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Identity And Regulatory Status — Explained

By Editorial Desk · published 2026-02-10 · last reviewed 2026-03-18 · News

A practical reference on GW501516: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

This page was last updated on 2026-03-18 and is reviewed periodically as new material appears.

Identity and Regulatory Status

Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.

Cardarine is a common name for GW501516, an investigational compound developed in the 1990s for metabolic conditions. It acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in lipid and energy metabolism. The compound is frequently mislabeled as a selective androgen receptor modulator, or SARM, but its molecular target is different. GW501516 reached early clinical testing before development was discontinued. It has no approved therapeutic use in any country. The name cardarine is not a formal international nonproprietary name.

Background and Regulatory History

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.

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.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516; GW-1516; endurobolGW501516 is the research code
Drug classPPARδ agonistNot a selective androgen receptor modulator
Molecular formulaC21H18F3NO3S2Established chemical formula
Molar mass453.5 g/molCalculated from the formula
Regulatory statusProhibited in sport; not approved as medicineStatus varies by country

Detection and Regulatory Landscape

A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.

Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.

Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.

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Mechanism and Detection

Anti-doping laboratories identify GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the usual matrix, and detection can occur after the parent compound has cleared from blood. The exact detection window depends on dose, formulation, individual metabolism, and assay sensitivity. Because the compound is prohibited at all times, athletes are subject to testing in and out of competition. Analytical methods continue to improve as new metabolites and designer analogs are characterized.

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.

Preclinical Findings and Safety Signals

Safety concerns emerged from long-term animal studies. In rodents given the compound for extended periods, researchers found an increased incidence of certain cancers, including liver and bladder tumors. These findings contributed to the discontinuation of clinical development. Whether similar risks apply to short-term or low-level exposure in humans is not established, and controlled human safety data are limited. The relevance of high-dose rodent carcinogenicity findings to human use remains a subject of debate.

Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.

Laboratory studies indicate that GW501516 activates PPARδ, a nuclear receptor involved in fatty acid oxidation and energy metabolism. In rodent experiments, treated animals often showed increased endurance and reduced fat mass. These effects were observed under controlled conditions and do not establish safe or effective use in humans. The exact dose-response relationship in humans remains poorly characterized. Species differences in metabolism can affect how results translate across animals and people.

Further detail

Examples of vertebrate and invertebrate necrophages (species names and dietary information with supporting references) from Zenodo datasets Maggot medicine (a video on maggot therapy) from National Geographic The museum in lockdown: who feeds the beetles (a video on dermestid beetles) from the Natural History Museum Eternal horizons (a podcast on sky burial) from BBC Audio

Li R, Bianchet MA, Talalay P, Amzel LM (1995). "The three-dimensional structure of NAD(P)H:quinone reductase, a flavoprotein involved in cancer chemoprotection and chemotherapy: mechanism of the two-electron reduction". Proc. Natl. Acad. Sci. U.S.A. 92 (19): 8846–50. Bibcode:1995PNAS...92.8846L. doi:10.1073/pnas.92.19.8846. PMC 41064. PMID 7568029.

== Competitions == The ARL controls the National Rugby League and NRL Women's Premiership as well as annual representative competitions such as the State of Origin series, the Indigenous All Stars Match, the Affiliated States Championship and the Women's National Championships. The ARL previously ran the National Youth Competition. This competition, which was for male players Under 20 years of age, was replaced in 2018 by state-run competitions. The New South Wales Rugby League run the Jersey Flegg Cup for male Under 21 players. The Queensland Rugby League run the Mal Meninga Cup for male Under 18 players, with players Under 21 that are outside NRL squads playing for clubs in the open-age Queensland Cup.

=== Snapping === Snapping involves two separate parts of the thread, both containing a bulky group. one part of the thread is then threaded to the macrocycle, forming a semi rotaxane, and end is closed of by the other part of the thread forming the rotaxane.

