Tipelukast

Modify Date: 2024-01-15 06:37:05

Tipelukast Structure
Tipelukast structure
Common Name Tipelukast
CAS Number 125961-82-2 Molecular Weight 530.673
Density 1.2±0.1 g/cm3 Boiling Point 735.3±60.0 °C at 760 mmHg
Molecular Formula C29H38O7S Melting Point N/A
MSDS N/A Flash Point 398.5±32.9 °C

 Use of Tipelukast


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

 Names

Name 4-[6-acetyl-3-[3-(4-acetyl-3-hydroxy-2-propylphenyl)sulfanylpropoxy]-2-propylphenoxy]butanoic acid
Synonym More Synonyms

 Tipelukast 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
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.

 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

 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
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