GW501516, also known as GW-501,516,GW1516 or GSK-516 is a PPAR***948; modulator
compound being investigated for drug use. It activates the same pathways
activated through exercise, including PPAR***948; and AMP-activated protein
kinase. GW501516 is being investigated as a potential treatment for obesity,
diabetes, dyslipidemia and cardiovascular disease. GW-501516 has a synergistic
effect when combined with AICAR: the combination has been shown to
significantly increase exercise endurance in animal studies more than either
compound alone.
GW501516
regulates fat burning through a number of widespread mechanisms; GW501516
increases glucose uptake in skeletal muscle tissue and increases muscle gene
expression, especially genes involved in preferential lipid utilization., This
shift changes the body’s metabolism to favor burning fat for energy instead of
carbohydrates or muscle protein, potentially allowing clinical application for
obese patients to lose fat effectively without experiencing muscle catabolism
or the effects and satiety issues associated with low blood sugar. GW-501516
also increases muscle mass, which improved glucose tolerance and reduced fat
mass accumulation even in mice fed a very high fat diet, suggesting that
GW-501516 may have a protective effect against obesity.
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