GW501516 raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.
This page was last updated on 2026-07-24 and is reviewed periodically as new material appears.
Sporting authorities added GW501516 to prohibited lists after it appeared in athlete samples and online markets. The World Anti-Doping Agency classifies it as a hormone and metabolic modulator, and its use can lead to an anti-doping rule violation. Some early laboratory work suggested effects on fatty acid oxidation and endurance-related metabolism in animals, but those findings do not establish safe or effective use in people. Reports of adverse events in humans are scarce and often anecdotal, which complicates risk assessment.
Legal status varies by country. In some places, cardarine is controlled under medicines or psychoactive substances laws; in others, it may be sold with minimal oversight as a research chemical. Customs agencies have intercepted shipments, and several national health agencies have issued warnings about products marketed for bodybuilding or performance enhancement. The lack of a standardized pharmaceutical supply means identity, purity, and contamination levels can differ widely between samples. These factors make cardarine a regulatory and public health concern rather than a conventional prescription drug.
Cardarine is a common name for GW501516, a synthetic compound first described in the 1990s as a selective agonist of the peroxisome proliferator-activated receptor delta. It was studied in preclinical models for metabolic and cardiovascular conditions, but it has not been approved as a medicine in the United States, Europe, or other major jurisdictions. Retail products labeled as cardarine are generally research chemicals or supplements, not pharmaceutical formulations. Because human safety and efficacy data remain limited, regulatory agencies treat it as an unapproved substance rather than a therapeutic product.
The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.
Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.
Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.
| Property | Value | Notes |
|---|---|---|
| IUPAC name | {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid | Systematic name for GW501516 |
| CAS Registry Number | 317318-70-0 | Unique identifier for the parent compound |
| Molecular formula | C21H18F3NO3S2 | Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur |
| Molecular weight | 453.5 g/mol | Approximate value for the neutral form |
| Appearance | White to off-white powder | Typical description for purified laboratory material |
GW501516 acts on PPARδ, a nuclear receptor that helps regulate fatty acid oxidation and energy homeostasis. In animal studies, activation of this receptor was associated with increased endurance and changes in lipid metabolism. Human trials examined effects on blood lipids and other metabolic markers, but the compound did not advance to approval. Rodent studies later reported tumors in multiple tissues at doses used in those experiments. Whether those findings translate to human risk remains uncertain, and the clinical relevance of the animal data is still debated.
Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.
A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.
Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.
=== The Mixers clan === The Mixers (also known as the Sebabti crime family), is a Moroccan crime family made up of five brothers who were born in Borgerhout, Antwerp, and originate from Berkane in north-eastern Morocco. The Mixers are suspected of having collaborated with Colombian cartels, where they had the role of smuggling drugs through the Port of Antwerp, and supplying criminal organisations all over Europe. The organisation became active in the early 2000s, and they are considered to be the oldest drug trafficking network which is still active in Antwerp. They are also considered to be one of the 5 Moroccan drug clans who control the cocaine trade in the port of Antwerp. The Mixers are seen by Belgian politicians as one of the most dangerous Belgian drug networks in the country, due to their excessive criminal staff and large numbers of people who are hired in exchange for large sums of money. In the summer of 2018, one of the Mixers was spotted in Tangier driving an exclusive Bentley Continental GT. In 2017, the Port of Antwerp once again broke an intercepted drug record. The Mixers were among the main suspects. The Belgian special services have joined forces with the Moroccan authorities to investigate this family in Morocco. The Moroccan police intercepted €10.2 million in cash in a €400,000 apartment in Tangier, alongside a villa in Berkane, as well as several luxury boats on the Saïdia coast. In 2019, a significant number of bombs and grenades were thrown in several neighbourhoods of Antwerp which were aimed at rival gangs.
== External links == Association of Biomolecular Resource Facilities ABRF Federation of American Societies for Experimental Biology FASEB ABRF Discussion Forum Journal of Biomolecular Techniques ABRF at LinkedIn Leadership
=== Stress === Sustained stress can lead to high levels of circulating cortisol (regarded as one of the more important of the several "stress hormones"). Women show larger increases in cortisol than men when chronically stressed.
