leukotriene B4 receptors; Montelukast sodium is a potent and competitive antagonist of leukotriene D4-induced contractions of non-tonal guinea-pig trachea with pA2 of 9.3; antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v. leukotriene D4, blocksleukotriene D4 induced bronchoconstriction in vivo.Allergy Approved(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.(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.

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. 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.

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. 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.

MK0476 | MK-0476

GPCR/G Protein

Leukotriene Receptor

CysLTR1

Inflammation/Immunology

Allergy

151767-02-1

608.2

C35H35ClNNaO3S

>98% (HPLC)

H2O: ≥ 70 mg/mL

CC(C)(C1=CC=CC=C1CC[C@H](C2=CC=CC(=C2)/C=C/C3=NC4=C(C=CC(=C4)Cl)C=C3)SCC5(CC5)CC(=O)[O-])O.[Na+]

Cyclopropaneacetic acid, 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]-, sodium salt (1:1)

(-20℃)

With Ice Pack

≥ 2 years