Athletes and biohackers alike are always looking for the latest and greatest substance to help with performance. One such substance, Cardarine, also referred to as GW501516, is a synthetic compound that serves as a metabolic modulator. The appeal, is that cardarine, shifts energy metabolism from glucose to fatty acids, in lieu of suppressing insulin levels and triglycerides. Dubbed, as “exercise in a pill” we’re going to explore the compound Cardarine, also referred to as GW501516 or Endurobol.
Often thought of as a SARM (selective androgen receptor modulator) Cardarine is actually classified under a class of drugs called peroxisome proliferator-activated receptor (PPAR) agonists.
Cardarine, also referred to as GW501516 or Endurobol, is a synthetic compound that serves as a metabolic modulator. Compounds like Cardarine rely on energy expenditure in cells, and are thought to increase energy expenditure.
Cardardine is therefore an attractive aid for bodybuilders, to help promote fat loss, and attain better body composition.
Researchers have found that Cardarine promotes the burning of fat instead of glucose for energy. This essentially increases time to exhaustion, by reserving glucose stores prolonging exercise endurance capacity. Thus, the body utilizes fatty acids, as opposed to relying on glucose for energy improving exercise capacity.
Carardine or GW501516 was originally created by Ligland Pharmaceuticals and GlaxoSmithKline with the goal of potentially treating metabolic disease such as diabetes and hyperlipidemia.
Due to its selective action, cardarine is often thought of as a SARM. However, cardarine is what’s known as a peroxisome proliferator-activated receptor (PPAR) agonist. Activation of the PPAR-delta pathway causes a sudden increase in endurance and accelerated metabolism while lowering blood lipid levels.
It entered clinical development as a drug candidate for metabolic and cardiovascular disease states, due it’s promising benefits on blood lipid levels.
Despite these promising early results, further investigation and development of GW501516 was discontinued in 2007 after observations in animal studies of its association with the rapid induction of cancers in several organs (liver, stomach, tongue, skin, bladder, ovaries, womb and testes [R].
GlaxoSmithKline was about to embark on Phase III clinical trials. Phase III is the last step required before FDA approval, which involves large, double-blind-placebo controlled trials. GSK found that GW501516 had long term toxicity.
Mice that had been given GW501516 over their lifespan (2 years), developed cancer at a higher rate, than their drug free cage mates.
To establish that cardarine was safe for use, at an even lower dose, would require conclusive evidence, that these same effects did not occur, with a 70-year trial.
Without the established proof, the F.D.A. would likely pose that the potential risks of using the drug to be greater than the actual dangers of high cholesterol.
Studies have shown that cardarine can improve exercise performance. A study published in the journal Cell conducted by Ronald M. Evans, an American biologist and Professor and Head of the Salk’s Gene Expression Laboratory, investigated the effects of GW501516 on mice and found extraordinary results. After just four weeks of GW501516 application, the mice increased their endurance—how far they could run, and for how long—by as much as 75%.
After eight weeks of GW501516, the mice could run for nearly an hour and half longer than their drug-free peers.
Researchers believe the exact mechanisms work by mimicking the effect of endurance exercise on one particular gene: PPAR-delta.
With a shift in energy metabolism, weight loss will follow. Like all genes, PPAR-Delta issues instructions to other cells, on how to work and how to utilize fuel for energy. GW501516 essentially reconfigures the chemical message signaling to break down body fat through lipolysis while simultaneously suppressing the message to break down sugar for energy. In exercise terms, GW501516, helps delay muscle fatigue, which in turn will help you burn more calories and induce greater weight loss with prolonged exercise duration.
By burning body fat and prolonging exercise capacity, endurance capacity will improve. Burning fat for energy, and saving carbohydrates or glycogen means it takes longer to hit, “the wall”. Improved exercise volume combined while inhibiting the use of glycogen, will improve exercise endurance capacity.
Metabolic syndrome, is a cluster of symptoms. It includes things like obesity, high blood pressure, and high blood sugar – precursors to heart disease and diabetes. The first trials of cardarine, showed promising results, lowering bad cholesterol and increasing good cholesterol, while also lowering insulin levels and triglycerides.
Cardarine is classified as an investigational new drug by the FDA, meaning that it is still being studied and has not been approved for human use. As such, it is illegal to sell or distribute Cardarine in the U.S. for any purpose other than FDA-approved clinical trials.
Due it’s role as a metabolic modulator and performance enhancer, Cardarine was added to the list of banned substances controlled by the World Anti-Doping Agency (WADA) in 2009.
You can legally buy and use Cardarine in every country in the world except for Australia. In Australia, it’s considered as a Schedule 9 compound by the TGA which means that it’s illegal even with a doctor’s prescription. Cardarine however is distributed by black or grey market research laboratories, making potency, as well as quality highly questionable.
Although cardarine has not been approved by the FDA as a pharmaceutical drug, plenty of people are taking it, especially athletes and bodybuilders. Once the structure of a new compound has been published, chemical-supply laboratories are free to synthesize it for sale, “for research purposes only”. Research has shown that cardarine may provide a number of health benefits associated with performance weight loss, and endurance capacity. More research is required to support the use of cardarine in human clinical trials for performance enhancing benefits.
Cardarine is only available through questionable black market laboratories due to its investigational classification. Due to the lack in evidence and questionable sourcing, cardarine is not recommended for use in ergogenic enhancement.
Swolverine is no way supports or condones the use of illegal or nefarious substances or compounds. This article is for informational purposes only.
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