=== Pacific islands === During an El Niño event, New Zealand tends to experience stronger or more frequent westerly winds during their summer, which leads to an elevated risk of drier than normal conditions along the east coast. There is more rain than usual though on New Zealand's West Coast, because of the barrier effect of the North Island mountain ranges and the Southern Alps. Fiji generally experiences drier than normal conditions during an El Niño, which can lead to drought becoming established over the Islands. However, the main impacts on the island nation is felt about a year after the event becomes established. Within the Samoan Islands, below average rainfall and higher than normal temperatures are recorded during El Niño events, which can lead to droughts and forest fires on the islands. Other impacts include a decrease in the sea level, possibility of coral bleaching in the marine environment and an increased risk of a tropical cyclone affecting Samoa. In the late winter and spring during El Niño events, drier than average conditions can be expected in Hawaii. On Guam during El Niño years, dry season precipitation averages below normal, but the probability of a tropical cyclone is more than triple what is normal, so extreme short duration rainfall events are possible. On American Samoa during El Niño events, precipitation averages about 10 percent above normal, while La Niña events are associated with precipitation averaging about 10 percent below normal.

Sources: en.wikipedia.org

Supporting material

Alpha cells are endocrine cells, meaning they secrete a hormone, in this case glucagon. Alpha cells store this glucagon in secretory vesicles that typically have an electron dense core and a grayish outer edge. It is believed that alpha cells make up approximately 20% of endocrine cells within the pancreas. Alpha cells are most commonly found on the dorsal side of the pancreas and are very rarely found on the ventral side of the pancreas. Alpha cells are typically found in compact Islets of Langerhans, which are themselves typically found in the body of the pancreas. Alpha cells function in the maintenance of blood glucose levels. Alpha cells are stimulated to produce glucagon in response to hypoglycemia, epinephrine, amino acids, other hormones, and neurotransmitters.

An ion-exchange membrane is a semi-permeable membrane that transports certain dissolved ions, while blocking other ions or neutral molecules. Ion-exchange membranes are therefore electrically conductive. They are often used in desalination and chemical recovery applications, moving ions from one solution to another with little passage of water. Important examples of ion-exchange membranes include the proton-exchange membranes, that transport H+ cations, and the anion exchange membranes used in certain alkaline fuel cells to transport OH− anions.

Though no new elements (apart from einsteinium and fermium) could be detected in the nuclear test debris, and the total yields of transuranium elements were disappointingly low, these tests did provide significantly higher amounts of rare heavy isotopes than previously available in laboratories. For example, 6×109 atoms of 257Fm could be recovered after the Hutch detonation. They were then used in the studies of thermal-neutron induced fission of 257Fm and in discovery of a new fermium isotope 258Fm. Also, the rare isotope 250Cm was synthesized in large quantities, which is very difficult to produce in nuclear reactors from its progenitor 249Cm; the half-life of 249Cm (64 minutes) is much too short for months-long reactor irradiations, but is very "long" on the explosion timescale.

Under certain circumstances, non-cognate amino acids will be charged, resulting in mischarged or misaminoacylated tRNA. These mischarged tRNAs must be hydrolyzed in order to prevent incorrect protein synthesis. While aa-tRNA serves primarily as the intermediate link between the mRNA coding strand and the encoded polypeptide chain during protein synthesis, it is also found that aa-tRNA have functions in several other biosynthetic pathways. aa-tRNAs are found to function as substrates in biosynthetic pathways for cell walls, antibiotics, lipids, and protein degradation. It is understood that aa-tRNAs may function as donors of amino acids necessary for the modification of lipids and the biosynthesis of antibiotics. For example, microbial biosynthetic gene clusters may utilize aa-tRNAs in the synthesis of non-ribosomal peptides and other amino acid-containing metabolites.

Enzymes like proteases, lipases, and amylases have an important role in the soaking, dehairing, degreasing, and bating operations of leather manufacturing. Proteases are the most commonly used enzymes in leather production. The enzyme must not damage or dissolve collagen or keratin, but should hydrolyze casein, elastin, albumin, globulin-like proteins, and nonstructural proteins that are not essential for leather making. This process is called bating. Lipases are used in the degreasing operation to hydrolyze fat particles embedded in the skin. Amylases are used to soften skin, to bring out the grain, and to impart strength and flexibility to the skin. These enzymes are rarely used.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a SARM?

No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.

Is cardarine approved for human use?

No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.

Why was its development discontinued?

Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.

Is cardarine a selective androgen receptor modulator?

No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.

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