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Identity And Regulatory Status — Field Notes

By Editorial Desk · published 2026-05-24 · last reviewed 2026-06-26 · Wiki

Nuclear receptor is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.

Last reviewed on 2026-06-26. Where a claim depends on a specific study, the study is described rather than over-claimed.

Identity and Regulatory Status

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.

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 Research Context

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.

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

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.

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

Cardarine Identity and Mechanism

Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.

Cardarine is the common name for GW501516, a synthetic compound studied as a peroxisome proliferator-activated receptor delta agonist. Researchers developed it to explore treatments for lipid disorders and metabolic conditions. It is not an approved medicine in any country. Early clinical work examined changes in HDL cholesterol and triglycerides, but development was discontinued after animal studies raised concerns about cancer. The compound remains available as a research chemical and appears in discussions of performance enhancement.

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Identity and Pharmacological Classification

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.

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.

Background from the literature

== Mechanism == Myelofibrosis is a clonal neoplastic disorder of hematopoiesis, the formation of blood cellular components. It is one of the myeloproliferative disorders, diseases of the bone marrow in which excess cells are produced at some stage. Production of cytokines such as fibroblast growth factor by the abnormal hematopoietic cell clone (particularly by megakaryocytes) leads to replacement of the hematopoietic tissue of the bone marrow by connective tissue via collagen fibrosis. The decrease in hematopoietic tissue impairs the patient's ability to generate new blood cells, resulting in progressive pancytopenia, a shortage of all blood cell types. However, the proliferation of fibroblasts and deposition of collagen is a secondary phenomenon, and the fibroblasts themselves are not part of the abnormal cell clone. In primary myelofibrosis, progressive scarring, or fibrosis, of the bone marrow occurs, for the reasons outlined above. The result is extramedullary hematopoiesis, i.e. blood cell formation occurring in sites other than the bone marrow, as the hemopoietic cells are forced to migrate to other areas, particularly the liver and spleen. This causes an enlargement of these organs. In the liver, the abnormal size is called hepatomegaly. Enlargement of the spleen is called splenomegaly, which also contributes to causing pancytopenia, particularly thrombocytopenia and anemia. Another complication of extramedullary hematopoiesis is poikilocytosis, or the presence of abnormally shaped red blood cells.

== Personal life == On 5 July 2008, Emma Griffiths married Busted member Matt Willis at Rushton Hall, Northamptonshire, after three years of dating. The wedding was featured in OK magazine. She gave birth to their first child, a daughter named Isabelle, on 20 June 2009. On 25 November 2011, the couple had a second child, a son named Ace. On 4 May 2016, Willis gave birth to their third child, a second daughter, named Trixie Grace. In an episode of Who Do You Think You Are?, Willis confirmed that she has longstanding roots in Birmingham, with her family tree being traced back to her great-great-great-grandfather, who was named James Gretton and was listed as a Horn and Hair Merchant in the census records. She also found she had Irish ancestors, a fact that came as a surprise to her. The revelations about her ancestry left her extremely uncomfortable with the actions of one, who she discovered was a violent Orangeman, but overall, she was happy to have found a connection to her more broad Irish heritage. