1159576-98-3

5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs) from arachidonic acid, primarily in certain leukocyte populations. CAY10606 is a potent, reversible inhibitor of 5-LO, both in cell-free assays (IC₅₀ = 86 nM) and in intact neutrophils (IC₅₀ = 230 nM).¹ It prevents the production of LTs in whole blood, whether 5-LO is activated with the calcium ionophore A23187 (IC₅₀ = 1.6 μM) or formyl peptide (fMLP) following priming with lipopolysaccharide (IC₅₀ = 830 nM). In rats subjected to carrageenan-induced pleurisy, CAY10606 significantly reduces both LT biosynthesis and the inflammatory reaction.¹

5-LOX-IN-6 (compound 11a) is a direct and reversible inhibitor of 5-lipoxygenase (5-LO). 5-LOX-IN-6 inhibits 5-LO activity in human neutrophils and recombinant human 5-LO with IC50 values of 0.23 and 0.086 μM, respectively. 5-LOX-IN-6 prevents leukotriene biosynthesis. 5-LOX-IN-6 can be used for inflammatory and allergic disorders research[1].

5-LO; LTB₄

Store at -20°C

1. Karg, E.M., Luderer, S., Pergola, C., et al. Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase J. Med. Chem. 52,3474-3483(2009).