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Identity And Pharmacological Mechanism — Evidence Review

By Editorial Desk · published 2026-01-30 · last reviewed 2026-02-13 · Faq

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.

Updated 2026-02-13. Numbers and descriptions here follow the published literature rather than marketing material.

Identity and Pharmacological Mechanism

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.

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.

Cardarine at a glance

PropertyValueNotes
Chemical classSynthetic PPARδ agonistNot a steroid or a selective androgen receptor modulator.
Common synonymsCardarine, GW501516, GW-501516, endurobolNames vary by supplier and literature source.
AppearanceWhite to off-white powderConsistent with many small-molecule research chemicals.
SolubilityLow in water; soluble in DMSO and ethanolOften prepared in organic solvent for laboratory work.
Primary targetPPARδ (NR1C2)Nuclear receptor involved in lipid and energy metabolism.

Detection and Regulatory Landscape

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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Identity and Regulatory Status

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.

Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.

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.

Mechanism and Research Context

GW501516 acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in transcription of genes related to lipid handling and energy use. Activation of PPARδ can shift skeletal muscle toward greater fatty acid oxidation in animal models, which is one reason it drew interest for metabolic disease and exercise research. The exact downstream effects depend on tissue, species, dose, and duration. Human data are sparse, so many proposed benefits remain hypotheses rather than established clinical outcomes.

Laboratory studies have examined GW501516 in cell cultures and rodents for conditions such as dyslipidemia, insulin resistance, and obesity. Some trials in humans were initiated, but development was discontinued after preclinical findings raised concerns about cancer in certain models. Those findings do not prove that the compound causes cancer in people, but they contributed to regulatory caution. Later reviews often describe the evidence as preliminary and insufficient for assessing long-term safety.

Regulatory Status and Detection Context

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.

Analytical laboratories typically identify cardarine and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is a common matrix in anti-doping testing, while blood and tissue may be used in research settings. Detection windows depend on the assay, the sample matrix, and the compound's metabolism. Because cardarine is extensively metabolized, laboratories often target specific metabolites to improve sensitivity and confirmation. Reference standards are required for reliable quantification. Method validation includes checks for selectivity, linearity, and carryover.

Notes from published material

A small 2002 study demonstrated that treatment twice daily for six weeks with crude onion juice from Australian brown onion, re-growth hair on alopecia areata (spot baldness) in 86.9% of the 23 participants. Twice as many flavonols are found in red onion than in yellow onion. Also, non-organic onions might contain pesticides on the peel and in the first scaly leaf. Compounds found in onion that stimulate hair growth:

=== Pulp stones === Pulp stones are calcified masses that occur in the pulp, either in the apical or coronal portions. They are classified according to their structure or location. According to their location, pulp stones can be classed either as free (completely surrounded by pulp), embedded (surrounded by dentine tissue) or adherent (attached to pulp wall continuous with dentine, but not fully enclosed). Depending on the structure, they are either true (dentine lined by odontoblasts), false (formed from degenerating cells that mineralise) or diffuse (more irregular in shape to false stones). The aetiology of pulp stones is little understood. It has been recorded that pulpal calcifications can occur due to:

Juan Calvete draws attention to this with explicitly when detailing the history of venomics. He declares that ''the last revolutions made in venomics research in the last decade (1989–1999) are the direct result of advancements made in proteomic-centered methods and the indirect result of more widely available and cost-effective forms of transcriptomics and bio-informatics analysis''. One of the first popular research topics of venomics was the pharmacological properties of the polypeptide toxins found in snake venom (Specifically, Elapidae and Hydrophidae) due to the neurotoxic properties and their ability to cause respiratory failure in animals. However, due to the lack of competent technology, less complex techniques (such dialysis to separate the venom), followed by simplistic chromatography and electrophoresis analysis, research was limited.

==== Political franchise ==== The principal ideological disagreement Socialist Studies has with the SPGB is its attitude towards attempts by workers living under political dictatorships to establish elementary democratic and trade union rights, especially in Eastern Europe in the 1980s and early 1990s. The stance of the SPGB since 1939 is summarised by the following 1990 party conference resolution:This Conference re-affirms the stand taken in the September [actually October] 1939 Socialist Standard and repeated in the September 1989 Socialist Standard, that the Socialist Party of Great Britain wholeheartedly supports the efforts of workers everywhere to secure democratic rights against the powers of suppression. Whilst we avoid any association with parties or political groups seeking to administer capitalism, we emphasise that freedom of movement and expression, the freedom to organise in trade unions, to organise politically, and to participate in elections, are of great importance to all workers and are vital to the success of the socialist movement. On the other hand, Socialist Studies regards the struggle by workers living under a dictatorship to establish some measure of political democracy as a reformist struggle which socialists should oppose. They believe that the difference between democratic capitalist governments and dictatorial capitalist governments is of no significance to workers, that political democracy is not essential for the propagation of socialist ideas and that workers in dictatorships should not directly confront the forces of suppression.

