An inhibitor of 5-LO (IC50 = 70 nM for 5-LO product formation in A23187-challenged PMNLs); inhibits recombinant 5-LO in a glutathione peroxidase-dependent manner (IC50 = 300 nM); reduces levels of LTB4 and decreases mechanical hyperalgesia in a rat model of chronic inflammatory pain induced by Freund's adjuvant (3-10 mg/kg); reverses tactile allodynia and increases hind paw weight bearing in a rat medial meniscal transection model of osteoarthritic pain (0.6-6 mg/kg)

CJ-13610 – 5 mg

Brand:
Cayman
CAS:
179420-17-8
Storage:
-20
UN-No:
Non-Hazardous - /

CJ-13610 is an inhibitor of 5-lipoxygenase (5-LO) that inhibits 5-LO product formation in human polymorphonuclear leukocytes (PMNLs) challenged with A23187 (Item No. 11016) in vitro (IC50 = 70 nM).{38804} 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; Item No. 20110) and decreases mechanical hyperalgesia in a rat model of chronic inflammatory pain induced by Freund’s adjuvant.{38805} 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.  

 

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Description

An inhibitor of 5-LO (IC50 = 70 nM for 5-LO product formation in A23187-challenged PMNLs); inhibits recombinant 5-LO in a glutathione peroxidase-dependent manner (IC50 = 300 nM); reduces levels of LTB4 and decreases mechanical hyperalgesia in a rat model of chronic inflammatory pain induced by Freund’s adjuvant (3-10 mg/kg); reverses tactile allodynia and increases hind paw weight bearing in a rat medial meniscal transection model of osteoarthritic pain (0.6-6 mg/kg),

Formal name: tetrahydro-4-[3-[[4-(2-methyl-1H-imidazol-1-yl)phenyl]thio]phenyl]-2H-pyran-4-carboxamide

Synonyms: 

Molecular weight: 393.5

CAS: 179420-17-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Lipoxygenases||Research Area|Neuroscience|Pain Research

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