Tipelukast(KCA757)是一种白三烯受体(leukotrienereceptor)拮抗剂，是一种可口服的抗炎剂，同时可用于哮喘治疗。
CAS：125961-82-2
分子式：C29H38O7S
分子量：530.67
纯度：98%
存储：Store at -20°C

Background:

Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.

Tipelukast inhibits the binding of [3H] LTD4 to the LTD4 receptors on pul-monary cell membrane of guinea-pigs (IC50 = 2.3 μmol)[2].

Fiftheen min after an aerosolized antigen challenge, and UNDW inhaled 5 min later into the guinea pigs, Tipelukast significantly alters the UNDW-induced bronchoconstriction[1]. Tipelukast (1 and 5 mg/kg) administered intravenously 15 min after antigen challenge reduces the propranolol-induced bronchoconstriction (PIB) in a dose-dependent manner in guinea-pigs[2].

[1]. Fujimura M, et al. No involvement of lipid mediators in a guinea pig model of ultrasonically nebulized distilled water-induced bronchoconstriction. Prostaglandins Other Lipid Mediat. 2000 Jan;60(1-3):49-58. [2]. Fujimura M, et al. Role of leukotrienes in post-allergic propranolol-induced bronchoconstriction in guinea-pigs. Clin Exp Allergy. 1997 Oct;27(10):1219-26.