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Background And Regulatory Status — Hands-On Walkthrough

By Editorial Desk · published 2026-01-10 · last reviewed 2026-01-25 · Topic

If you have been reading about GW501516 and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.

Last reviewed on 2026-01-25. 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.

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.

Regulation and Analytical Detection

Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.

Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.

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

Background and Research Context

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.

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Regulation and Detection

Cardarine is frequently described as a fat-burning or endurance-enhancing supplement, but these claims exceed the available evidence. The compound is not a hormone, steroid, or selective androgen receptor modulator. Research articles discuss it as a tool compound for studying PPARδ biology, while anti-doping literature focuses on its abuse and detection. Quality of unapproved products is uncertain, and independent analyses have found impurities or incorrect labeling. Open questions include whether human cancer risk resembles that seen in rodents and how often non-athletes use the substance.

Cardarine has no approved therapeutic indication and is not marketed as a medicine. The World Anti-Doping Agency lists GW501516 as a prohibited substance at all times, covering both in-competition and out-of-competition periods. National laws vary: some countries treat it as an unapproved drug subject to import controls, while others have specific restrictions on sale for human consumption. It is often sold as a research chemical, a label that does not imply safety or legality. Enforcement actions have targeted online vendors and shipments.

Mechanism and Detection Methods

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.

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.

Background and Regulatory History

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.

Cardarine is a common name for the investigational chemical GW501516, also written GW-1516. It was developed as a peroxisome proliferator-activated receptor delta agonist for metabolic conditions such as dyslipidemia. Early research focused on lipid handling and energy use in skeletal muscle and other tissues. The compound was never approved as a medicine. In public discussion, it is often grouped with performance-enhancing substances, although its receptor target differs from that of anabolic steroids or selective androgen receptor modulators. Regulatory and health authorities have issued warnings about its use.

Further detail

=== Fasegram === A Fasegraphy allows expanding the system of Electrocardiography diagnostic features, based on the evaluation of the speed characteristics of the process, and thereby increasing the sensitivity and specificity of ECG-diagnostics. Fasegraphy allows determining the initial features of changes in the cardiac muscle, even on a single-channel ECG, which are underestimated in traditional ECG diagnostics.

The Financial Times reported that the US pushed Pakistan to broker a temporary ceasefire in early April. The next ceasefire proposal was introduced on 5 April, amidst threats from US president Trump to destroy Iranian power plants and bridges if Iran did not re-open the Strait of Hormuz. It was reportedly negotiated between Pakistani army staff chief Asim Munir, US vice president JD Vance, US special envoy Steve Witkoff, and Iranian foreign minister Abbas Araghchi. On 7 April, Trump threatened that "A whole civilization will die tonight, never to be brought back", if Iran did not reach an agreement with the US. On 21 April, Trump announced that the US was extending the ceasefire with Iran pending negotiations, while instructing the naval blockade to remain in place and telling the military to remain prepared to resume fighting. However, Axios reported that Trump does not intend to extend the ceasefire for more than a few days. On June 11, Trump announced that a ceasefire for further 60 days was reached, that would enable the parties to negotiate all the contentious issues for a final agreement.

The lymphatic system extracts, transports and metabolizes lymph, the fluid found in between cells. The lymphatic system is similar to the circulatory system in terms of both its structure and its most basic function, to carry a body fluid.

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These cyclic dipeptides incorporate both donor and acceptor groups for hydrogen bonding. They are conformationally constrained nearly planar scaffolds. Diversity can be introduced at up to six positions and stereochemistry controlled at up to four positions. They are stable to proteolysis. These characteristics underpin theis biologically activity and utility in medicinal chemistry. As a consequence of their predominant biosynthetic origin from L-α-amino acids most naturally occurring 2,5-DKPs are cis configured as the cyclo(L-Xaa-L-Yaa) isomers. 2,5-DKPs epimerize under basic, acidic and thermal conditions. The composition of the cis and trans isomers in the equilibrium state varies widely depending on the bulk of the side chains, if a ring (e.g. proline) is present, or if the nitrogen atoms are alkylated . Although epimerization was historically an issue in the synthesis of 2,5-DKPs, several mild methods have been developed recently that avoid epimerization.

Sources: en.wikipedia.org

Background from the literature

CLE peptides are coded by the CLE genes. These peptides vary in structure, with each peptide structure performing a different job within the plant. The minimal length of functioning CLE peptides has been found to be 12 amino acids with several critical residues. There are two different peptide structures that are found within the plant and they are A-type and B-type. When A-type hormones are secreted the plant slows down the rate of root growth whereas the secretion of B-type peptides effects the vascular growth of the plant. The secretion of A-type peptides speeds up the vascular development of the plant that is mediated by the B-type peptides. This suggests that these two types of peptides work together to regulate the growth of the plant. The specific peptides are: A-type peptides B-type peptides CLE 41/44/TDIF CLE 42 CLE 43 CLE 46

Abnormal basal metabolic rate refers to a high or low basal metabolic rate (BMR). It has numerous causes, both physiological (part of the body's normal function) and pathological (associated with disease). An abnormal basal metabolic rate is not necessarily indicative of disease; a number of physiological factors can alter the BMR by influencing cellular metabolic activity. For instance, males are more likely than females to have a high BMR, and in women, the BMR may rise to abnormal levels during pregnancy or lactation. An individual's BMR varies greatly with age: infants and children typically have a high BMR, required for growth, while the elderly have a low BMR. Tall, thin people have a higher BMR than their shorter counterparts, even with the same weight, due to the greater surface area of their skin. The metabolic rate also decreases during sleep and increases in exercise, and individuals who exercise regularly have a higher BMR than those who are sedentary. Environmental temperature also has an effect: the BMR is increased in both heat and cold.

