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Background And Regulatory Status — Evidence Review

By Editorial Desk · published 2025-09-21 · last reviewed 2025-10-11 · Topic

GW501516 comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.

Last reviewed on 2025-10-11. Where a claim depends on a specific study, the study is described rather than over-claimed.

Background and Regulatory Status

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.

Background and Research Context

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.

In laboratory settings, cardarine is studied as a tool compound for probing PPARδ biology. Published experiments often use cell cultures, rodent models, or isolated tissues. Some investigations focus on metabolic effects, while others assess potential risks such as carcinogenicity observed in long-term animal studies. Because human trials are sparse, most knowledge comes from preclinical work and adverse event reports. Scientific literature frequently notes the gap between animal findings and human outcomes. The compound is not a dietary supplement and is not intended for human consumption.

Cardarine at a glance

PropertyValueNotes
IUPAC name{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acidSystematic name for GW501516
CAS Registry Number317318-70-0Unique identifier for the parent compound
Molecular formulaC21H18F3NO3S2Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur
Molecular weight453.5 g/molApproximate value for the neutral form
AppearanceWhite to off-white powderTypical description for purified laboratory material

Mechanism and Detection Methods

GW501516 acts as a selective agonist at PPARδ, a nuclear receptor that regulates transcription of genes involved in lipid handling and energy metabolism. Activation of PPARδ in preclinical models increases fatty acid oxidation, mitochondrial biogenesis, and exercise endurance in rodents. These effects have made the compound a subject of metabolic research and also a target for sport anti-doping rules. In humans, however, controlled studies are limited, and whether similar endurance or metabolic changes occur at tolerated exposures remains an open question. The receptor’s broad tissue distribution also means downstream effects may vary by organ and condition.

Detection of GW501516 in biological samples generally relies on liquid chromatography coupled with tandem mass spectrometry. Urine is a common matrix in anti-doping analysis, while blood or plasma may be used in research settings. Sample preparation can involve enzymatic hydrolysis, protein precipitation, or solid-phase extraction before instrumental analysis. Because the compound undergoes metabolism, assays may target the parent molecule, one or more metabolites, or both. Detection windows are not fixed; they depend on factors such as dose, route, individual metabolism, and assay sensitivity. Reference standards are required for accurate identification and quantification.

Handling and quality assessment of cardarine reference material follow general laboratory practices for poorly characterized compounds. It typically appears as a white to off-white powder and is sparingly soluble in water but soluble in organic solvents such as dimethyl sulfoxide and ethanol. Storage recommendations usually specify a cool, dry, dark place, with long-term storage at low temperature and desiccation. Purity may be checked by high-performance liquid chromatography with ultraviolet detection, while identity is confirmed by mass spectrometry and nuclear magnetic resonance. No pharmacopeial monograph exists, so reported purity and stability depend on the supplier’s methods.

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Mechanism and Detection

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.

Further detail

Lichens are defined by the International Association for Lichenology to be "an association of a fungus and a photosynthetic symbiont resulting in a stable vegetative body having a specific structure". The fungi, or mycobionts, are mainly from the Ascomycota with a few from the Basidiomycota. In nature, they do not occur separate from lichens. It is unknown when they began to associate. One or more mycobiont associates with the same phycobiont species, from the green algae, except that alternatively, the mycobiont may associate with a species of cyanobacteria (hence "photobiont" is the more accurate term). A photobiont may be associated with many different mycobionts or may live independently; accordingly, lichens are named and classified as fungal species. The association is termed a morphogenesis because the lichen has a form and capabilities not possessed by the symbiont species alone (they can be experimentally isolated). The photobiont possibly triggers otherwise latent genes in the mycobiont. Trentepohlia is an example of a common green alga genus worldwide that can grow on its own or be lichenised. Lichen thus share some of the habitat and often similar appearance with specialized species of algae (aerophytes) growing on exposed surfaces such as tree trunks and rocks and sometimes discoloring them.

=== Control strategies === There is no known method of eradication or control for invasive Cercopagis pengoi. Containing the spread to new areas is the only form of management. Stricter ballast water regulations and awareness would prevent the spread. The C. pengoi invasion of the Great Lakes occurred after the United States passed a regulation requiring ships exchange freshwater ballast water with ocean water to kill off potential invaders. This means that either the resting eggs remain viable even after boats filled with ballast water switch out their ballast water in the ocean, or the required ballast water regulations are not being followed, or the species was brought into the Great Lakes in no-ballast-on-board (NOBOB) vessels (the most like possibility). NOBOB vessels carry only residual water (<50000L) but were not required to exchange ballast water at the time of Cercopagis' invasion. Locally C. pengoi spread can be limited by only releasing bait or bait water into the water body where the bait was originally collected. Boat owners should wash their boats and equipment with high pressure and hot water (above 40 °C) to limit the spread of adult C. pengoi. Alternatively boats and equipment should be allowed to dry for at least five days before moving to another body of water.

