Amidst the several products and supplements for weight management, some of them have achieved a significant standard or status. Cardarine (GW501516) is one of these products because it is a newly developed supplement suitable for research (due to usage and clinical applications).
However, despite all the properties and benefits of this supplement, a few considerations are related to its usage. For professional athletes, the use of Cardarine (GW501516) is somehow discouraged on account of its associated actions.
This article will be focusing on the scientific evidence related to the use of Cardarine (GW501516), its potential benefits, and its side effects.
- Generic Name — Cardarine
- Group – Investigational, Experimental
- Type – Small molecule
- Molecular formula – C21H18F3NO3S2
- Molecular weight – 453.498 g/mol
What is Cardarine (GW501516)?
Cardarine (GW501516) is a SARM (selective androgen receptor modulator) that acts as the AR (androgen receptor) agonist. The development of Cardarine (GW501516) was to treat aging, HIV, AIDS, cancer, and muscle wasting. Cardarine is useful for building lean muscle mass in individuals who cannot engage in extraneous physical activities either due to age or any medical condition. Originally, this drug was referred to as Endurobol due to its capability to increase physical endurance during running and racing.
According to clinical evidence, Cardarine helps in increasing skeletal muscle mass and mitochondrial biogenesis. An increase in biogenesis causes the cell to produce more energy in comparison to the individuals who aren’t taking these supplements. Initially, Cardarine was also called a ‘fitness pill’ due to its exceptional physical benefits and results.
Cardarine (GW-501516) is a synthetic molecule developed as the SARM. Selective androgen receptor modulators belong to the novel classification of drugs that tend to mimic the action of testosterone. However, SARMs do not produce side effects associated with testosterone hormone in the body.
Testosterone is the hormone (androgenic) that is responsible for the development of secondary male characteristics. According to the different research pieces, Cardarine helps improve the endurance of professional athletes by enhancing the saturation of oxygen in their muscles. This drug also helps burn the fat, which can be helpful for people who are aiming to reduce the percentage of body fat.
Cardarine is often confused as the SARM, but Cardarine is Peroxisome Proliferator-Activated Receptor (PPARδ) agonist. Regular consumers of the Cardarine drug claim that this supplement has several positive effects on the vascular system.
The composition of cardarine consists of monocarboxylic acid (also known as Endurobol). Cardarine is the member (chemically) of 1,3-thiazoles, which belongs to the organofluoride compounds. Moreover, 1,3-thiazole is an aromatic ether and an aryl sulfide. Moreover, Cardarine is an oral supplement that requires a proper exercise regimen for its proper digestion. Cardarine is used during periods of dryness to eliminate the fat cells in the body. This action helps in quicker fat loss without loss of muscle mass.
Discovery of Cardarine:
In 1992, Cardarine was initially developed due to collaboration between Ligand Pharmaceuticals and GSK. In the year 2001, the Proceedings of the National Academy of Sciences of US published its discovery and reported that this drug was developed by the use of structure-based drug design and combinatorial chemistry.
In the era of 2000s, R&D Focus Drug News reported the phase-1 trial of this drug for the intervention of hyperlipidemia via GSK. The same trial underwent a phase-2 trial two years later, in 2002. In the year 2003, Ligand Pharmaceuticals successfully earned a one million dollar payment due to continuing phase-1 development of the GSK. By the year 2007, Cardarine went through successful phase-2 trials related to cardiovascular disease, dyslipidemia, diabetes, and obesity.
Later, according to the report in The Wall Street Journal and The New York Times, a higher dosage of Cardarine was found helpful in boosting physical performance in the mice. At first, the investigation of Cardarine was halted due to a few cancer-causing side effects of Cardarine during animal testing. Recently, Cardarine has gained popularity in enhancing endurance, lean muscle mass, and physical performance among humans.
Mechanism of action:
Before going further in detail, there is a need to be a bit technical in describing the mechanism of action of Cardarine.
Cardarine (GW501516) was initially developed in the scientific labs by the collaboration of two pharmaceutical companies. Our bodies consist of nuclear receptors, which are approximately the size of a few molecules. These nuclear receptors are responsible for getting sensations for the different compounds and steroids. When a nuclear receptor touches any specific compound, it triggers different biological functions.
One of this family’s most significant nuclear receptors is PPAR (Peroxisome proliferator-activated receptor). These receptors are divided into delta and beta groups (Greek letters as δ and β). Cardarine works by the activation of the PPAR-δ receptors in the human body.
In human fat tissues and muscles, PPAR-δ receptors tend to play two customized functions. In the fat tissues or adipose tissues, PPAR-δ receptors tend to increase the oxidation to aid in burning fat fast. On the other hand, in muscle tissues, PPAR-δ receptors increase muscle fiber action and fat burning during the exercise.
