CJ-13610 is an inhibitor of 5-lipoxygenase (5-LO) that inhibits 5-LO product formation in human polymorphonuclear leukocytes (PMNLs) challenged with A23187 in vitro (IC50 = 70 nM). It inhibits recombinant 5-LO in a glutathione peroxidase-dependent manner (IC50 = 300 nM). CJ-13610 also inhibits 5-LO product formation induced by phosphorylation in PMNLs and HeLa cells. In vivo, CJ-13610 (3-10 mg/kg) reduces levels of leukotriene B4 and decreases mechanical hyperalgesia in a rat model of chronic inflammatory pain induced by Freund's adjuvant. It also reverses tactile allodynia and increases hind paw weight bearing in a rat medial meniscal transection model of osteoarthritic pain when administered at doses ranging from 0.6 to 6 mg/kg.
References:
[1]. Fischer, L., Steinhilber, D., and Werz, O. Molecular pharmacological profile of the nonredox-type 5-lipoxygenase inhibitor CJ-13,610 Br. J. Pharmacol. 142(5), 861-868 (2004).
[2]. Cortes-Burgos, L.A., Zweifel, B.S., Settle, S.L., et al. CJ-13610, an orally active inhibitor of 5-lipoxygenase is efficacious in preclinical models of pain Eur. J. Pharmacol. 617(1-3), 59-67 (2009).