Refers to the testing of experimental drugs in the test tube or in animals - the testing that occurs before trials in humans may be carried out. (NLM) Research using animals to find out if a drug, procedure, or treatment is likely to be useful. Preclinical studies take place before any testing in humans is done. (NCI) Predictive factor

Sources: en.wikipedia.org

Supporting material

Founder and lately Teacher, Harmanli Refugee Camp Play School, Bulgaria. For services to the Humanitarian Support of Refugee Children in Bulgaria. Sadie Clasby-Jarrous. Founder and lately Manager, Harmanli Refugee Camp Play School, Bulgaria. For services to the Humanitarian Support of Refugee Children in Bulgaria. Timothy Robert Conibear. Founder, Waves for Change. For services to Young People Overseas. John David Crouch. Lately Technical Works Supervisor, British Embassy Mogadishu, Somalia. For services to the UK Government Overseas. Sophie Louise Dyer. Lately Counsellor, Trade Policy, British Embassy Tokyo, Japan. For services to Trade. Deborah Carol Edgington. Councillor for Tourism, Fuerteventura, Canary Islands, Spain. For services to British Nationals in Fuerteventura. Richard John Field. Independent Voluntary and Charity Worker in rural Uganda. For services to Young People and Health in Uganda. Kelly Teresa Fisher. Professional Pool, Snooker and English Billiards player. For services to Sport. Nigel James Fossey. Principal, The Sultan's School, Oman and formerly Headmaster, King´s College School, Panama. For services to British Education Overseas. Lowri Mai Griffiths. Head, Ocean Policy Unit, Legal Directorate, Foreign, Commonwealth and Development Office. For services to Ocean Protection. Joanne Margaret Hare. Deputy Director, Foreign, Commonwealth and Development Office. For services to National Security. Elizabeth Ann Haydon. Head, Harrow International School, Hong Kong. For services to British Education in the UK and Hong Kong. Frank Alexander Menzies-Hearn.

=== By U-Pb age discordance === Before applying detrital zircon ages, they should be evaluated and screened accordingly. In most cases, data are compared with U-Pb Concordia graphically. For a large dataset, however, data with high U-Pb age discordance (>10 – 30%) are filtered out numerically. The acceptable discordance level is often adjusted with the age of the detrital zircon since older population should experience higher chances of alteration and project higher discordance. (See Uranium–lead dating)

But when he finally presented his results he reported an excess heat of only one degree Celsius, a result that could be explained by chemical differences between heavy and light water in the presence of lithium. He had not tried to measure any radiation and his research was derided by scientists who saw it later. For the next six weeks, competing claims, counterclaims, and suggested explanations kept what was referred to as "cold fusion" or "fusion confusion" in the news. In April 1989, Fleischmann and Pons published a "preliminary note" in the Journal of Electroanalytical Chemistry. This paper notably showed a gamma peak without its corresponding Compton edge, which indicated they had made a mistake in claiming evidence of fusion byproducts. Fleischmann and Pons replied to this critique, but the only thing left clear was that no gamma ray had been registered and that Fleischmann refused to recognize any mistakes in the data. A much longer paper published a year later went into details of calorimetry but did not include any nuclear measurements. Nevertheless, Fleischmann and Pons and a number of other researchers who found positive results remained convinced of their findings. The University of Utah asked Congress to provide $25 million to pursue the research, and Pons was scheduled to meet with representatives of President Bush in early May. On 30 April 1989, cold fusion was declared dead by The New York Times. The Times called it a circus the same day, and the Boston Herald attacked cold fusion the following day.

Sources: en.wikipedia.org

Notes from published material

=== (Dis)Honesty: The Truth About Lies === Directed by Yael Melamede and released in 2015, (Dis)Honesty: The Truth About Lies is a documentary film exploring dishonesty in contemporary society. Ariely presents the film, offering analysis on the psychological mechanisms that drive deceit. With references to behavioral experiments and anecdotes—from athletic and academic cheating to political scandals—Ariely draws on his research on behavioural economics and irrationality to shed light on why and how people lie. Numerous people make appearances in the documentary, including the author and marketer Ryan Holiday, to share their personal experiences with dishonesty and lies.

Soybean meal is used in food and animal feeds, principally as a protein supplement, but also as a source of metabolizable energy. Typically 1 bushel (i.e. 60 lbs. or 27.2 kg) of soybeans yields 48 lbs. (21.8 kg) of soybean meal. Most soybean meal is defatted, produced as a co-product of soybean oil extraction. Some, but not all, soybean meal contains ground soybean hulls. Soybean meal is heat-treated during production, to denature the trypsin inhibitors of soybeans, which would otherwise interfere with protein digestion.

===== Digital wallet scheme ===== Paetongtarn has overseen the implementation of the 10,000-baht digital wallet scheme, the flagship economic policy of the Pheu Thai Party. The scheme was originally promised during the 2023 election campaign as a one-time universal handout to nearly all Thais aged 16 and over, intended to deliver a large-scale stimulus to the domestic economy. However, since the Paetongtarn government took office, the program has faced significant modifications, delays, and criticism regarding its funding, implementation, and economic necessity. The initial plan to fund the 500 billion baht scheme through a special loan bill was scrapped due to legal concerns and fears of violating fiscal discipline laws. Instead, the government has relied on the national budget. The universal nature of the handout was also curtailed, with eligibility restrictions introduced to exclude high-income earners (those with an annual income over 840,000 baht) and individuals with more than 500,000 baht in savings. Phase 1, launched in September 2024, provided 10,000 baht in cash to approximately 14.5 million recipients, including state welfare cardholders and individuals with disabilities. Phase 2, implemented between January and April 2025, extended the cash transfers to an estimated 3 million senior citizens aged 60 and over. The first truly "digital" phase, which was set to target around 2.7 million young people aged 16–20 via a government application, has been indefinitely postponed.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine approved for human use?

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.

Why is cardarine banned in sport?

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.

What is the difference between cardarine and GW501516?

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.

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist developed for research. It has not been approved as a medication in any country. It is classified as an unapproved drug and a prohibited substance in sport.

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