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Background And Regulatory History — Reference Sheet

By Editorial Desk · published 2026-06-14 · last reviewed 2026-07-01 · Info

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

Reviewed 2026-07-01. Anything still debated is marked as such rather than presented as settled.

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.

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.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineCommon internet and media name.
Research codeGW501516Also written GW-1516.
Drug classPPARδ agonistNot a selective androgen receptor modulator.
Development statusDiscontinuedClinical development halted after rodent cancer findings.
Regulatory statusProhibited in sportListed by WADA; not approved as medicine.

Mechanism and Detection

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.

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.

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Preclinical Findings and Safety Signals

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.

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.

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.

Cardarine is a common name for GW501516, also GW-1516, a synthetic compound developed as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. It belongs to a class of agents that modulate gene transcription related to lipid and energy metabolism. The compound was studied in preclinical and early clinical research for metabolic and cardiovascular conditions, but it did not progress to approved therapeutic use. Its name appears in fitness and sports contexts despite not being approved as a drug.

Notes from published material

== History == MD was originally developed in the early 1950s, following earlier successes with Monte Carlo simulations—which themselves date back to the eighteenth century, in the Buffon's needle problem for example—but was popularized for statistical mechanics at Los Alamos National Laboratory by Marshall Rosenbluth and Nicholas Metropolis in what is known today as the Metropolis–Hastings algorithm. Interest in the time evolution of N-body systems dates much earlier to the seventeenth century, beginning with Isaac Newton, and continued into the following century largely with a focus on celestial mechanics and issues such as the stability of the Solar System. Many of the numerical methods used today were developed during this time period, which predates the use of computers; for example, the most common integration algorithm used today, the Verlet integration algorithm, was used as early as 1791 by Jean Baptiste Joseph Delambre. Numerical calculations with these algorithms can be considered to be MD done "by hand".

To reinforce his intentions for the Smithsonian, Henry established laboratories, developed a robust physical sciences library, and started the Smithsonian Contributions to Knowledge, the first of many publications intended to disseminate research results. For Henry, the Library of Congress was the obvious choice as the national library. Unable to resolve the conflict, Henry dismissed Jewett in July 1854. In 1865, the Smithsonian building, also called the Castle due to its Norman architectural style, was severely damaged by fire. This incident presented Henry with an opportunity related to the Smithsonian's non-scientific library. Around this time, the Library of Congress was planning to build and relocate to the new Thomas Jefferson Building, designed to be fireproof. Authorized by an act of Congress, Henry transferred the Smithsonian's non-scientific library of 40,000 volumes to the Library of Congress in 1866. In 1861, President Abraham Lincoln appointed John G. Stephenson as Librarian of Congress; the appointment is regarded as the most political to date. Stephenson was a physician and spent equal time serving as librarian and as a physician in the Union Army. He could manage this division of interest because he hired Ainsworth Rand Spofford as his assistant. Despite his new job, Stephenson focused on the war. Three weeks into his term as Librarian of Congress, he left Washington, D.C., to serve as a volunteer aide-de-camp at the battles of Chancellorsville and Gettysburg during the American Civil War.

=== Phase I - modification === In phase I, a variety of enzymes acts to introduce reactive and polar groups into their substrates. One of the most common modifications is hydroxylation catalysed by the cytochrome P-450-dependent mixed-function oxidase system. These enzyme complexes act to incorporate an atom of oxygen into nonactivated hydrocarbons, which can result in either the introduction of hydroxyl groups or N-, O- and S-dealkylation of substrates. The reaction mechanism of the P-450 oxidases proceeds through the reduction of cytochrome-bound oxygen and the generation of a highly-reactive oxyferryl species, according to the following scheme:

The drug must be found to be effective against the disease for which it is seeking approval (where 'effective' means only that the drug performed better than placebo or competitors in at least two trials). The drug must meet safety criteria by being subject to animal and controlled human testing. Gaining FDA approval usually takes several years. Testing done on animals must be extensive and must include several species to help in the evaluation of both the effectiveness and toxicity of the drug. The dosage of any drug approved for use is intended to fall within a range in which the drug produces a therapeutic effect or desired outcome. The safety and effectiveness of prescription drugs in the U.S. are regulated by the federal Prescription Drug Marketing Act of 1987. The Medicines and Healthcare products Regulatory Agency (MHRA) has a similar role in the UK. Medicare Part D is a prescription drug plan in the U.S. The Prescription Drug Marketing Act (PDMA) is an act related to drug policy. Prescription drugs are drugs regulated by legislation.

== Principles == Ion milling operates on the principles of sputtering and erosion. Sputtering occurs as the high-energy ions bombard the sample surface. Ions collide with the atoms and molecules on the surface and knock off surface atoms. As the high-energy ions are directed onto the material's surface, a collision cascade occurs. Ions bombard the surface of the specimen, and energy is transferred from the ions onto the surface atoms. If the transferred energy surpasses the binding energy of the target atoms, they are dislodged from the surface. Material that juts out has less surface binding energy and is more likely to be ejected through sputtering. As the ion milling process continues, the sample surface is slowly eroded away, resulting in a thin, flat, and damage-free surface. Specific results can be achieved by changing the angle of incidence of ions, the ion energy, and the type of ions used.

