Tipelukast

Product NameTipelukast
CAS125961-82-2
MFC29H38O7S
MW530.67282
EINECS
MOL File125961-82-2.mol

Chemical Properties

Melting point	82-84°C
Boiling point	735.3±60.0 °C(Predicted)
Density	1.22
storage temp.	Hygroscopic, Refrigerator, under inert atmosphere
solubility	Chloroform (Slightly), Ethyl Acetate (Slightly)
pka	4.59±0.10(Predicted)
form	Solid
color	Off-White to Pale Beige

Usage And Synthesis

Uses

Tipelukast a novel oral anti-inflammatory agent, suppresses bladder hyperactivity in a rat model.

Definition

ChEBI: Tipelukast is an aromatic ketone.

Biological Activity

Tipelukast is a Leukotriene D4 (LTD4) receptor antagonist and an inhibitor of 5-lipoxygenase (5-LO) and also phosphodiesterases PDE3 and PDE4. It has been found to have antifibrotic and anti-inflammatory activity. Tipelukast has been investigated as a possible treatment for nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH).

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].

IC 50

LTD₄: 6.41 (pA2, In guinea-pigs); LTE₄: 6.45 (pA2, In guinea-pigs)