Clinical applications of Cardarine:
A few most significant applications and uses of Cardarine are:
- Enhanced brain health:
According to one of the early animal studies, Cardarine helps better blood circulation and reduces oxidative stress in the brain. Cardarine has both anti-inflammatory and pro-inflammatory effects on the inflammation of the brain cells. A few inflammatory cells as TNF-alpha tend to decrease in concentration in the presence of the Cardarine.
In some cases, Cardarine can also increase the IL-6 concentration, but the benefits of Cardarine outweigh its harms.
- Weight management and obesity control:
According to a research study conducted on the six obese volunteers, Cardarine had the association with a reduction in the symptoms of metabolic syndrome in the patients. These participants significantly decreased liver fat (20% decrease) and improved insulin resistance (11%).
Moreover, fat concentration dropped in the blood by 23-30% as:
- 30% decrease in the triglycerides
- 26% decrease in APOB (Apolipoprotein B) and VLDL (very low-density lipoprotein)
- 23% decrease in the LDL (low-density lipoprotein)
In different animal studies, Cardarine has significant evidence of increasing the concentration of HDL, improving insulin sensitivity, and reducing LDL concentration. These effects have, however, less scientific evidence in humans.
- Antioxidant and anti-inflammatory properties:
Generally, activation of PPAR-delta receptors tends to suppress the inflammation in the body. By activating PPAR-delta receptors, Cardarine can reduce the inflammation of the liver in animals.
According to some researchers, Cardarine blocks a few substances involved in the inflammatory responses and reduces the inflammatory gene’s activity.
In animal studies, consumption of Cardarine has a potent association with the reduction in inflammatory markers as NFκB, IL-6, TNF-alpha, and MCP-1.
An application of Cardarine on the skin is associated with improving diabetic wound healing due to a reduction in inflammation. Cardarine also increases the production of antioxidant enzymes such as catalase and SOD1.
- Vasculature effects:
Other than reducing cholesterol levels, Cardarine can directly affect the vasculature (blood vessels) in the body.
According to animal studies, Cardarine can prevent oxidative damage in blood vessels. Furthermore, Cardarine helps in reducing the risk of buildup of plaques in the arteries. Cardarine increases the concentration of blood vessels-relaxing and protective nitric oxide in the arteries. Nitric oxide causes vasodilation to regulate blood flow and circulation. Low Cardarine dosage causes a reduction in inflammation and tissue damage in the arteries. Low Cardarine dosage helps clear up the blood vessels. Thus, it reduces the risk of complications and heart diseases.
Cardarine also increases the production of new blood vessels in the human heart cells. VEGF (vascular endothelial growth factor) angiogenesis supports blood vessels to keep the smooth flow of blood in the body. This action of the VEGF is beneficial for patients with cardiovascular diseases. However, there should be restrictions on Cardarine consumption in cancer patients because angiogenesis in the cancer cells causes tumor proliferation.
- Improved stamina and muscle growth:
According to one study, PPAR-delta activation through Cardarine increases muscle fibers development in the human body. Development of the muscle fibers enhances the physical performance and endurance in an individual twice as compared to the individual not taking it.
- Liver damage:
The liver is one of the basic targets of the Cardarine. The liver has a significant role in burning, releasing, and storing fats in the body. PPAR-delta activation causes the switch of energy source by the liver from glucose to FA (fatty acids), which reduces blood sugar levels.
According to the cell studies, cardarine exposed cells have significantly less production of IL-6, which helps prevent insulin resistance. In animal studies, cardarine had less liver damage and was less likely to have non-alcoholic fatty liver diseases.
Dosage of Cardarine:
Generally, the recommended dosage of Cardarine is about 10-20 mg of drug per day for about six-eight weeks. Cardarine is available in both powder and capsule forms. The best way to consume the Cardarine is in the powder form by mixing it with the water and taking sips of the mixture throughout the day. Cardarine consumption doesn’t exert additional pressure on the body and vital organs.
During the initial consumption of the Cardarine, you should start with a 5-10 mg dosage of the drug. With time, you can increase it by 5-mg to the recommended dose. In this way, you can reduce the risk of side effects on the body if you are allergic and don’t know.
How long does it take for the Cardarine to work?
Cardarine is a potent drug with quicker effects and good body health and performance prognosis. You can witness the initial improvements after consuming the drug for at least two weeks daily.
The half-life of cardarine is about 24-hours in the human body to participate in different functions.
Is the consumption of Cardarine legal?
Cardarine has a few restrictions for selling and purchasing this product compared to the other products. Cardarine is not legal for its consumption in humans. A few side-effects are associated with the Cardarine, making it unsuitable for legal status. However, several athletes and bodybuilders take this drug to boost energy levels and endurance in the body. Organizations such as WADA (world anti-doping agency) have issued several warnings regarding the consumption and associated toxicity of the drug in the human body.
