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.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Furuhashi, M., et al. 2007. Nature447, 959. Sulsky, R., et al. 2007. Bioorg. Med. Chem. Lett.17, 3511.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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