GW-501516 also referred to as Cardarine, is a popular compound that was first developed in the early 1990s. Its main purpose is to prevent the formation of tumors in organs like the prostate, colon and breast tissue.
Although it was developed for a completely different purpose, the bodybuilding community started noticing it as a unique and potentially powerful SARM (Selective Androgen Receptor Modulator).
That’s because it has the ability to burn fat, boost endurance and reduce the amount of time that bodybuilders need to recover.
The best part is that GW-501516 is said to not have any side effects.
If all this is true then it’s the best thing since sliced bread for the bodybuilding community. But is it all that it’s cracked out to be? Let’s find out.
WHAT IS GW501516?
Pharmaceutical giant GlaxoSmithKline developed GW501516 with the intention to leverage its benefits for the treatment of blood vessels, heart, and diabetes.
But, research on this SARM stopped during phase 2 because the animals being tested started developing cancer.
The same results haven’t been observed in humans however, which means that it’s probably only dangerous for animals.
Besides, it would take much longer for the substance to start showing a cancer risk if it were to be tested for that effect on humans.
How was Cardarine discovered, you ask?
Well, the research community has always grappled with trying to find a suitable treatment for lifestyle diseases like inflammation, heart disease, and diabetes.
At some stage, scientists were looking for a compound that would make it possible to increase physical endurance while accelerating the body’s fat burning ability. This is when they stumbled upon the PPAR-delta pathway.
They found that by activating this pathway, they could instantly improve endurance, stimulate muscle growth, burn fat and increase energy while decreasing blood lipids.
Cardarine is one of the few compounds that have the ability to bind itself to the PPAR-delta pathway.
It’s interesting to note that most of the PPAR-delta is found in the muscles, so activating it naturally leads to:
- Improved muscle growth
- Heart health
- Reduced inflammation
Based on these facts we can conclude that GW501516 is a promising compound.
IS CARDARINE CONSIDERED A SARM?
No, Cardarine is NOT a SARM.
First of all, selective androgen receptor modulators (SARMs) are compounds that act on androgen receptors. These androgen receptors are located in muscle and bone tissues in order to increase muscle mass.
SARMs such as LGD4033 and RAD140 have been created with the intention to duplicate the activity of testosterone.
Cardarine is a PPAR-delta pathway activator. This means that it doesn’t target androgen receptors directly.
- Helps Burn Fat
PPAR-delta has the ability to activate a large number of fat burning genes.
In fact, a human study was recently conducted to corroborate these claims and found that Cardarine has the ability to reduce fatty acids, triglycerides and VLDL proteins.
These results were based on a double-blind, randomized and controlled trial study involving 13 men who suffered from bad cholesterol and excess belly fat.
The subjects were given a low dosage of just 2.5 mg per day over a period of 6 weeks.
In yet another study with 12 inactive males, the participants were given 5 to 10 mg of Cardarine per day for 12 weeks.
The results show that Cardarine was able to drastically reduce their levels of HDL cholesterol, triglycerides, and APOB.
- Helps with Muscle Growth and Boosts Stamina
Since Cardarine can activate PPAR-delta pathways, it can also improve strength endurance. One study showed that the compound might increase muscle fibers associated with peak physical performance.
- Protects the Brain
One animal study showed that Cardarine can help maintain normal blood flow to the brain. This protects brain vessels from oxidative damage and stress.
PPAR activators are known to enhance the development of nerve cells. PPAR-delta pathways can also help us achieve that result.
But when tested on rat brain cells, Cardarine was shown to have both pro and anti-inflammatory effects.
GW501516 increased the action of inflammatory cells like IL-6 while reducing others like TNF-alpha. So there’s no telling yet if Cardarine is good or bad for the brain.
- Helps with Obesity
In another double-blind randomized and controlled trial study with 6 overweight volunteers, Cardarine was able to reverse symptoms associated with metabolic syndrome and all without causing any adverse side effects.
The participants were given 2.5 to 10 mg of Cardarine per day for 2 weeks and showed reduced liver fat, insulin, and blood fat levels in just 2 weeks.
As if that weren’t enough, Cardarine traveled through the PPAR-delta pathways to help prevent the effects of inflammatory substances.
Thus, it was concluded that Cardarine may be of assistance in dealing with obesity-induced insulin resistance as well as chronic inflammation.
