CJ-13610

CJ-13610 is an inhibitor of 5-lipoxygenase (5-LO) that inhibits 5-LO product formation in human polymorphonuclear leukocytes (PMNLs) challenged with A23187 (Cay-11016) 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 (LTB4, Cay-20110) 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.Formal Name: tetrahydro-4-[3-[[4-(2-methyl-1H-imidazol-1-yl)phenyl]thio]phenyl]-2H-pyran-4-carboxamide. CAS Number: 179420-17-8. Molecular Formula: C22H23N3O2S. Formula Weight: 393.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 10 mg/ml, Ethanol: 1 mg/ml. lambdamax: 258 nm. SMILES: NC(C1(CCOCC1)C2=CC=CC(SC3=CC=C(N4C(C)=NC=C4)C=C3)=C2)=O. InChi Code: InChI=1S/C22H23N3O2S/c1-16-24-11-12-25(16)18-5-7-19(8-6-18)28-20-4-2-3-17(15-20)22(21(23)26)9-13-27-14-10-22/h2-8,11-12,15H,9-10,13-14H2,1H3,(H2,23,26). InChi Key: VPTONMHDLLMOOV-UHFFFAOYSA-N.