179420-17-8CJ-13610

产品属性：

Cas No.179420-17-8

别名 N/A

化学名 tetrahydro-4-[3-[[4-(2-methyl-1H-imidazol-1-yl)phenyl]thio]phenyl]-2H-pyran-4-carboxamide

分子式 C22H23N3O2S

分子量 393.5

溶解度 DMSO: 10 mg/ml,Ethanol: 1 mg/ml

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
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).