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Beschreibung

A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor delta (PPARdelta) agonist (Ki = 6 nM for hPPARdelta and 730 nM for hPPARgamma). Potently induces adipocyte differentiation in NIH-PPARdelta cells at 500 nM and raises total cholesterol in insulin resistant db/db mice without altering glucose or triglycerides levels. Increases UCP3 (uncoupling protein 3) gene expression in L6 myotubes. Inhibits cytokine-induced expression of VCAM-1 (vascular cell adhesion molecule-1) and the secretion of MCP-1 (monocyte chemotactic protein-1) in EAhy926 cells., A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor delta (PPARdelta) agonist (Ki = 6 nM for hPPAR delta and 730 nM for hPPARgamma). Induces adipocyte differentiation in NIH-PPARdelta cells at 500 nM. Also reported to raise total cholesterol in insulin-resistant db/db mice without altering glucose or triglyceride levels. Shown to increase uncoupling protein 3 (UCP3) gene expression in L6 myotubes. Also shown to inhibit cytokine-induced expression of vascular cell adhesion molecule-1 (VCAM-1) and the secretion of monocyte chemotactic protein-1 (MCP-1) in Eahy926 cells.

Strukturformel

L-165,041

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