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Identity And Regulatory Status — Field Notes

By Editorial Desk · published 2026-03-10 · last reviewed 2026-04-15 · Blog

Everything below concerns GW501516. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Last reviewed on 2026-04-15. Where a claim depends on a specific study, the study is described rather than over-claimed.

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.

Cardarine as Investigational PPARδ Agonist

The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.

Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.

Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.

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

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.

In the fitness and bodybuilding literature, cardarine is frequently discussed as an endurance agent or fat-loss compound, although such claims are not supported by robust clinical evidence. Online descriptions often mix animal data, user anecdotes, and marketing language. Researchers who study PPARδ agonists distinguish between receptor activation in controlled experiments and unsupervised use of unverified products. The latter introduces unknown purity, dose, and interactions, making reported experiences difficult to interpret scientifically.

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Mechanism and Laboratory Detection

Published human data are sparse and mostly come from early-phase trials. Those studies examined short-term changes in lipids, glucose, and exercise capacity, but they were not large enough to establish efficacy or long-term safety. Some animal experiments reported increased running endurance, yet such findings do not prove a performance benefit in people. Anti-doping laboratories detect GW501516 and its metabolites in urine or blood using liquid chromatography-tandem mass spectrometry. Detection windows depend on dose, sample type, and individual metabolism. The method is sensitive enough to identify trace residues in tested samples.

Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.

GW501516 binds and activates PPARδ, a nuclear receptor that influences transcription of genes involved in fatty acid oxidation and energy use. Activation shifts some metabolic pathways in preclinical models, which is why the compound has been studied for lipid disorders and exercise-related endpoints. The exact downstream effects in humans are incompletely mapped. PPARδ is expressed in many tissues, including skeletal muscle, liver, and adipose tissue, so broad activation may have varied consequences. Researchers continue to examine how selective or partial activation might alter the balance between benefits and risks.

Regulatory Status and Detection Context

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.

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.

Identity and Pharmacological Classification

PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.

Published studies have examined GW501516 in animal models of obesity, insulin resistance, and exercise endurance. Early human trials reportedly ended, and development was discontinued after preclinical findings raised concerns about cancer in some rodent studies. Regulatory agencies have not approved cardarine for any medical use. Its availability through non-pharmaceutical channels raises questions about identity, purity, and legal status that are separate from its laboratory pharmacology. Those questions are often addressed through analytical testing rather than assumptions about product labels.

Notes from published material

In 2015, the Department of Defense released an updated cyber strategy memorandum detailing the present and future tactics deployed in the service of defense against cyberwarfare. In this memorandum, three cybermissions are laid out. The first cybermission seeks to arm and maintain existing capabilities in the area of cyberspace, the second cybermission focuses on prevention of cyberwarfare, and the third cybermission includes strategies for retaliation and preemption (as distinguished from prevention). One of the hardest issues in cyber counterintelligence is the problem of cyber attribution. Unlike conventional warfare, figuring out who is behind an attack can be very difficult.

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More recent publications have defined the usually recommended doses as 50 mg DMT and 100 mg harmaline orally. Besides DMT with harmaline, the properties and effects of oral DMT in combination with harmine have also been studied by Jonathan Ott. He found that the threshold dose was 20 or 30 mg DMT and 120 mg harmine orally. Shulgin also reported in TiHKAL that 35 to 40 mg DMT and 140 to 190 mg harmine were unmistakably active, whereas smaller doses of 30 mg DMT and 120 to 140 mg harmine orally were inactive. In notable contrast to harmaline, harmine does not have its own psychoactive effects when used at doses of up to at least 300 mg orally. In pharmahuasca, the harmala alkaloid is usually taken first and then DMT is taken 15 to 20 minutes later, although a shorter or longer interval may also be employed. The onset of oral DMT with an MAOI is within 1 hour and its duration is 4 to 6 hours.

Alexander of the United States Army Intelligence and Security Command; Hal Puthoff, of SRI International in California; remote viewer Ingo Swann and the subsequent Stargate Project, at Fort Meade in Maryland; Keith Harary, who worked with Russell Targ. Narrated by Jim Schnabel, produced by Alex Graham, directed by Bill Eagles, made by Wall to Wall Television 3 September Cybersecrecy, the mathematician Fred Piper of the Information Security Group; the UK gave out Enigma machines to Commonwealth countries for secret telecommunications, without telling these countries that the UK could read every message; Phil Zimmermann, inventor of the PGP encryption algorithm; Simon Davies (privacy advocate); when at MIT in 1976, Whitfield Diffie found how to make encryption much more secure, to have public key encryption; Mark Rotenberg; Dorothy E. Denning, and criminal methods of encryption; Wayne Madsen (journalist); Ross J. Anderson of the Department of Computer Science and Technology, University of Cambridge and how the (French-designed) A5/1 encryption for the European mobile network in the 1990s had weak security; journalist Stephen Dorril; the NSA's Clipper chip; journalist James Bamford, author of The Puzzle Palace; a documentary in the style of Panorama. Produced by David Frank, directed by Martin Durkin, made by RDF Media 10 September Guru Busters investigates the activities of people in India who claim to have mystical powers. Producer and directed by Robert Eagle, narration by Art Malik, production company Eagle & Eagle.

Sources: en.wikipedia.org

Further detail

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Upregulation An increase in the number or sensitivity of receptors on a neuron, often in response to reduced stimulation or drug exposure. A mechanism of plasticity. Utricle A structure within the vestibular system that detects linear acceleration and head position relative to gravity. Works in tandem with the saccule. Uveitis Inflammation of the uveal tract (including the iris, ciliary body, and choroid), which can cause visual disturbances and is sometimes associated with autoimmune neurological disorders.

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.

What is cardarine?

Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.

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