FABP4 INHIBITOR 1PC X 5MG

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.

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

Molecular Weight: 474.55. Empirical Formula: C₃₁H₂₆N₂O₃. Quality Level: 200. Assay: ≥. 98% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: ethanol: 20 . mg/mL, DMSO: 50 . mg/mL, methanol: 50 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. InChI: 1S/C31H26N2O3/c1-2-27-30(22-12-5-3-6-13-22)31(23-14-7-4-8-15-23)32-33(27)28-19-10-9-18-26(28)24-16-11-17-25(20-24)36-21-29(34)35/h3-20H,2,21H2,1H3,(H,34,35). InChI key: SJRVJRYZAQYCEE-UHFFFAOYSA-N. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.