125961-82-2

125961-82-2 structure

Name: Tipelukast
Chemical Name: 4-[6-acetyl-3-[3-(4-acetyl-3-hydroxy-2-propylphenyl)sulfanylpropoxy]-2-propylphenoxy]butanoic acid
CAS Number: 125961-82-2
Molecular Formula: C₂₉H₃₈O₇S
Molecular Weight: 530.673
Catalog: Signaling Pathways GPCR/G Protein Leukotriene Receptor
Create Date: 2018-11-23 20:41:41
Modify Date: 2024-01-15 06:37:05
Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.

Name	4-[6-acetyl-3-[3-(4-acetyl-3-hydroxy-2-propylphenyl)sulfanylpropoxy]-2-propylphenoxy]butanoic acid
Synonyms	MN-001 Butanoic acid,4-[6-acetyl-3-[3-[(4-acetyl-3-hydroxy-2-propylphenyl)thio]propoxy]-2-propylphenoxy] Tipelukast [USAN:INN] KCA 757 Tipelukast (USAN) 4-(6-acetyl-3-(3-(4-acetyl-3-hydroxy-2-propylphenylthio)propoxy)-2-propylphenoxy)butyric acid Tipelukast Butanoic acid, 4-[6-acetyl-3-[3-[(4-acetyl-3-hydroxy-2-propylphenyl)thio]propoxy]-2-propylphenoxy]- 4-(6-Acetyl-3-{3-[(4-acetyl-3-hydroxy-2-propylphenyl)sulfanyl]propoxy}-2-propylphenoxy)butanoic acid

Description	Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor Research Areas >> Inflammation/Immunology
Target	LTD4:6.41 (pA2, In guinea-pigs) LTE4:6.45 (pA2, In guinea-pigs)
In Vitro	Tipelukast inhibits the binding of [3H] LTD4 to the LTD4 receptors on pul-monary cell membrane of guinea-pigs (IC50 = 2.3 μmol)[2].
In Vivo	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].
References	[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.