Cardarine (GW-501516)

Mechanism of Action

Cardarine (GW-501516) is a selective PPARδ (peroxisome proliferator-activated receptor delta) agonist. Despite commonly being grouped with SARMs, it is not an androgen receptor ligand. PPARδ activation enhances fatty acid oxidation, mitochondrial biogenesis, and metabolic efficiency in skeletal muscle. In preclinical models, GW-501516 dramatically increased running endurance (type I muscle fiber transformation) and improved metabolic markers. Clinical development was halted after Phase II due to concerns about potential carcinogenicity in animal models, though the clinical relevance remains debated. Studied for metabolic syndrome, exercise performance, and lipid modulation.

Evidence Level

In Vivo - Animal

6 studies published