GW-501516 (Cardarine)

Cardarine (or GW 501516) is a SARM invented in the 90s via research conducted by GlaxoSmithKline and Ligand Pharmaceuticals (1). Initially it was developed to hinder and remedy the formation of tumors in the breasts, prostate & large intestines and to aid in cardiovascular diseases. As research continued further, individuals using the drug realized it enhanced their endurance levels and they had improvements in stamina notably in cardiovascular exercises.

Due to these effects the popularity of Cardarine soared especially among bodybuilders, athletes and sportsmen. As more research on the drug continued, more uses and advantages were discovered such as burning of excess fatty tissue, aiding recovery, improving endurance and aiding in muscle development.

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Studies from as recent as 2015 showed that the drug forms pro-inflammatory markers in specific tissues and reduces the rate of the metabolic formation of fat (lipogenesis). This makes the body to have the ability to stop the formation of fatty acid chains which would subsequently be stored as fat.


How it Works

Cardarine works by attaching to the Peroxisome Proliferator Activator Receptor (PPAR). These receptors are transcription factors which belong to a nuclear hormone receptor family. GW-501516 only binds to PPAR delta found in specific tissues in the body. PPAR delta occurs mainly in the adipose tissue (located in the bone marrow), underneath the skin, around multiple organs, in breast tissue and in the brain.

When these transcription factors (PPAR delta) area activated by cardarine, a lot of systems inside the body can be affected. Specifically, the activation of PPAR delta results to an interaction with the PGC-1a enzyme which regulates the expression of proteins that are involved in energy use. In short, it allows the body to be able to handle extremely high levels of energy use than usual.

The process results in a high metabolism of fatty acids in rats (2). In monkeys it resulted in the raising of good cholesterol and lowering of bad cholesterol.

cardarine studies
Treatment of wild-type and ob/ob mice with GW501516 enhanced the increase in plasma GLP-1 level after an oral glucose load and improved glucose tolerance

Health Benefits of Cardarine/GW501516

1.      Brain Protection

The brain can suffer from oxidative stress which can be caused by its inability to get rid of toxins, inefficiency in fending off bacteria in the immune system or lack of proper formation of energy from glucose. The activation of PPAR delta by cardarine fuels the development of new nerve cells which can aid the brain when it’s under oxidative stress. It protects blood vessels from the oxidative stress. Cardarine also assists the brain blood vessels in reducing the chances of vessel dysfunction.

2.      Benefits the Heart

Oxidative stress can hamper the levels of oxidation in the blood that the heart pumps. It also expresses responses that trigger indifferences in the expression of genetics, cellular hypertrophy and death of cells. These three conditions are common in heart failure patients. Cardarine helps by preventing inflammatory buildups in the coronary arteries. The drug is rich in nitric acid which lowers the likelihood of inflammation.

In animal studies, cardarine increases the levels of High Density Lipoprotein (HDL) cholesterol (also known as ‘the good cholesterol’) and lowering the levels of Low Density Cholesterol (LDL) otherwise known as ‘the bad cholesterol’ (3). It also causes a decrease in triglycerides. This can potentially mean a decrease the risk of cardiovascular disease in humans.

cardarine (gw-501516) research
Low-density lipoprotein cholesterol (LDL-C) response over time by treatment of GW-501516 VS Placebo

3.      It reduces Kidney Inflammation

Lab experiments on mice have shown that cardarine aids in the reduction in the amount of inflammation in the kidney cells. The drug accomplishes this by reducing the expression of MCP-1 which can cause kidney disease. Limiting the expression of MCP-1 is beneficial to diabetes patients.

4.      It helps the immune system

GW 501516 suppresses of inflammation in multiple organs in the body such as the skin, immune cells (red blood cells, T cells, platelets, and white blood cells) and the colon. GW 501516 achieves after activating PPAR delta which suppresses inflammation by regulating molecules which add to inflammatory responses.

Active PPAR delta also shield specific skin cells from cell death while the body is undertaking a wound healing process in that skin area.

Cardarine also helps to fasten the closure of a diabetic wound.

5.      It prevents Liver Damage

The activation of PPAR delta by Cardarine makes the liver to go from using glucose as the energy source to fatty acids. This results in a reduction in blood sugar and reduces the chances of overworking the liver.

Cardarine helps to prevent insulin resistance in liver cells by inhibiting an interleukin (IL-6). Il-6 stimulates the inflammatory and auto-immune responses found in diseases like arthritis and diabetes.

6.      Boosts Stamina and Muscle Growth

The activation of PPAR delta by GW-501516 results to an increase in the number of muscle fibers in the body. Generation of energy in the muscles leads to athletes and weightlifters to have more stamina. The combination of having more energy and lasting longer can result to athletes, bodybuilders and weightlifters to boost their muscle growth.

7.      Wound Healing, Skin Diseases and Improving Blood Flow

The activation of PPAR delta could improve the inflammation in a skin affected by a skin disorder.

Additionally, the activation of PPAR delta results in an increase in the production of BH4 which in turn increases the production of Nitric Oxide in the blood vessels. Nitric oxide assists in improving blood flow in the body and it also aids in the process of wound healing.

Potential Health Risks

  • GW 501516 increases the death of liver cells, studies have shown that it may be a cause of Fibrosis among mice with liver disease.
  • Prolonged exposure to GW 501516 in animals resulted to a risk to the development of the placenta and fetus.
  • It causes Cancer in rats after exposure to ridiculously large amounts of GW 501516. The same correlation is yet to be established in humans.

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Recommended Daily Dosage

The recommended dosage per day is 2mg/kg. This will be sufficient to activate PPAR delta

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Cardarine aka GW 501516 is hands down one of the best performance enhancing drug around due to the price and efficiency. It has many good uses and benefits to the body. Like any other drug, it has side effects with a potential for harming the body but its ups far outweigh the downs.


  1. Cardarine (GW 501516), 2015, Kai Bogartti, Banned Nutrition
  2. PPARβ/δ Activation Induces Enteroendocrine L Cell GLP-1 Production – Gastroenterology Gastroenterology, Volume 140, Issue 5, May 2011, Pages 1564-1574
  3. Lipid Effects of Peroxisome Proliferator-Activated Receptor-Δ Agonist GW501516 in Subjects With Low High-Density Lipoprotein Cholesterol – Arteriosclerosis, Thrombosis, and Vascular Biology. 2012;32:2289-2294. Originally published August 15, 2012