Montelukast (MK0476 free base) 是半胱氨酰白三烯受体 1 (CysLT1) 的有效、选择性和口服活性拮抗剂。
货号:ajcx28390
CAS:158966-92-8
分子式:C35H36ClNO3S
分子量：586.2
溶解度:DMF: 2 mg/ml,DMSO: 2 mg/ml,Ethanol: insol,PBS (pH 7.2): insol
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Montelukast is a cysteinyl leukotriene 1 (CysLT₁) receptor antagonist (IC₅₀= 4.9 nM in HEK293 cell membranes expressing the human receptor).¹It is selective for CysLT₁over CysLT₂receptors (IC₅₀= >10,000 nM in COS-7 cell membranes expressing the human receptor).²Montelukast inhibits bronchoconstriction induced by leukotriene D₄in anesthetized guinea pigs (ED₅₀= 69 nmol/kg, p.o.).³It inhibits ovalbumin-induced airway hyperresponsiveness and increases in the number of total cells and eosinophils in bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma when administered at doses of 3 and 10 mg/kg.⁴Formulations containing montelukast have been used in the treatment of asthma, allergic rhinitis, and exercise-induced bronchoconstriction.

1.Sarau, H.M., Ames, R.S., Chambers, J., et al.Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptorMol. Pharmacol.56(3)657-663(1999) 2.Heise, C.E., O’Dowd, B.F., Figueroa, D.J., et al.Characterization of the human cysteinyl leukotriene 2 receptorJ. Biol. Chem.275(39)30531-30536(2000) 3.CabrÉ, F., Carabaza, A., GarcÍa, A.M., et al.Pharmacological profile of MEN91507, a new CysLT1 receptor antagonistEur. J. Pharmacol.451(3)317-326(2002) 4.Eum, S.Y., Maghni, K., Hamid, Q., et al.Involvement of the cysteinyl-leukotrienes in allergen-induced airway eosinophilia and hyperresponsiveness in the mouseAm. J. Respir. Cell Mol. Biol.28(1)25-32(2003)