Identification | Back Directory | [Name]
4-Thiazolecarboxylic acid, 2-[2-(4-octylphenoxy)acetyl]-, methyl ester | [CAS]
1621517-53-0 | [Synonyms]
GK470 GK-470 GK 470 4-Thiazolecarboxylic acid, 2-[2-(4-octylphenoxy)acetyl]-, methyl ester | [Molecular Formula]
C21H27NO4S | [MOL File]
1621517-53-0.mol | [Molecular Weight]
389.51 |
Hazard Information | Back Directory | [Description]
GK470 is a inhibitor of group IVA cytosolic phospholipase A2 (GIVA cPLA2). | [Uses]
GK470 (compound 28) is an inhibitor of group IVA cytosolic phospholipase A2 (GIVA cPLA2) with an IC50 of 300 nM in vesicle assays. GK470 has anti-inflammatory activity, inhibiting the release of arachidonic acid in SW982 fibroblast-like synoviocytes with an IC50 value of 0.6 μM. GK470 exhibits comparable anti-inflammatory effects to Methotrexate (HY-14519) in a preventive collagen-induced arthritis model and significantly reduces plasma PGE2 levels[1]. | [References]
[1] Kokotos G, et al. Inhibition of group IVA cytosolic phospholipase A2 by thiazolyl ketones in vitro, ex vivo, and in vivo[J]. Journal of medicinal chemistry, 2014, 57(18): 7523-7535. DOI:10.1021/jm500192s |
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