CAY10606

Description

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

References

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).