== Treatment == The mainstay of treatment for GPS is plasmapheresis, a procedure in which the affected person's blood is sent through a centrifuge and the various components are separated based on weight. The plasma contains the anti-GBM antibodies that attack the affected person's lungs and kidneys, and is filtered out. The other parts of the blood (the red blood cells, white blood cells, and platelets) are recycled and intravenously reinfused. Most individuals affected by the disease also need to be treated with immunosuppressant drugs, especially cyclophosphamide, prednisone, and rituximab, to prevent the formation of new anti-GBM antibodies to prevent further damage to the kidneys and lungs. Other, less toxic immunosuppressants such as azathioprine may be used to maintain remission.
=== Nucleic acids === The convention for a nucleic acid sequence is to list the nucleotides as they occur from the 5' end to the 3' end of the polymer chain, where 5' and 3' refer to the numbering of carbons around the ribose ring which participate in forming the phosphate diester linkages of the chain. Such a sequence is called the primary structure of the biopolymer.
Sources: en.wikipedia.org
=== Multiple sclerosis === Multiple sclerosis (MS) is a neurodegenerative disease in which the immune system attacks myelin, a protective covering of nerve fibers in the central nervous system, causing communication problems between the brain and the rest of the body. Symptoms can include fatigue, difficulty walking, numbness or tingling, muscle weakness, and problems with coordination and balance. MS is associated with an increased risk of central nervous system cancer, primarily in the brain.
Mitsubishi and Mitsui were involved in the opium trade during the Japanese occupation of China. Mao Zedong government is generally credited with eradicating both consumption and production of opium during the 1950s using unrestrained repression and social reform. Ten million addicts were forced into compulsory treatment, dealers were executed, and opium-producing regions were planted with new crops. Remaining opium production shifted south of the Chinese border into the Golden Triangle region. The remnant opium trade primarily served Southeast Asia, but spread to American soldiers during the Vietnam War; based on a study of opiate use in soldiers returning to the United States in 1971, 20 percent of participants were dependent enough to experience withdrawal symptoms.
== Approval history == The US FDA New Drug Application (NDA) was granted approval in May 2012, for use in adults. The US FDA Supplemental New Drug Application (sNDA) for pediatric use was granted approved in August 2014. In Israel, the Israeli Ministry of Health granted approval in September 2012. In Brazil, the Brazilian Health Surveillance Agency (ANVISA) granted approval in March 2013. In Canada, Health Canada issued a Notice of Compliance in May 2014, for both adults and pediatric patients. Taliglucerase alfa is made by the Israeli biotherapeutics company Protalix and sold by the American pharmaceutical company Pfizer.
==== Invertebrates ==== Nematodes that survive below 0 °C include Trichostrongylus colubriformis and Panagrolaimus davidi. Cockroach nymphs (Periplaneta japonica) survive short periods of freezing at -6 to -8 °C. The red flat bark beetle (Cucujus clavipes) can survive after being frozen to -150 °C. The fungus gnat Exechia nugatoria can survive after being frozen to -50 °C, by a unique mechanism whereby ice crystals form in the body but not the head. Another freeze-tolerant beetle is Upis ceramboides. See insect winter ecology and antifreeze protein. Another invertebrate that is briefly tolerant to temperatures down to -273 °C is the tardigrade. The larvae of Haemonchus contortus, a nematode, can survive 44 weeks frozen at -196 °C.
Sources: en.wikipedia.org
The molecular evolution of vampire bat venom highlights the dominant contributions of Draculin and DSPA to its anticoagulant and proteolytic functions. Transcriptomic and proteomic data from the submaxillary glands of Desmodus rotundus show active expression of Draculin at both the RNA level and the corresponding protein production level. Venom secretion, containing Draculin and the desmoteplase salivary plasminogen activator DSPA, enables vampire bats to sustain a hawmatophagous lifestyle by disrupting the prey's normal physiological and biochemical responses during feeding. Vampire bats frequently revisit the same host for repeated feedings, and typically relick the wound for approximately 30 minutes per fe feeding, prolonging exposure of host tissues to salivary components. The parasitic nature of vampire bat feeding, coupled with the extensive application of saliva to the wound and the antigenic properties of the anticoagulants, can trigger an acquired immune response in the bat's prey. Although prey animals have been known to develop acquired immunological resistance to Draculin over prolonged exposure, the frequent site-directed or focul [sic?] mutagenesis with the venom limits the rapid evolution of such resistance.
