GW501516

GW501516 (also known as Cardarine or Endurobol) is a peroxisome proliferator-activated receptor delta (PPARδ) agonist that was initially developed by GlaxoSmithKline (GSK) and Ligand Pharmaceuticals for its potential therapeutic applications in metabolic and cardiovascular diseases. However, its development was discontinued in 2007 due to preclinical evidence of carcinogenicity.

History

GW501516 was first synthesized in the 1990s as part of a collaborative effort between GSK and Ligand Pharmaceuticals. The compound was initially developed as a potential treatment for metabolic and cardiovascular diseases, including diabetes, dyslipidemia, and heart disease. However, during preclinical trials, the compound was found to cause cancer in laboratory animals, leading to the discontinuation of its development in 2007.

Mechanism of Action

GW501516 acts as a PPARδ agonist. PPARδ is a nuclear hormone receptor that regulates gene expression. When activated by GW501516, PPARδ forms a heterodimer with the retinoid X receptor (RXR) and binds to specific regions of DNA known as PPAR response elements (PPREs). This binding results in the transcription of genes involved in energy expenditure, lipid metabolism, and insulin sensitivity.

Use in Sports

Despite its discontinued development, GW501516 has been used illicitly in the world of competitive sports due to its ability to enhance endurance. In 2013, the World Anti-Doping Agency (WADA) added GW501516 to its list of prohibited substances, warning athletes of its potential health risks.

Health Risks

The primary health risk associated with GW501516 is its potential to cause cancer. In animal studies, the compound has been shown to cause various types of cancer, including liver, bladder, and stomach cancer. As such, the use of GW501516 is strongly discouraged outside of a controlled research setting.

See Also

• Peroxisome proliferator-activated receptor
• GlaxoSmithKline
• Ligand Pharmaceuticals
• World Anti-Doping Agency