GW1516 activates AMP-activated protein kinase and stimulates glucose uptake in skeletal muscle tissue, and has been shown to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome. It most likely does this by stimulating fatty acid oxidation. It has been proposed as a potential treatment for obesity and related conditions, especially when used in conjunction with a synergistic compound such as AICAR. The mechanism by which PPARδ agonists increase HDL seems to be a consequence of increased expression of ABCA1, the cholesterol transporter. It is a SARM that acts as a PPARδ modulator.

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