GW-501516

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GW-501516 (also known as Cardarine or Endurobol) is a PPARδ receptor agonist that was invented in a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. It was initially developed as a drug for the treatment of metabolic diseases and cardiovascular diseases.

History[edit | edit source]

GW-501516 was first synthesized in the 1990s through a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline. The aim was to create a drug that could potentially treat metabolic diseases and cardiovascular diseases. However, during the clinical trials, it was found that the drug caused cancer in rats and mice, leading to the discontinuation of its development.

Mechanism of Action[edit | edit source]

GW-501516 is a PPARδ receptor agonist. Peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor proteins that function as transcription factors regulating the expression of genes. GW-501516 specifically targets the delta subtype of these receptors.

Uses[edit | edit source]

Despite the discontinuation of its development, GW-501516 has been used illicitly in the world of sports. It is known to increase endurance and fat burning, and it is often used as a doping agent. However, it is banned by the World Anti-Doping Agency due to its potential to give athletes an unfair advantage.

Side Effects[edit | edit source]

The main side effect of GW-501516 is its potential to cause cancer. This was discovered during animal testing, where it was found that the drug caused cancer in rats and mice. As a result, it is not approved for human use.

See Also[edit | edit source]

GW-501516 Resources
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Contributors: Prab R. Tumpati, MD