Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1.

Both Iralukast and CGP 57698 are able to compete for the two sites labelled by [3H]-LTD4. As in all the G-protein coupled receptors, Iralukast and CGP 57698 do not discriminate between the high and the low affinitystates of the CysLT receptor labelled by LTD4 (Ki1=Ki2=16.6 nM±36% CV and Ki1=Ki2=5.7 nM±19% CV, respectively). Iralukast, displays a slow bindingkinetic, because preincubation (15 min) increases its antagonist potency. Iralukast and CGP 57698 antagonize LTD4-induced contraction of humanbronchi, with pA2 values of 7.77±4.3% CV and 8.51±1.6% CV, respectively, and slopes not significantly different from unity[2].

151581-24-7

C38H37F3O8S

710.76

Iralukast (CGP 45715A)

DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years