Application

GW501516 has been used to study its effect on mutation-driven colorectal tumorigenesis and tumor invasion using mouse model.

GW501516 has been used as a peroxisome proliferator-activated receptor (PPAR) δ agonist: to treat the differentiated L6 myotubes to test its effect on free fatty acid (FFA) uptake under mild hypoxia conditionsin organoid culture medium to test its effect on self-renewal of PR domain containing 16 (Prdm16)-depleted intestinal stem cellsas a component in the defatting medium for primary human hepatocytes (PHH) culture

Biochem/physiol Actions

GW501516 is a selective Peroxisome Proliferator-Activated Receptor delta (PPARδ) agonist with high affinity (Ki = 1 nM) and potency (EC₅₀ = 1 nM) for PPARδ and > 1000 fold selectivity over PPARα and PPARγ. GW501516 was shown to activate some of the same pathways activated through exercise, and was investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. However, GW501516 also showed an increase in cancer in rats.

PPARδ activation by GW501516, retards weight gain through fatty acid catabolism in adipose tissue and skeletal muscles. GW501516 causes an increase in the levels high-density lipoprotein cholesterol and apolipoprotein A (apoA) and reduction in the low density-lipoprotein cholesterol, apoB, and triglyceride.

Packaging

5, 25 mg in glass bottle