Does Cardarine cause potential side effects such as baldness and hair loss?
Generally, Cardarine is safe to use and provides beneficial benefits for the body. It doesn’t cause any side effects like hair loss and baldness in the consumers.
What do you need to consider while you are consuming Cardarine?
There are a few important considerations that you need to focus on while you are consuming these supplements as:
- Regular exercise – during the oral consumption of the cardarine (either in the form of powder or capsules), you need to focus on physical activity. The exercises and increased physical activity helps in increased efficiency of the metabolic system to improve digestion and yield benefits.
- Water consumption – while taking the drug orally, you need to double the water intake on a daily basis. An increased water consumption aids in the good absorption and digestion of the drug inside the GI tract. Moreover, it also aids in reducing the risk of acidity associated with the supplements.
Cardarine is a potential drug developed to enhance physical performance and fat burning. However, in the initial stages, the developer companies halted the clinical trials and research due to evidence of cancer-causing agents due to the consumption of cardarine.
Despite different safety warnings, Cardarine is quite popular among athletes and bodybuilders. Consumers claim that this product can instantly boost muscle growth, burn fat, and improve endurance. Different animal studies suggest that Cardarine is beneficial for improving the function of metabolism, brain, renal system, and musculoskeletal system. Different companies and anti-doping agencies recommend intensive care while consumption of these drugs which instantly improve physical performances in the athletes.
- Is, W. I. Cardarine Supplement Tips (Diet & Pre Workout Dosage Guide) Categories.
- Rice, R. Y. What Supplements Can I Take To Improve Cholesterol?–Dr. Khash Farzam.
- Weihrauch, M., & Handschin, C. (2018). Pharmacological targeting of exercise adaptations in skeletal muscle: Benefits and pitfalls. Biochemical pharmacology, 147, 211-220.
- Kintz, P., Ameline, A., Gheddar, L., & Raul, J. S. (2020). Testing for GW501516 (cardarine) in human hair using LC/MS–MS and confirmation by LC/HRMS. Drug testing and analysis, 12(7), 980-986.
- Kadayat, T. M., Shrestha, A., Jeon, Y. H., An, H., Kim, J., Cho, S. J., & Chin, J. (2020). Targeting peroxisome proliferator-activated receptor delta (PPARδ): a medicinal chemistry perspective. Journal of Medicinal Chemistry, 63(18), 10109-10134.
- Mitchell, J. A., & Bishop-Bailey, D. (2019). PPAR β/δ a potential target in pulmonary hypertension blighted by cancer risk. Pulmonary circulation, 9(1), 2045894018812053.
- Contreras, F., Romero, B., Suárez, N., González, M., Fouillioux, C., Guevara, E., … & Velasco, M. (2002). Gw501516 Sarms Fabricante polvo crudo Cardarine CAS: 317318-70-0 Endurobol Gw 501516. Archivos Venezolanos de Farmacología y Terapéutica, 21(2), 148-155.
- Hwai, H. (2019). PPAR-δ GW501516.
- Park, J., & Kim, J. Y. (2021). Cardarine (GW501516) Effects on Improving Metabolic Syndrome. Journal of Health, Sports, and Kinesiology, 2(2), 22-27.
- Trevisiol, S., Moulard, Y., Delcourt, V., Jaubert, M., Boyer, S., Tendon, S., … & Bailly‐Chouriberry, L. (2021). Comprehensive characterization of the peroxisome proliferator activated receptor‐δ agonist GW501516 for horse doping control analysis. Drug Testing and Analysis, 13(6), 1191-1202.
- McVeigh, J., Salinas, M., & Ralphs, R. (2021). A sentinel population: The public health benefits of monitoring enhanced body builders. International Journal of Drug Policy, 95, 102890.
- Whitaker, D. L., Geyer-Kim, G., & Kim, E. D. (2021). Anabolic steroid misuse and male infertility: management and strategies to improve patient awareness. Expert Review of Endocrinology & Metabolism, 16(3), 109-122.
- Read, M. F., & Zone, B. The Ultimate Guide To Sarms.
- Ainsworth, N. P., Shelley, J., & Petróczi, A. (2018). Current Trends in Performance-and Image-Enhancing Substance Use Among Gym Goers, Exercisers, and Athletes. In Handbook of Novel Psychoactive Substances (pp. 56-89). Routledge.
- Fink, J., Schoenfeld, B. J., Hackney, A. C., Matsumoto, M., Maekawa, T., Nakazato, K., & Horie, S. (2019). Anabolic-androgenic steroids: procurement and administration practices of doping athletes. The Physician and sportsmedicine, 47(1), 10-14.
Disclaimer: “This product is intended for medical research purposes only. This product is not for human consumption. You must be a licensed and qualified healthcare practitioner to work with this product.”