Tipelukast  (Synonyms: KCA 757; MN 001)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

530.67

C₂₉H₃₈O₇S

125961-82-2

Solid

White to off-white

CC(C1=C(O)C(CCC)=C(SCCCOC2=C(CCC)C(OCCCC(O)=O)=C(C(C)=O)C=C2)C=C1)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [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.  [Content Brief]