GW-501516

gw-501516, cardarrine also known as GW501516 or Endurobol, is a PPAR (peroxisome proliferator-activated receptor) agonist and ligand-activated transcription factor that binds to receptors in skeletal muscle tissue and body fat and pushes skeletal muscle cells towards preferential lipid utilization and fat burning. It is often wrongly classified as a selective androgen receptor modulator (SARM). As a PPAR, it shares certain commonalities with SARMs but differs from them in a few important ways. GW 501516 does not affect androgen receptors or alter testosterone levels.gw-501516

Cardarine Mechanism of Action

Invented in the early 1990s, Cardarine is also known by a number of alternate names, including GW1516 and GSK-516. It displays high affinity (Ki = 1 nM) and potency for PPARδ with over 1,000-fold selectivity over PPARα and PPARγ [5]. Binding of GW501516 to PPARδ recruits the coactivator PGC-1α. The PPARδ/coactivator complex in turn upregulates the expression of proteins involved in energy expenditure [6]. By activating AMP-activated protein kinase, it is widely believed to provide a broad range of experimental effects, such as:

• Increases fatty acid oxidation and promotes fat loss
• Lower LDL cholesterol (“bad cholesterol”)
• Higher HDL cholesterol (“good cholesterol”)
• Increases endurance
• Reduces inflammation
• Decreases insulin resistance and improves glucose tolerance

Data indicates that PPAR activity preserves glucose for use in tissues like the brain while promoting the mobilization of fatty acids for muscular endurance [10]. PPAR has also been observed playing an important role in temperature regulation, inflammation mediation, mitochondrial respiration, keratinocyte differentiation, and skin and muscle repair. Molecular analyses revealed that PPAR regulates the expression of genes associated with contractile proteins, lipid oxidation, and mitochondrial biogenesis [10].

The benefits and side effects of GW501516 however, have not been confirmed by the Food and Drug Administration (FDA) and like other SARMs for sale, it should be used for research purposes only. Due to its tendency to increase endurance and energy, the World Anti Doping Agency (WADA) has banned the use of Cardarine in professional sports and several athletes have tested positive for the drug and dismissed.gw-501516

Studies including Cardarine

A number of human and animal studies have been performed that point to the Cardarine’s ability to enhance certain physiological processes related to energy metabolism as well as potential improvements in blood lipids:gw-501516

• One study on mice found that GW501516 promotes fatty acid oxidation and fat burning in skeletal muscle tissue and alleviates metabolic syndrome
• Another study discovered that peroxisome proliferator-activated receptors can markedly increase running endurance in Kunming mice
• Yet another study on mice revealed that PPARs augment exercise endurance by preventing exhaustion of glucose (“hitting the wall”) [
• A study involving obese rhesus monkeys found that GW 501516 increased high-density lipoprotein (HDL) and lowered very-low-density lipoprotein (VLDL), indicating potential cardioprotective effects from Cardarine. gw-501516
• Two separate phase II clinical studies in humans found positive effects of Cardarine on obesity, diabetes, dyslipidemia, and cardiovascular disease, as well as suppression in macrophage-derived inflammation gw-501516
• A study in rats that were fed a high fructose diet found that GW 501516 reduced inflammation markers, especially in the liver, and increased the expression of genes that regulate beta-oxidationgw-501516

Side Effects of Cardarine

While Cardarine is not known to cause androgenic side effects like anabolic androgenic steroids, data in rats indicates that doses of 3mg/kg/day (180-240mg per day in the average 60-80kg adult), significantly higher than those used in human trails, caused cancer to develop quickly in several organs [9]. Anecdotal data online indicates little in the way of noticeable side effects but more research is necessary to determine the overall safety profile of GW501516 before it can be approved for human use.gw-501516