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GW501516 is a chemical with many purported health benefits. It can protect the brain and heart and improve muscle growth. However, it also has its negative effects. Read more below to learn about this chemical.

Note: By writing this post, we are not recommending this drug. Some of our readers who were already taking the drug requested that we commission a post on it, and we are simply providing information that is available in the scientific literature. Please discuss your medications with your doctor.

Introduction

GW501516 is a chemical that binds to and activates the peroxisome proliferator activator receptor delta (PPAR delta). PPARẟ is a transcription factors, which is a protein that increases the expression of many genes (R).

The activation of PPARẟ has significant implication in improving cardiovascular health, metabolism, and as an anti-inflammatory agent. However, there are some negative effects to GW as well.

Health Benefits of Cardarine/GW501516

1) Cardarine Protects the Brain

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In animals, GW 501516 protects brain vessels when they are under oxidative stress (R).

Activation of PPARẟ by GW 501516 could drive the development of nerve cells (R).

Additionally, it prevents blood vessel dysfunction, especially in brain vessels (R).

2) Cardarine Benefits the Heart

GW 501516 prevents oxidative damage in the heart (R).

It decreases the risk and severity of atherosclerosis (plaque buildup in the arteries) through a number of mechanisms. GW 501516 increased levels of nitric oxide, which protects against atherosclerosis (R).

It also reduces lesions and inflammation associated with atherosclerosis in mice (R).

GW 501516 increases VEGF production from human blood vessel cells, which triggers cell and blood vessel formation (R).

GW 501516 results in an increase of HDL cholesterol and a decrease in triglycerides in animal studies, potentially decreasing the risk of cardiovascular disease in patients (R).

3) Cardarine Increases Metabolism and Prevents Obesity

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GW 501516 activates PPARẟ, which may increase the breakdown of fatty acids and increase energy expenditure in muscle. This could help treat obesity (R).

PPARẟ activates the expression of a number of genes involved in reducing cholesterol and increasing energy expenditure (R).

This treatment could protect against weight gain due to diet (R).

Also, GW 501516 decreases glucose output by the liver and increases insulin sensitivity in mice (R).

By driving muscle fiber development in mice, GW 501516 creates a resistance to obesity (R).

4) Cardarine Protects the Kidneys

In mice, it was shown to inhibit inflammation in kidney cells, and may protect against kidney disease. It does this by lowering MCP-1 expression that is generally increased in such kidney diseases (R).

5) Cardarine Helps the Immune System

GW 501516 is associated with the suppression of inflammation (R).

Activated PPARẟ suppresses inflammation in the liver in animals by inhibiting molecules that contribute to inflammatory responses (R).

GW 501516 can activate PPARẟ which protects specific skin cells from undergoing spontaneous cell death during the wound healing process (R).

It was also shown to accelerate diabetic wound closure (R).

6) Cardarine Protects Against Liver Damage

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PPARẟ activation by GW 501516 causes the liver to switch its energy source from glucose to fatty acids, thus reducing blood sugar (R).

In mice, GW 501516 inhibited IL-6, which may help prevent insulin resistance in liver cells (R).

Short-term use can reverse the liver damage that was due to a high fructose diet (R).

Also, it can improve nonalcoholic liver disorder in mice (R).

7) Cardarine Improves Muscle Growth and Stamina

Activation of PPARẟ via GW501516 drives the development of muscle fibers in mice. These muscle fibers are associated with increased physical performance. They were able to run almost twice as long as other mice, indicating improved endurance (R).

8) Cardarine May Help Heal Skin Diseases

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Activation of PPARẟ could improve the inflammation caused by psoriasis (a skin disorder) (R).

9) Cardarine May Improve Blood Flow and Wound Healing

By activating PPARẟ, Cardarine may increase the synthesis of BH4, which increases nitric oxide production in blood vessels (eNOS) (R, R).

Increasing nitric oxide helps improve blood flow.

It also helps during wound healing (R).

10) Cardarine Has Antioxidant and Anti-inflammatory Potential

Cardarine increases the production of the antioxidant enzymes SOD1 and catalase (R).

It also inhibits the production of inflammatory molecules such as MCP-1, TNF-alphaIL-6, and NFκB (R).

The anti-inflammatory effects can improve fibrosis caused by inflammation in rats (R).

Potential Risks/Side Effects

GW 501516 increases cell death in liver cells and may cause fibrosis in mice with liver disease (R).

In animals, there is a potential risk to placental and fetal development with prolonged are large exposure to GW 501516 (R).

In rats, GW 501516 can cause cancer. There are not enough studies done on humans to show the same effect (R).

GSK abandoned further development of the drug in 2007 because animal testing showed that the drug caused cancer to develop rapidly in several organs (R).

Because GW 501516 has a vast amount of influence in a number of places in the body, you should consider its side effects before pursuing it as a treatment (R).

Dosage

A normal dosage is 2mg/kg per day to selectively activate PPARẟ (R).

Buy Cardarine

Selfhacked is not making a recommendation to buy this substance by providing this link or publishing this post.

