Iralukast  (Synonyms: CGP 45715A)

Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pK_i 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 (K_i1=K_i2=16.6 nM±36% CV and K_i1=K_i2=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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

710.76

C₃₈H₃₇F₃O₈S

151581-24-7

O=C(C1=CC(C2=CC=C(S[C@H]([C@H](O)C3=CC=CC(C(F)(F)F)=C3)/C=C/C=C\CCCCOC4=CC=C(C(C)=O)C(O)=C4CCC)C=C2O1)=O)O

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Magnus Bäck, et al. Update on leukotriene, lipoxin and oxoeicosanoid receptors: IUPHAR Review 7. Br J Pharmacol. 2014 Aug; 171(15): 3551–3574.  [Content Brief]

  [2]. Valérie Capra, et al. Pharmacological characterization of the cysteinyl-leukotrieneantagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro.Br J Pharmacol. 1998 Feb; 123(3): 590–598.  [Content Brief]