Guillaume made several guest appearances on sitcoms, including Good Times, The Jeffersons, Sanford and Son, Saved by the Bell: The College Years and in the 1990s sitcoms The Fresh Prince of Bel-Air and A Different World. Guillaume also played Dr. Franklin in season 6, episode 6 ("Chain Letter") of the series All in the Family, in which he coyly referenced Marcus Welby, M.D., a TV series in which he had guest-starred in 1970. His series-regular debut was on the ABC series Soap, playing Benson, a butler, from 1977 to 1979. Guillaume continued the role in a spin-off series, Benson, which ran for 158 episodes from 1979 until 1986. In 1985, Guillaume appeared in the television mini-series North and South as abolitionist leader Frederick Douglass, who escaped from slavery and became a leader of the anti-slavery movement prior to the American Civil War. He also appeared as marriage counselor Edward Sawyer on The Robert Guillaume Show (1989), Detective Bob Ballard on Pacific Station (1991–1992), and television executive Isaac Jaffe on Aaron Sorkin's short-lived but critically acclaimed Sports Night (1998–2000). Guillaume suffered a mild stroke on January 14, 1999, while filming an episode of the latter series. He recovered and his character was later also depicted as having had a stroke. He also made a guest appearance on 8 Simple Rules for Dating My Teenage Daughter.

Oxitriptan, also known as L-5-hydroxytryptophan (5-HTP) and sold under various brand names, is a medication and over-the-counter dietary supplement used in the treatment of depression and for other indications. It is taken by mouth. Side effects of oxitriptan include appetite loss, nausea, diarrhea, vomiting, and serotonin syndrome. The drug is a centrally permeable monoamine precursor and prodrug of serotonin and hence acts as a serotonin receptor agonist. Chemically, oxitriptan is an amino acid and a tryptamine. Oxitriptan has been used clinically since at least the 1970s.

Sources: en.wikipedia.org

Reference notes

=== United Kingdom === In the U.K., as with all other vertebrates and some invertebrates, any scientific procedure which is likely to cause "pain, suffering, distress or lasting harm" is regulated by the Home Office under the Animals (Scientific Procedures) Act 1986. U.K. regulations are considered amongst the most comprehensive and rigorous in the world. Detailed data on the use of laboratory mice (and other species) in research in the U.K. are published each year. In the U.K. in 2013, there were a total of 3,077,115 regulated procedures undertaken on mice in scientific procedure establishments, licensed under the Act.

the Kremlin walls Zemlyanoy Gorod (Earthwork Town) the Kamer-Kollezhsky Rampart the Garden Ring the small railway ring The Moscow Ring Road (MKAD) has been Moscow's boundary since 1960. Similarly circular are the main Moscow subway line, the Ring Line, and the so-called Third Automobile Ring (which was completed in 2005). Thus, radial and circular planning continues to define Moscow's development. However, contemporary Moscow has also absorbed a number of areas outside the MKAD—such as Solntsevo, Butovo, and the town of Zelenograd. Part of Moscow Oblast's territory was merged into Moscow on 1 July 2012; as a result, Moscow is no longer fully surrounded by Moscow Oblast, and the city now shares a border with Kaluga Oblast. In total, Moscow gained about 1,500 square kilometers (580 sq mi) and 230,000 inhabitants. Moscow's Mayor Sergey Sobyanin praised this expansion as helping Moscow and the neighboring region, a "mega-city" of 20 million people, to develop "harmonically". Each administrative okrug and district has its own coat of arms and flag, as well as an individual leader. In addition to the districts, there are Territorial Units with Special Status. These units usually include areas with small or no permanent populations. Examples include the All-Russia Exhibition Centre, the Botanical Garden, large parks, and industrial zones. In recent years, some territories have been merged with other districts. Moscow has no ethnic-specific areas, such as the Chinatowns in certain North American and East Asian cities.

Glutathione synthetase deficiency (GSD) is a rare autosomal recessive metabolic disorder that prevents the production of glutathione. Glutathione helps prevent damage to cells by neutralizing harmful molecules generated during energy production. Glutathione also plays a role in processing medications and cancer-causing compounds (carcinogens), and building DNA, proteins, and other important cellular components.

Lebrikizumab, sold under the brand name Ebglyss, is a humanized monoclonal antibody used for the treatment of atopic dermatitis (atopic eczema). It is an interleukin 13 antagonist. It is given by subcutaneous injection. The most common side effects include injection site reactions, dry eye and conjunctivitis, including allergic conjunctivitis. Lebrikizumab was approved for medical use in the European Union in November 2023, in Canada in June 2024, and in the US in September 2024.

Although it has expanded outward from its original geographic base, most new restaurants are located in suburban areas of the Southern US. Since 1997, the Atlanta-based company has sponsored the Peach Bowl, an annual college football bowl game played in Atlanta on New Year's Eve. Chick-fil-A also sponsors the Southeastern Conference and the Atlantic Coast Conference of college athletics. In 2008, Chick-fil-A was among the first fast-food restaurants to become completely free of trans fats. In October 2015, the company opened its largest restaurant, a three-story 5,000 square feet (460 m2) restaurant in Manhattan.

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.

Is cardarine legal to buy?

Legal status varies by country, but cardarine is not approved as a medicine in major jurisdictions. It is often sold as a research chemical, a category that may not be lawful for human use. Buyers should check local laws and product labels carefully.

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