  • Cardarine by IRC.bio – a research chemical vendor which you can buy these substances.

FDA Compliance

The information on this website has not been evaluated by the Food & Drug Administration or any other medical body. We do not aim to diagnose, treat, cure or prevent any illness or disease. Information is shared for educational purposes only. You must consult your doctor before acting on any content on this website, especially if you are pregnant, nursing, taking medication, or have a medical condition.

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21 COMMENTS

  • John

    Has anyone had experience with a reputable brand?

  • Noel

    Would it help extreme ultra endurance challenge 400km 80 hrs race?… Need back to back consume?

  • woofah

    This supplement is amazing. I am a former golden gloves champion and now body builder and alls I can says is WOW

  • Coco

    I took GW for 4 days and suddenly I got floaters in my left eye. Stopped it.
    Floaters still there but less.

  • Brian

    Excellent article on GW501516 in the Nov. 6, ’17 New Yorker.

  • Evan Walters

    Hey SelfHacked, big fan of your articles but you need to change the optimum dose of cardarine to 5-15mg per day. Thanks, Evan

  • Bill Sardi

    A 2 mg/kilogram human equivalent dose for a 154-lb. person (70 kilograms) would be 70 X 2 = 140 mg.

    This is a synthetically made molecule that inexplicably carries an FDA disclaimer as if it is a dietary supplement (which it is not).

    As a PPAR agonist it would promote growth factors which would facilitate the outcropping of new blood vessels if circulation in heart muscle (or any muscle) were impaired. It would enhance muscle building. However, it might also cause new abnormal blood vessels to outcrop at the back of the eyes (macula) and impair vision. This is why it promoted cancer growth (but did not initiate cancer). Cancer growth is driven by growth factors. For comparison, the red wine molecule resveratrol activates new blood vessels in a damaged heart to produce collateral circulation but simultaneously inhibits new blood vessel formation at the back of the eyes.

    Many of the scientific references provide inferred evidence from studies involving PPAR agonists (activators) but not GW 501516 itself.

    The author of this article discloses a financial interest.

  • Nick

    Can somebody link the incidents reported of anxiety to PPAR in the brain. The technical stuff in studies I can’t make sense of. GW users have clearly stated anxiety as a side effect. I have experienced this twice. No stimulants in the supplement. People would know if they are stimulated to anxiety.

  • Levi Mitchell

    Hi,

    Would GW come up on an military urine test ?

  • Markus

    @Christopher

    the dose was not 10 000 as high as the human equivalence dose (HED), Is was comparable to a daily HED of about just 20 mg for a 80kg/185lb human being.

    Those rats were given 2 mg/kg body weight. As rats have a higher skin area/kg plus a much higher metabolism (J/kg) one has to adjust this rate for humans. As BEZ has already stated this would be a factor. Even with negelecting those metabolic differences, just for the sake of YOUR argument, one would have to take 2mg/kg*80 kg =160 mg. That’s about 10 your proposed dosage, not the 10,000 you have mentioned. That a fu**ing difference and still damn near to the 15 mg daily you are proposing!

    BTW, there are also humans being with 50 kg body weight so that margin of error shrinks down further to your disadvantage….

  • Christopher

    Markus, The rat study actually used outrageous levels of Cardarine, not normal amounts. I believe the amount was around 10,000 times the normal dosage. The equivalent amount of aspirin to a human would probably be deadly. The rat study was way off and men have now used Cardarine every day for over a decade without side effects and unreal benefits.
    10mg Cardarine and 25 MG of Testosterone a day can prevent the average male from needing a series of cardiovascular meds, ED meds, Cholesterol Meds, etc etc. This is the reason they are suppressed by the FDA. Big pharma knows the results.

  • australopithicus

    Chris, what exactly are your qualifications to assess scientific studies and determine their validity? In the first paragraph alone you have multiple spelling errors. First line in 2nd paragraph you have spelled their when it is clearly not the place for a possessive pronoun. The spelling would be there. The first sentence in the next paragraph you are most certainly putting the previous post down and in a very condescending, arrogant, and pseudo-intellectual way. You state also that the physiology of certain animals is superior to chimps with their(note the possessive pronoun). How about a reference. Next time, how about a useful post you smug pseudo-intellectual. If we are lucky, there will not be a next time.

  • Tommix

    If this drug sooo super and cancer only in rats – so why GSK dumped this wonderful gold mine?

  • An Actual Scientist

    As far as the cancer link goes, not only is the dose high, but PPAR agonists are known to cause cancer in rats and not humans. If you give a rat one of the fibrate drugs like lopid, their livers fill with cancerous too.

    This doesn’t happen in humans because PPAR agonism doesn’t actually cause proliferation of peroxisomes. That only happens in some lower life forms like rats. Their number of peroxisomes shoots up, causing vastly increased oxidative stress which fries their dna and causes cancer.

