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Tipelukast

Names

[ CAS No. ]:
125961-82-2

[ Name ]:
Tipelukast

[Synonym ]:
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

Biological Activity

[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.


[Related Small Molecules]

MK-571 | Zafirlukast | Pranlukast | Nedocromil | AS-35 | LY223982 | Darbufelone mesilate | LM-1484 | Quinotolast sodium | RG-12525 | RS-601 | CI-949 | CP 105696 | CP-96486 | DW-1350

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
735.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C29H38O7S

[ Molecular Weight ]:
530.673

[ Flash Point ]:
398.5±32.9 °C

[ Exact Mass ]:
530.233826

[ PSA ]:
135.43000

[ LogP ]:
7.85

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.582

Related Compounds