CB1 receptors are found primarily in the brain, particularly in the basal ganglia, limbic system, hippocampus, and striatum. They are also present in the cerebellum, and male and female reproductive systems, but absent in the medulla oblongata, which controls respiratory and cardiovascular functions. CB1 is also found in the human anterior eye and retina.
21°Bx = 200 mg N/L 23°Bx = 250 mg N/L 25°Bx = 300 mg N/L 27°Bx = 350 mg N/L However, other studies have shown successful fermentation be conducted with YAN levels below these recommendations as well as sluggish/stuck fermentations occurring even when YAN levels are in line with recommendations.
===== MeSH D08.811.913.555 – one-carbon group transferases (EC 2.1) ===== MeSH D08.811.913.555.150 – amidinotransferases MeSH D08.811.913.555.275 – carboxyl and carbamoyl transferases MeSH D08.811.913.555.275.200 – aspartate carbamoyltransferase MeSH D08.811.913.555.275.600 – ornithine carbamoyltransferase MeSH D08.811.913.555.400 – hydroxymethyl and formyl transferases MeSH D08.811.913.555.400.100 – aminomethyltransferase MeSH D08.811.913.555.400.300 – glutamate formimidoyltransferase MeSH D08.811.913.555.400.500 – glycine hydroxymethyltransferase MeSH D08.811.913.555.400.625 – phosphoribosylaminoimidazolecarboxamide formyltransferase MeSH D08.811.913.555.400.750 – phosphoribosylglycinamide formyltransferase MeSH D08.811.913.555.500 – methyltransferases MeSH D08.811.913.555.500.100 – acetylserotonin n-methyltransferase MeSH D08.811.913.555.500.175 – betaine-homocysteine S-methyltransferase MeSH D08.811.913.555.500.250 – catechol O-methyltransferase MeSH D08.811.913.555.500.350 – dna modification methylases MeSH D08.811.913.555.500.350.500 – dna (cytosine-5-)-methyltransferase MeSH D08.811.913.555.500.350.700 – site-specific dna-methyltransferase (adenine-specific) MeSH D08.811.913.555.500.350.850 – site-specific dna methyltransferase (cytosine-specific) MeSH D08.811.913.555.500.387 – glycine N-methyltransferase MeSH D08.811.913.555.500.425 – guanidinoacetate N-methyltransferase MeSH D08.811.913.555.500.500 – histamine N-methyltransferase MeSH D08.811.913.555.500.625 – homocysteine S-methyltransferase MeSH D08.811.913.555.500.645 – 5-methyltetrahydrofolate-homocysteine s-methyltransferase MeSH D08.811.913.555.500.650 – nicotinamide N-methyltransferase MeSH D08.811.913.555.500.700 – phenylethanolamine N-methyltransferase MeSH D08.811.913.555.500.710 – phosphatidyl-N-methylethanolamine N-methyltransferase MeSH D08.811.913.555.500.712 – phosphatidylethanolamine N-methyltransferase MeSH D08.811.913.555.500.800 – protein methyltransferases MeSH D08.811.913.555.500.800.400 – histone-lysine n-methyltransferase MeSH D08.811.913.555.500.800.650 – o-6-methylguanine-DNA methyltransferase MeSH D08.811.913.555.500.800.750 – protein-arginine n-methyltransferase MeSH D08.811.913.555.500.800.800 – protein o-methyltransferase MeSH D08.811.913.555.500.800.800.700 – protein d-aspartate-l-isoaspartate methyltransferase MeSH D08.811.913.555.500.862 – thymidylate synthase MeSH D08.811.913.555.500.925 – trna methyltransferases
Lipoate–protein ligase (EC 2.7.7.63, LplA, lipoate protein ligase, lipoate–protein ligase A, LPL, LPL-B) is an enzyme with systematic name ATP:lipoate adenylyltransferase. This enzyme catalyses the following chemical reaction
Sources: en.wikipedia.org
No. Major drug regulators have not approved GW501516 for treating any medical condition. Products sold as cardarine are typically unapproved research chemicals or supplements, so their contents and safety are not assured.
It is prohibited by the World Anti-Doping Agency as a hormone and metabolic modulator. Athletes who test positive for GW501516 can face sanctions, including suspensions and loss of results.
Cardarine is a common or trade-style name, while GW501516 is the research code for the same chemical entity. Some sources also use Endurobol or GSK-516. The names refer to the same compound, not distinct drugs.
Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.