General 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 (K_i = ﹤2 nM in a competitive binding assay using 1,8-ANS), while exhibiting much lower affinity for muscle and epidermal FABP′s (K_i = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Furuhashi, M., et al. 2007. Nature447, 959.Sulsky, R., et al. 2007. Bioorg. Med. Chem. Lett.17, 3511.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)