Product Description
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AI Product Description
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GW501516, commonly known as Cardarine or GW-0742, is a potent synthetic non-steroidal peroxisome proliferator-activated receptor delta (PPARδ) agonist. Originally developed by Ligand Pharmaceuticals in the late 1990s for the treatment of metabolic disorders such as obesity, type 2 diabetes, and dyslipidemia, its primary mechanism involves activating PPARδ receptors found abundantly in skeletal muscle and heart tissue. This activation mimics the physiological effects of endurance exercise by shifting cellular metabolism toward increased fatty acid oxidation and glucose uptake, thereby enhancing aerobic capacity and reducing fatigue without the need for physical exertion.
The molecular formula of GW501516 is C23H28FN3O3S, with a corresponding CAS number of 260713-21-7. Structurally, it features a complex arrangement including a difluorophenyl group and a thiazole ring, which are critical for its high affinity and selectivity toward the PPARδ subtype over other PPAR isoforms. During clinical trials, the compound demonstrated remarkable efficacy in improving lipid profiles and increasing running distance in animal models. However, development was abruptly halted in 2008 due to safety concerns. Long-term studies in rodents revealed that while the drug significantly extended survival rates in some contexts, it also induced rapid onset of multiple cancer types, including hepatocellular carcinoma and bladder tumors. Consequently, the U.S. Food and Drug Administration (FDA) did not approve the drug for human use, and it remains classified strictly as a research chemical.
Despite its regulatory status, GW501516 has gained notoriety in athletic communities and bodybuilding circles as a performance-enhancing substance, often marketed under the nickname "Cardarine." Users report significant improvements in stamina and fat loss, though these benefits come with severe unverified health risks. It is crucial to note that the World Anti-Doping Agency (WADA) prohibits its use in competitive sports. While the theoretical promise of PPARδ agonists for treating metabolic syndrome persists in scientific research, GW501516 itself is no longer pursued for therapeutic application due to its carcinogenic potential. Current medical focus has shifted toward developing safer analogs that retain metabolic benefits without triggering oncogenic pathways.