  • Bez

    Mg/kg assumes 60kg for humans typically as it’s not actually concerned with weight but with skin area (weight is used as a simpler approximation). Anyway, 2mg/kg is still way too high of a dose and honestly it’s incredibly irresponsible that they’ve left that up. 3mg/kg was where rats in one study developed some cancers after 104 weeks. Like Markus posted then, I also assume that’s where 2mg/kg came from. Using a loose HED standard for human conversions, you multiply a rat mg/kg dose by 0.16 (an average ratio of rat size to human size) and then multiply by 60, which would be 19.2mg as equivalent to a rat sized 2mg/kg.

  • Blake

    what is the proper or best use in administering this particular chemical, cream, oral, injection? I’ve read various articles, and there hasn’t been a clear consistent understanding or explanation for that matter on the way to administer this. How should one research the best way tp purchase, maybe you can share how you are able to order and find a distributor?

  • greg

    Would be interesting to follow up the endurance athletes that have taken Gw-501516. The drug has been around since the 1990’s. A number of cyclists have taken the drug (a test was established for the drug). Would be interesting to find out if they had any long term issues. This isn’t proper science as proper cause and effect cannot be correlated definitively. However if users all had side effects there would be cause for concern.

  • Mark

    Umm, Markus, 2mg/kg would be about 160mg in the average male.

  • Inspector More-Anonymous

    2mg/kg would be an insanely high dosage in humans, humans shouldnt exceed 20mg per day. Also, it should be noted that the study that showed to cause cancer in mice is a known flawed study where the mice receive way to much GW per/kg of weight and if that were to be recreated in humans with the same ratio the levels of GW would also be extremely high, and I have a feeling thats where the 2mg/kg is coming from here

    1. Chris

      The study isn’t flawed. To a laymen it might appeared flawed but if you know how different types of animal physiology are closely related to humans in specific areas there are types of studies and research which while seemingly given in excess to the uninformed these studies are perfectly valid. Some human systems of the body more closely resemble a mouse than a chimpanzee or some other animal you ignt thing would be more relevant. Rats and rabbits also are better candidates for certain biological processes.

      So the most important lesson to learn is their was no flaw in the study. In fact that’s common for studies. There are too many variables to keep track of for experts let alone someone who only knows what they’ve read on Wikipedia when it comes to biology. Rats, mice, and rabbits are generally given larger doses because in whatever area of the body being studied one must take into account these still are not humans. They are the best analogies to humans biologists to work with (assuming human ethical standards are adhered to). So these animals have a very largely scaled down length of life and scaled up level (higher) metabolism. So it’s complete ignorance to state the study was/is flawed simply because you have a something you think is logical (the high doses given to rats) but doesn’t fit any logical processes. One, unless you have your doctorate in biology and can state the similarities in the areas that rats have with humans where increased cancer rates were seen than you may as well defend your point of view by stating anthrax vaccines have no unusual long term effects on cattle so would not on humans.

      I’m not trying to put you down or saying your statement is even wrong but I am saying your statement is without merit at best and damaging worse. Maybe in 30 years of use of this substance would have the same effect on a person when it comes to the liver as the rats in this study. And other areas where it’s detrimental (or beneficial) effects on rats in 2 years doesn’t equate into any effects on humans in 50 years.

      In fact small scale human studies in limited early phases showed some promise. But you have to remember that the studies done on rats are not at all flawed and should be taken seriously before talking about using it on the human population in general. It may prove to not show negatige effects, of at least the same negative effects at the same level.

      The last thing to keep in mind is this drug is not being designed for the athletic community. All statements made by the athletic community are usually libelous at worst or uninformed (even if well meaning) at best. If I had to chose between the athletic community or researchers at a university (who would have a vested interest in stating the drug has no drawbacks) my bet would be on the medical community. My guess is the chemical will be refined into separate drugs to do a better job at targeting specific sites in the body. Which would reduce the unnecessary risks involved with a single drug that acts at all sites in people whether they are healthy or not. So target the liver for instance instead of everything in the body. Or the brain in people showing signs of dementia. Or arteries in people with heart conditions.

      Anyway believe what you want or not about the drug’s potential side effects (I use it myself but I don’t plan to take it long term only during periods of injury or when I take too long of a break from working out). But the study is not flawed for any reason I’ve heard anyone come up with that I would consider valid. I’ve only heard severely flawed logical arguments heavily embedded in bias to keep the drug in stock because it works for athletes, again not why these drugs are developed. However after 7 hears my best bet is the study was far from flawed but the company realizes it wouldn’t make it to market as it currently is so needs to refined into separate drugs that target specific sites or simply abandoned. If the study were as flawed as you think it wouldn’t stop a pharmaceutical company from making a block buster drug (even a 1 to 2 billion dollar fine on these drugs arely makes a dent in their total profits). So no the study wasn’t flawed. Nor was it even questionable that it would translate into human cancer if a huge pharmaceutical conglomerate would simply moth ball the project.

      Again believe what you want about it causing cancer but its fact that the study was done with well established and accepted methodologies.

  • Markus

    Regarding the “normal dosage”, the 2mg/kg mentioned should refer to rat studies, so a human equi. dosage would be about 15 mg which is a dosage that is typically used by many of it’s human users-

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