Sources: en.wikipedia.org

Further detail

==== Albums and EPs ==== Chain, a 1989 album by Paul Haig Chain (The Family Stand album), 1990 Chain (Pylon album), 1990 Chains (album), by Yōko Oginome, 1997 Chain (Bonnie Pink EP), 2008 Chain (KAT-TUN album), 2012 Chain (NCT 127 EP), 2018

=== Tempe bacem === Tempe bacem is a traditional Javanese dish originating in Central Java. Bacem is a Javanese cooking method of braising in spices and palm sugar and boiling the food in a closed place until the water runs out. The tempeh is first braised in a mixture of coconut water, palm sugar, and spices including coriander seeds, shallots, galangal, and bay leaves, and then briefly deep-fried. The result is a moist, sweet and spicy, dark-colored tempeh. Tofu may also be used, yielding tahu bacem.

Registered voters: 125,090 valid: 104,941 turnout: 84% The West Prussian plebiscite area remained with Germany and became part of the new West Prussia Government Region, which was annexed to East Prussia in 1922.

However, in 2015 a study building on earlier research found that happiness has no effect on mortality. "This "basic belief that if you're happier you're going to live longer. That's just not true." Consistent results are that "apart from good health, happy people were more likely to be older, not smoke, have fewer educational qualifications, do strenuous exercise, live with a partner, do religious or group activities and sleep for eight hours a night." Happiness does however seem to have a protective impact on immunity. The tendency to experience positive emotions was associated with greater resistance to colds and flu in interventional studies irrespective of other factors such as smoking, drinking, exercise, and sleep. Positive emotional states have a favorable effect on mortality and survival in both healthy and diseased populations. Even at the same level of smoking, drinking, exercise, and sleep, happier people seem to live longer. Interventional trials conducted to establish a cause-effect relationship indicate positive emotions to be associated with greater resistance to objectively verifiable colds and flu.

Sources: en.wikipedia.org

Background from the literature

state of the 2028 presidential primaries cycle for the Democratic Party in the upcoming presidential election. August 17 Trump orders the Pentagon to reduce yearly joint exercises with South Korea, saying that the ally refused to help with the 2026 Iran war and citing his good relationship with North Korean leader Kim Jong Un. The 60-day deadline for the US and Iran to negotiate a "final deal" to end the 2026 Iran war expires. Following the official end of the US-Iran ceasefire, Trump urges Iran to surrender. Trump states that the Iranian regime will not agree to the deal that the US feels is needed, and he is not looking to extend the Memorandum of Understanding. Opening statements begin in the murder trial of Duane "Keffe D" Davis, who is accused of orchestrating the 1996 drive-by shooting that killed rapper Tupac Shakur in Las Vegas. August 18 The Defense Department orders an audit of 30 universities' partnerships with foreign institutions, most of which are Chinese, but also include Russian and Iranian institutions. President Tomoko Akane of the International Criminal Court and a senior trial lawyer at the court who was part of a team which sought an arrest warrant for Israeli Prime Minister Benjamin Netanyahu for alleged war crimes in the Gaza war is sanctioned by the US. Newly revealed emails show that a silent channel between ICE and the Iranian government shaped deportation flights in 2025 and 2026 despite tensions mounting between the two states. The national debt surpasses $40 trillion for the first time.

The fas receptor (First apoptosis signal) – (also known as Apo-1 or CD95) is a transmembrane protein of the TNF family which binds the Fas ligand (FasL). The interaction between Fas and FasL results in the formation of the death-inducing signaling complex (DISC), which contains the FADD, caspase-8 and caspase-10. In some types of cells (type I), processed caspase-8 directly activates other members of the caspase family, and triggers the execution of apoptosis of the cell. In other types of cells (type II), the Fas-DISC starts a feedback loop that spirals into increasing release of proapoptotic factors from mitochondria and the amplified activation of caspase-8.

Foot-and-mouth disease virus (FMDV) is a virus in the genus Aphthovirus that causes foot-and-mouth disease in cattle. As a member of the family Picornaviridae, FMDV is a positive-sense, single-stranded RNA virus. 2A is located between the capsid proteins and polymerases and proteases required for the capsid assembly in the late stages of the infection. The incomplete ribosomal skipping during the viral RNA translation mediated by the 2A results in "ribosome drop off" in some cases, after which the translation doesn't restart. This leads to a prevalence of the N-terminal proteins and allows for the increased production of the structural proteins relative to the non-structural proteins.

Sources: en.wikipedia.org

Frequently asked questions

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.

Why did clinical development stop?

Preclinical rodent studies reported cancers, including liver and bladder tumors, at tested doses. The human relevance of those findings is uncertain, but development was discontinued. No approved human product resulted.

Is cardarine approved for medical use?

No. It remains an investigational compound without approved therapeutic labeling. Sports regulators prohibit its use, and health agencies have warned against consuming it.

Is cardarine banned in sports?

Yes, WADA prohibits cardarine as a PPARδ agonist. It appears on the prohibited list and can be detected in urine or blood. Athletes using it risk sanctions.

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