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GW501516 (GW1516 or GSK-516) is a drug that acts as a PPAR delta regulator. GW 501516 activates AMP-activated protein kinases and stimulates glucose uptake in skeletal muscle tissue, GW 501516 has been shown to reverse the metabolic abnormalities of obese men with pre-diabetic metabolic syndrome, most likely by stimulating fatty acid oxidation. Potential treatments for obesity and related disorders have been proposed, particularly when used in conjunction with the synergistic compound AICAR, since the combination has been shown to significantly enhance exercise tolerance in animal studies.

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