GW501516 (Cardarine)

What is GW501516?

GW501516 is a PPARδ receptor agonist. It entered clinical development as a drug candidate for metabolic and cardiovascular diseases, but was abandoned in 2007 because animal tests showed that the drug would cause cancer to develop rapidly in multiple organs.

A study published in 2007 showed that giving mice high doses of GW501516 significantly improved their physical functions; this work was widely discussed in the mass media, and led to drug candidates entering the black market and leading athletes to abuse it as a stimulant . The World Anti-Doping Agency (WADA) tested GW501516 and other related chemicals and put it on the banned list in 2009; it has issued additional warnings to athletes that GW501516 is unsafe.

Performance enhancer
Before the 2008 Beijing Olympics, there were concerns that GW501516 might be used by athletes as a function-enhancing drug. At present, the drug is not controlled by regulations or cannot be detected by standard tests. Therefore, one of the main researchers in the endurance enhancement study developed a urine test to detect this drug and provided it to the International Olympic Committee. The World Anti-Doping Agency (WADA) has developed a test for GW501516 and other related PPARδ modulators and added these drugs to the banned list in 2009.

GW501516 has been promoted on fitness and sports websites, and has been on the black market for some time in 2011. In 2011, it was reported that the cost of 10 grams was $1,000. In 2012, WADA reclassified GW501516 from a gene doping compound as a “hormonal and metabolic regulator”.

In 2013, the World Anti-Doping Agency took rare measures to warn potential users of the compound that there may be health risks, stating that “the substance has not yet been clinically approved and will not be given”; new scientists attribute the warning to the drug’s carcinogenicity risks of.

Many athletes tested positive for GW501516. In the Vuelta Ciclista race in Costa Rica in December 2012, four Costa Rican drivers tested positive for GW501516. Three of them were suspended for two years, and the fourth was suspended for 12 years because it was the second time he took doping. In April 2013, Russian cyclist Valery Kaykov was suspended by the bicycle management agency UCI after testing positive for GW501516. Kaykov’s team RusVelo immediately fired him. In May 2013, Venezuelan Miguel Ubeto was temporarily suspended by the Lampre team. In February 2014, Russian race walker Elena Lashmanova tested positive for GW501516. In April 2019, heavyweight boxer Jarrell Miller tested positive for GW501516, which caused his challenge to the Anthony Joshua World Heavyweight Championship to be cancelled. On December 2, 2020, Miller was suspended for two years for repeated violations.

Benefits

Cardarine binds to these PPARδ receptors, which are a group of nuclear proteins found in muscles and fatty acids in the body. Therefore, these receptors are activated and help the body burn fat, increase muscle endurance and build lean muscle. It also has a positive effect on your vascular system.

Cardarine can lower low-density lipoprotein cholesterol levels, thereby reducing the risk of heart attack.
It may also activate the PPARδ receptor, which has anti-inflammatory properties and can reduce oxidative damage to blood vessels and tissues.
The anti-inflammatory properties of Cardarine can also protect brain cells from oxidative stress and help reduce kidney inflammation.
It attempts to increase the level of nitric oxide in the arteries, thereby increasing the distribution of blood vessels and improving the wound healing process.
Due to the increased distribution of blood vessels, it can help increase your endurance level, thereby prolonging your exercise time.
Cardarine also attempts to inhibit glucose metabolism in the liver because it can help convert the energy source from glucose to fatty acids. Therefore, it can improve your body’s fat burning capacity and can also inhibit insulin resistance.
In most cases, Cardarine also has a slight ability to increase muscle mass, but when it is superimposed with SARM, the results may be improved.
In most cases, no post-cycle treatment is required after using Cardarine. This may be because it may not cause your testosterone levels to decrease. Cardarine can also be used during the PCT after the SARM cycle to avoid increasing body fat.

Dosage

Cardarine doses used in clinical trials on humans range from 2.5 mg/day to 10 mg/day, although some people have used 20 mg/day.

The following are Cardarine dosage guidelines:

Beginner: 5 mg per day
Intermediate: 10 mg per day
Advanced: 20 mg per day

Side effects

According to the Australian Department of Health and clinical studies, there are no known side effects from taking Cardarine.
Although Cardarine has few short-term side effects in humans, more research should be conducted on the long-term effects.
A common problem is related to a study that found that GW501516 caused cancer growth in the organs of laboratory mice.
However, it has been noted that the mice in this study received this PPARδ receptor continuously (without rest) for approximately 2/3 of their lives.
With this in mind, the evidence that Cardarine can cause cancer in humans is unstable at best-no bodybuilder would take Cardarine every day for two-thirds of his life (approximately 50 consecutive years).