This article will discuss the danger of using Cardarine, why it was originally studied, and its status in sanctioned sports.
Cardarine, is classified as a Peroxisome Proliferator Activator Receptor (PPAR-delta), a type of agonist which functions by the activation of the PPAR-delta pathway in the body at certain receptor sites. During its pinnacle of popularity, Cardarine was hyped as the scientific breakthrough for treating diabetes, hyperlipidemia and obesity. During the late 1990s, Cardarine peaked a lot of interest in athletes and bodybuilders, and originally sold as Enduborol. Moreover, there is unconfirmed speculation that Cardarine was used by a considerable number of athletes during the 2008 Olympics.
Cardarine, which is also referred to as GW501616, is a research compound which was developed in 1991, by pharmaceutical companies, Ligand and Glaxo Smith Kline. Cardarine was developed for treatment of cardiovascular issues as well as for metabolic syndrome, specifically for increasing metabolism, counteracting obesity and increasing muscle growth. Although researchers were optimistic about the promising benefits of Cardarine, research stopped once it was discovered that Cardarine could cause cancer within a relatively short period of use.
Today, Cardarine is classified as illegal substance for human consumption. The supposed benefits of Cardarine are unsubstantiated and undocumented. More importantly, while Cardarine was being researched prior to its advancement to clinical trials, it was discovered that it could cause cancer. We cannot emphasize enough how dangerous this compound is, and should be avoided at all costs. The information provided here regarding Cardarine/GW501616 has been compiled from current clinical and scientific research papers and/or studies.
Even though Glaxo Smith Kline and Ligand discontinued producing Cardarine for its studies, small independent research studies still continue, however Cardarine has yet to be proven safe in order to conduct a viable human study.
Cardarine is a complex compound finalized by Glaxo Smith Kline, and used in research furthering additional beneficial treatment for blood vessels, diabetes and heart conditions. In 2014, an animal study, combined peroxisome proliferator-activated receptor (PPAR) modulators were combined with Cardarine or GW501616, a selective PPAR modulator (SPPARM), to determine whether the combination would be effective in treating cardiometabolic disease by insulin sensitization, modifying lipids, and reducing inflammation. Researchers had to stop during the second phase of the study when they determined that Cardarine or GW501616, was responsible for causing cancer in the test subjects.
Advocates of Cardarine claim that risk of cancer resulted only in animal studies and to date there have been no human studies. The response from the scientific community is that in order to conduct a human study, the compound must first be determined safe, prior to substantiating a long-term human study, which has not been the case.
The answer is simple, just look at the modern sedentary lifestyle. People are spending more hours sitting at their desk than ever before, that sitting for long periods of time has been categorized more dangerous than smoking cigarettes. Today, our inactive lifestyle creates many additional metabolic problems, including diabetes, high blood pressure, increased inflammation and cardiovascular disease. Research scientists began to work on compounds that could increase fat burning and physical endurance in sedentary and overweight adults. In particular, researchers began exploring the PPAR-delta route.
Initiation of PPAR delta is linked with greater energy, burning of fat, muscle growth, greater endurance and reduction of lipids in blood. Cardarine starts up PPAR delta simply by connecting to it. Because PPAR delta is already present in muscle cells, is the main reason that it stimulates so many genes which are essential for energy use and production.
When researchers discovered that the activation of PPAR delta was correlated with building muscle, advancing heart health, increasing metabolism and lowering inflammation, they were using GW50156 as the activator. Initially this seemed to be a very promising compound, but once the researchers observed that Cardarine caused cancer, they stopped using it immediately.
Advocates of using Cardarine despite the danger, claim that it may:
In the scientific community, those who have clinical experience are emphatic about the many dangers of using Cardarine, including but not limited to:
PPAR delta, is a hormone receptor which regulates a range of biological processes in addition to having potential roles in a number of chronic diseases, such as atherosclerosis, cancer, diabetes and obesity. Additionally, it has been determined that PPAR delta is essential for optimum cardiovascular function, production of energy, effective endurance function, decreasing inflammation and obesity.
Additionally, PPAR delta has been shown to:
It is important to note that cancer studies which examined the function of PPAR delta on cancer cells, showed conflicting results as to whether PPAR delta encouraged or blocked cancer formation.
PPAR delta also has a role with cholesterol and fat absorption in addition to facilitating intestinal mucosal growth as a response to fat. Moreover, PPAR delta reduces inflammation response of macrophages and is associated with substantially elevating HDL cholesterol. When PPAR is activated, the liver glucose output is reduced by the liver, which in turn helps with glucose tolerance as well as insulin sensitivity.
Cardarine’s popularity has essentially been spread through the internet via multiple hardcore bodybuilding and drug forums, where the side effects and dangers are not even mentioned. As a result of the talk online, Cardarine or GW501516 has become available for sale on the black market and as a research substance. Some sites are even marketing Cardarine as Endurobol, an endurance enhancing compound.
Normally, the World Anti-Doping Agency has its policies clearly written on its website and printed literature that it provides. Due to the Cardarine’s popularity on the web, the World Anti-Doping Agency issued a first of its kind warning to athletes about the very real life-threatening dangers associated with Cardarine detailing in particular it’s toxicity.
It is tough to get the truth online without doing some detailed research due to certain bodybuilding sites and unscrupulous testosterone clinics that are not disclosing the dangers or serious toxicity that is caused by using Cardarine.
If you are still wondering whether Cardarine is legal after reading all of this, it is not!