Sources: en.wikipedia.org

Further detail

Homo sapiens FGFR1 oncogene partner 2 (FGFR1OP2), transcript variant 1, mRNA (NCBI) Homo sapiens FGFR1 oncogene partner 2 isoform 1 (NCBI) FGFR1OP2 human gene location in the UCSC Genome Browser. FGFR1OP2 human gene details in the UCSC Genome Browser.

==== Commander of the Order of the British Empire (CBE) ==== Military Division Royal Navy Captain Paul Branscombe, . Captain William Keith Hutchison. Captain Keith Frank Read. Army Major General Cedric Norman George Delves, , (485712), late The Devonshire and Dorset Regiment. Brigadier Kevin John Watson Goad, , (472543), late Royal Army Ordnance Corps. Colonel (Acting Brigadier) Keith Skempton (487055), late The Cheshire Regiment. Colonel (Acting Brigadier) Albert Edward Whitley, , (495259), late Corps of Royal Engineers. Royal Air Force Group Captain Roger Hubert Beazley, , (Retired). Group Captain George William Gibson, (Retired). Air Commodore Ernest William Tyack. Civil Division John Edwin Adshead. For services to the National Training Awards and to Vocational Training. Nicholas Kenneth Alston, Assistant Secretary, Ministry of Defence. Michael Day Beaumont, . For political and public service. Arthur John Armstrong Bell. For political and public service. Alastair John Bellingham, Professor of Haematology, King's College Hospital School of Medicine and Dentistry. For services to Medicine and to the Royal College of Pathologists. Professor Sushantha Kumar Bhattacharyya, Professor of Manufacturing Systems Engineering, University of Warwick. For services to Industry and to Technology. John David Stuart Brown, . For political and public service. Christopher John Skidmore Burd. For services to the Forestry Industry. David Thomas Burke, Expert Special Adviser on the Environment, Department of the Environment. David Adam Cairns, Music Critic, The Sunday Times.

In 1953, scientists at the Sloan Kettering Institute in New York City demonstrated that cigarette tar painted on the skin of mice caused fatal cancers. This work attracted much media attention; the New York Times and Life both covered the issue. The Reader's Digest published an article entitled "Cancer by the Carton". On January 11, 1964, the United States Surgeon General's Report on Smoking and Health was published; this led millions of American smokers to quit, the banning of certain types of advertising, and required warning labels on tobacco products. These results were first widely accepted in the medical community and publicized among the general public in the mid-1960s. The medical community's resistance to the idea that smoking tobacco caused disease has been attributed to bias from nicotine-dependent doctors, the novelty of the adaptations needed to apply epidemiological techniques and heuristics to non-infectious diseases, and cigarette industry pressure. The harmful health effects of smoking have been significant for the development of the science of epidemiology. As the mechanism of carcinogenicity is radiomimetic or radiological, the effects are stochastic. Definite statements can be made only on the relatively increased or decreased probabilities of contracting a given disease. For a particular individual, it is impossible to definitively prove a direct causal link between exposure to a radiomimetic poison such as tobacco smoke and the cancer that follows; such statements can only be made at the aggregate population level.

Sources: en.wikipedia.org

Supporting material

Vaccines typically contain attenuated, inactivated or dead organisms or purified products derived from them. There are several types of vaccines in use. These represent different strategies used to try to reduce the risk of illness while retaining the ability to induce a beneficial immune response.

=== Acting === Shawn's involvement with theater began in 1970 when he met Andre Gregory, who has since directed several of his plays. As a stage actor, he has appeared mostly in his own plays and other projects with Gregory. He made his film debut in 1979, playing Diane Keaton's ex-husband in Woody Allen's Manhattan and an insurance agent in Bob Fosse's All That Jazz. His best-known film roles include Earl in Strange Invaders (1983) and Mr. Hall in Clueless (1995). After seeing his performance in My Dinner with Andre (1981), casting director Janet Hirshenson was so fond of his delivery of the word "inconceivable" that she cast him as Vizzini in The Princess Bride (1987), for whom the word is a catchphrase. Other roles include Baron Von Westphalen in Southland Tales, Cyrus Rose on Gossip Girl, Marty in Vegas Vacation (1997), and Ezra in The Haunted Mansion (2003).

== Chemistry == ETH-LAD, also known as 9,10-didehydro-N,N,6-triethylergoline-8β-carboxamide or as 6-ethyl-6-nor-LSD, is a substituted lysergamide derivative related to lysergic acid diethylamide (LSD; also known as METH-LAD). It is the 6-ethyl derivative of nor-LSD (6-nor-LSD; H-LAD) and is the derivative of LSD with an ethyl group instead of methyl group at the 6 position of the ergoline ring system.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

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.

How does cardarine interact with the body?

It binds to and activates PPARδ, a nuclear receptor that regulates genes related to fatty acid oxidation and energy use. This activation alters transcription in tissues such as skeletal muscle and liver. The full range of downstream effects in humans is not fully established.

Is cardarine found naturally?

No, cardarine is not known to occur naturally in plants, animals, or humans. It is a synthetic molecule produced for laboratory research. Products labeled as cardarine should therefore be treated as manufactured chemicals with variable purity.

What did animal studies show?

Rodent studies reported increased endurance and fat oxidation after GW501516 exposure. Long-term studies also found higher rates of some tumors, which led to halted development.

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