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Description

A cell-permeable biphenylazolo-oxyacetate that acts as a potent and selective inhibitor of adipocyte Fatty-Acid-Binding Protein (aFABP/aP2) by targeting its fatty acid-binding pocket (Ki = <2 nM in a competitive binding assay using 1,8-ANS), while exhibiting much lower affinity for muscle and epidermal FABP's (Ki = 250 nM and 350 nM, respectively). Shown to effectively block foam cell transformation and the cellular expression of inflammatory mediators in aP2-positive, but not aP2-negative, THP-1 macrophage in vitro, as well as improve the glucose metabolism and insulin sensitivity in mice in vivo.