Cinalukast

Names

[ Name ]:
Cinalukast

[Synonym ]:
Cinalukast
4-[3-[(E)-2-(4-cyclobutyl-1,3-thiazol-2-yl)ethenyl]anilino]-2,2-diethyl-4-oxobutanoic acid

Biological Activity

[Description]:

Ro 24-5913 (Cinalukast) is an orally active and potent LTD4 antagonist with an IC50 value of 6.4 nM. Ro 24-5913 can be used for the research of asthma[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor

Research Areas >> Inflammation/Immunology

[Target]

IC50: 6.4 nM (LTD4)[1]

[In Vitro]

Ro 24-5913 competes with [3H]LTD4 for its binding site in guinea pig lung membranes with an IC50 value of 6.4 nM[1]. Ro 24-5913 shows effective antagonist efficacy to LTD4-induced contractions with a pKB value of 9.3[1].

[In Vivo]

Ro 24-5913 (10 mg/kg i.v. and 100 mg/kg p.o.; once) inhibits LTD4-induced bronchoconstriction in guinea pigs with LD50s of 0.13 and 0.12 mg/kg for i.v. and p.o. respectively[1]. Animal Model: Guinea pigs[1] Dosage: 10 mg/kg Administration: Oral gavage; 10 mg/kg once Result: Inhibited LTD4-induced bronchoconstnction and antigen-induced bronchoconstnction in guinea pigs.

Chemical & Physical Properties

[ Density]:
1.258g/cm3

[ Molecular Formula ]:
C₂₃H₂₈N₂O₃S

[ Molecular Weight ]:
412.54500

[ Exact Mass ]:
412.18200

[ PSA ]:
107.53000

[ LogP ]:
5.87360

[ Index of Refraction ]:
1.655

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Participation of leukotriene C(4) in the regulation of suicidal erythrocyte death.

J. Physiol. Pharmacol. 60(3) , 135-43, (2009)

Eryptosis, the suicidal death of erythrocytes, is characterized by cell shrinkage and cell membrane scrambling with phosphatidylserine exposure at the erythrocyte surface. Eryptosis is triggered by in...

Prolonged protection against exercise-induced bronchoconstriction by the leukotriene D4-receptor antagonist cinalukast.

J. Allergy Clin. Immunol. 99(2) , 210-5, (1997)

The degree and duration of protection against exercise-induced bronchoconstriction afforded by three doses of a specific leukotriene D4 receptor antagonist, cinalukast, were assessed after an initial ...

Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma.

Biochem. Pharmacol. 44(7) , 1411-5, (1992)

We have identified and characterized two different subclasses of binding site for the novel peptido-leukotriene (LT) antagonist, [3H]ICI 198,615, in membranes from human lung parenchyma using a recept...