GW501516 , also known as Cardarine, is a synthetic agonist of peroxisome proliferator-activated receptor β/δ (PPARβ/δ) . It has been shown to have various effects on human cells, including promoting endothelial cell proliferation and angiogenesis , changing lipid/glucose metabolism and gene expression in human skeletal muscle cells , preventing the down-regulation of AMPK caused by a high-fat diet in the liver and amplifying the PGC-1α-Lipin 1-PPARα pathway leading to increased fatty acid oxidation , and switching fuel preference from glucose to fatty acids in isolated rat skeletal muscle . GW501516 has also been shown to negatively modulate cell migration and invasion of cancer cells , and to have an apoptotic effect on invasive bladder cancer cells . In addition, GW501516 has been found to increase the regenerative capacity of human endothelial progenitor cells by stimulating biosynthesis of tetrahydrobiopterin , and to improve the inflammatory state in the kidney . Finally, GW501516 has been shown to reduce liver fat content and increase fatty acid oxidation in dyslipidemic subjects with central obesity .
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