That’s because obese insulin-resistant patients usually carry around belly fat that exposes them to higher inflammatory cytokines when compared to healthy people who have more PPAR-delta.
Another study conducted on obese monkeys suggests that Cardarine may help decrease the risk of heart disease by reducing the occurrence of HDL cholesterol, LDL cholesterol, triglycerides, and insulin.
In a study done with mice, GW501516 was shown to prevent the overproduction of glucose by the liver, while increasing insulin sensitivity. If the same results can be achieved with human subjects, then Cardarine might be a fitting candidate for an effective treatment for Type 2 diabetes and obesity.
The mice even showed improvement in muscle fiber development, which could help prevent obesity without the need for physical exercise. The compound may also help prevent weight gain that’s caused by diet and lifestyle by accelerating fat burning in muscles.
- Protects Heart and Blood Vessels
Evidence suggests that taking Cardarine might actually influence the way our blood vessels work.
A study done on mice showed that it can prohibit oxidative damage that happens in blood vessels. This is in addition to boosting vessel-relaxing nitric oxide which helps protect blood vessels from the build-up of plaque in the arteries.
In lower doses, Cardarine has been found to offer tremendous benefits in terms of lowering inflammation and tissue damage. If it can do that, then it could contribute to reducing the risk and complications associated with heart disease.
We also know that it has the ability to boost new blood vessel growth in actual human heart cells. This is promising news for heart disease sufferers but it’s only effective in limited doses. Cardarine’s ability to increase blood vessels may also be a risk factor for cancer patients.
- Lowers the Chances of Kidney Inflammation
According to a study done on mice, GW501516 can significantly diminish the occurrence of kidney inflammation which can preclude kidney disease. In the mentioned study, Cardarine was able to slow down the genes associated with kidney disease.
- It’s Antioxidant
Generally speaking, Cardarine is an effective inflammation suppressant.
It has been shown to suppress liver inflammation in animals by activating PPAR-delta. It can even suppress inflammation on the DNA level, causing inflammatory genes to slow down. In one study, Cardarine was applied topically on mice suffering from diabetic wounds and it greatly accelerated their healing.
Using the PPAR-delta pathway, Cardarine was able to curb inflammation and promote the survival of skin cells in order to improve the skin’s ability to heal the wound. When looking deeper, scientists found that Cardarine can also prevent the production of inflammatory molecules like NFκB, IL-6, TNF-alpha, and MCP-1.
It didn’t stop there, however, as GW501516 stimulated the production of beneficial antioxidant enzymes as well.
- Protects Liver from Damage
This compound mainly targets the liver because it’s a major organ that’s responsible for regulating fat at different stages, from burning to storing and releasing it.
GW501516 can help reduce blood sugar by forcing the liver to derive its energy from fatty acids instead of glucose.
A study done with mice showed that Cardarine may also prohibit insulin resistance by reducing the production of IL-6. To prove this point, researchers gave Cardarine to a group of mice who were consuming a high fructose diet and it actually protected them from liver damage.
Further research showed that this compound has the ability to prevent liver damage in mice by killing degenerative cells.
POTENTIAL CARDARINE SIDE EFFECTS
In a study with mice that had liver disease; Cardarine was shown to escalate liver cell death which had the side effect of actually worsening the liver damage.
It was also discovered through animal studies that Cardarine is not safe for use during pregnancy as it can inhibit fetal development. In rats, it showed the potential to cause cancer. But, the rats were given extremely high dosages of Cardarine for longer periods of time.
The discovery of these and other risks led GSK to pause research on this compound even though there’s no evidence to suggest that it would have the same effect on human subjects.
If you’re thinking of taking GW501516 then you should consider these side effects and the lack of evidence so that you can make an informed decision in the end.
Remember, it’s only available as a research chemical.
During clinical studies, researchers used dosages of 2.5 mg to 10 mg per day for 12 weeks at a time.
Bodybuilders and fitness enthusiasts will use anywhere from 10 to 20mg of Cardarine per day.
A typical SARMs stack that includes GW501516 will last anywhere from 6 to 10 weeks. These often include Ostarine and Andarine to help with building muscle.
You’ll also see plenty of researchers stack it with SR9009.
GW501516 is one of the most widespread compounds in the bodybuilding community. Even athletes turn to this compound to boost their performance and maximize gains.
While we know about GW501516’s ability to increase energy, shred fat and build muscle, the only available research we have is based on animal studies and anecdotal evidence.