CJ-13610 |
| Catalog No.GC18728 |
CJ-13610, un inhibiteur de 5-LO de type non redox, supprime de manière dose-dépendante la formation de produit 5-LO dans le PMNL stimulé par l'ionophore A23187 en l'absence d'AA exogène avec une IC50 d'environ 70 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 179420-17-8
Sample solution is provided at 25 µL, 10mM.
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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).
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