You may have seen some sites online that are classifying Cardarine as a selective androgen receptor modulator otherwise known as SARM. This classification is incorrect as Cardarine is definitely not a SARM because it does not work on androgen receptors. Cardarine is an activator of PPAR-delta, whereas SARMs work on activation of androgen receptors in certain particular tissues such bone or muscle in order to stimulate muscle growth.
The first Cardarine animal study attempted to see if it could lower oxidative stress in the brain. The initial results were positive and showed that mice who were given Cardarine showed to have improved blood circulation in brain tissue and a lowered amount of oxidative stress.
Although the initial result looked promising, Cardarine was also discovered to have pro inflammatory effects on the animal brain cells. For example, while Cardarine lowered certain inflammatory cytokines such as TNF (Tumor Necrosis Factor), it increased others like IL-6 (Interleukin 6), which can cause brain cell damage at elevated levels.
The study concluded the positive aspect of Cardarine on oxidative stress were quickly negated due to the high potential for brain damage.
Cardarine’s fat burning potential was one of the main factors that interested researchers. The researchers already knew that cardarine would kickstart PPAR-delta, which would thereby turn on a significant number of genes which played a role in fat burning and increasing energy.
Not long ago, a very small human study (less than 15 subjects) examined Cardarine’s fat burning effects. In that particular study, the subjects were men who had high cholesterol and significant storage of belly fat. Cardarine was given to the subjects at a dose of 2.5 mg per day for a period of 6 weeks. At the conclusion of the study, the subjects had lowered their levels of triglycerides, fatty acids and VLDL, a low-density lipoprotein similar to LDL.
Shortly thereafter, another small human study examined the fat burning and energy increasing effects of l-carnitine. At the end of the study the researchers concluded that the fat burning and energy increase effects were better than Cardarine. The researchers noted that while Cardarine provides some low-quality fat burning and does reduce blood fats, the danger of using Cardarine far outweighs any of its purported benefits.
Researchers began looking at Cardarine as a potential solution in the prevention of obesity. In an animal study using obese moneys with increased cholesterol as subjects, it was found that Cardarine had a direct effect in the reduction of metabolic syndrome. At the conclusion of the study, the subjects had a 20% decrease in liver fat, 11% decrease in insulin, mand more than a 20% drop in triglyceride, VLDL and LDL levels.
Similarly, in a study where mice were given Cardarine, which resulted in lower glucose production by the liver and a greater sensitivity to insulin.
Research scientists discovered that smaller doses of Cardarine decreased tissue damage and inflammation in the arteries and blood vessels of mice. This discovery led the researchers to see if Cardarine could be used to reduce the risk of heart disease as well as its complications.
In animal studies conducted on mice, Cardarine was responsible for inhibiting oxidative damage to blood vessels. It was also presumed Cardarine would increase nitric oxide production and as a result could lower plaque buildup in the arteries. Moreover, mice given low doses of Cardarine did show a reduction in inflammation and tissue damage in their arteries.
Adding Cardarine to human heart cells in the laboratory, produced an increase in the growth of new blood vessels. While this result may be helpful for someone with heart disease, it could be excessive for a healthy person or a person who had a propensity of developing cancer.
In the same animal study, kidney inflammation was measured in the mice prior to the administration of Cardarine. After the mice were given a small dose of Cardarine, inflammation in the kidneys was reduced followed by an overall lowered activity of genes which indicate the presence of kidney disease.
The primary focus of studying Cardarine was how it would affect the liver. The liver is the most critical organ involved in the burning, release and storage of fat in the body. PPAR-delta is responsible for regulating glucose metabolism and insulin sensitivity, by triggering the liver to shift its source of energy from glucose to fatty acids, thereby reducing blood sugar.
During the initial mouse and cell studies, Cardarine showed promising results as being potentially advantageous to liver health. Liver cells which were exposed to Cardarine, produced lower levels of cytokines, which was thought to aid in preventing insulin resistance. Mice who were feed a high fructose diet, showed lower levels of liver damage as a result of Cardarine and had lower chances of developing fatty liver disease.
However, in a relatively short period of time, Cardarine was shown to have caused death of liver cells as well as fibrosis or liver damage, advancing the position that the compound was too dangerous for human studies.
Endurance training can stimulate adaptive muscle fiber transformation as well the increase mitochondrial synthesis, by means of activating scripted changes in gene expression. To date, there is no identified transcription factor which can control this process in humans.
In one particular animal study, PPAR delta, activated by Cardarine, improved muscle fiber development in mice. The mice were made to continuously run for long periods and were able to achieve this targeted expression by increasing the number of type I muscle fibers in their body.
The new muscle fibers showed greater resistance to obesity and perfected metabolic profiles, even when not exercised. The study results also showed that mice who grew new muscle also had improved their endurance abilities and were able to run more than twice the duration of regular mice.
During the Cadarine research studies, doses ranged from 2 to 10 mg per day and were used for a period of up to 3 months. Due to the fact that this compound never got approval and clinical research being halted as a result of the compounds cancer causing properties, no dosage of Cardarine could be considered safe.
In the animal studies, Cardarine was shown to be the culprit in higher levels of cell death in liver cells as well as substantial liver damage in subjects with even low levels of liver disease. As a result of Cardarine being shown to cause cancer in animal studies (the primary reason why drug manufacturers Glaxo Smith Kline and Ligand aborted further development), human safety standards will never be accepted due to the obvious dangers associated with this compound.
Be cautious of aspiring testosterone replacement therapy clinics who undermine the dangers and neglect to mention the side effects of this compound. There is a considerable amount of clinical data available, evidencing the danger of using Cardarine.