GSK2190915

GSK2190915 is a selective inhibitor of human 5-lipoxygenase-activating protein (FLAP; IC₅₀ = 2.9 nM).¹ It is selective for FLAP over 5-, 12-, and 15-lipoxygenase, leukotriene A₄ (LTA₄) hydrolase, LTC₄ synthase, COX-1, and COX-2 (IC₅₀s = >10 µm for all). GSK2190915 inhibits production of LTB₄ induced by the calcium ionophore A23187 (Item No. 11016) in isolated whole blood from human, rat, and mouse (IC₅₀s = 436, 223, and 148 nM, respectively). It decreases increases in the levels of cysteinyl leukotriene (CysLT) and LTB₄ induced by lung instillation of A23187 in the bronchoalveolar lavage fluid (BALF) of rats when administered at doses of 1 and 3 mg/kg. GSK219095 (3 mg/kg) also reduces increases in the levels of CysLT, LTB₄, myeloperoxidase (MPO), and plasma protein extravasation in a mouse model of peritonitis induced by zymosan in mice.

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1. Lorrain, D.S., Bain, G., Correa, L.D., et al. Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation. Eur. J. Pharmacol. 640(1-3), 211-218 (2010).