An inhibitor of 5-LO
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CJ-13610

Item No. 21764

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/mlEthanol: 1 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $130

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    10 mg

    $236

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    25 mg

    $527

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    Product Description

    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).1 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.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description 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).

    Product Citations

    Ferguson, H.E., Kulkarni, A., Lehmann, G.M., et al. Electrophilic peroxisome proliferator-activated receptor-γ ligands have potent antifibrotic effects in human lung fibroblasts. Am. J. Respir. Cell Mol. Biol. 41, 722-730 (2009).