GW501516

Product description: 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.

Alternate Names/Synonyms: GSK-516; GW1516; Endurobol; 2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]acetic acid

CAS: 317318-70-0

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