GW501516

White to off-white solid. Soluble in DMSO (30mg/ml), dimethylformamide (30mg/ml), ethanol (10mg/ml) or methanol (30mg/ml). Sparingly soluble in water. Potent and selective peroxisome proliferator-activated receptor (PPAR) delta agonist/activator with high affinity (Ki=1nM) and potency (EC50=1nM) for PPARdelta and >,1000 fold selectivity over PPARalpha and PPARgamma. The peroxisome proliferator-activated receptor delta (PPAR delta) has emerged as an important regulator of lipid homeostasis and inflammatory signaling. Recent in vitro, in vivo and human clinical studies have highlighted a role for PPARdelta activation in the prevention and treatment of insulin resistance and atherosclerosis, Antidiabetic compound, Shown to activate pathways initiated through exercise and was investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. Off-target high doses lead to tumor progression in rodents, Increases ABC A1 transporter expression and induces apolipoprotein A1-mediated cholesterol efflux in vitro, Increase serum HDL cholesterol and lowers small-dense LDL levels in obesity in vivo models, Reduces plasma triglyceride concentration, Increases expression of genes involved in lipid utilization, beta-oxidation, cholesterol efflux and energy uncoupling, as well as apolipoprotein-A1 specific efflux of intracellular cholesterol, indicating the muscle tissue is an important target, Model compound for a new type of obesity therapeutic, as well as a selective pharmacological tool for understanding lipid metabolism.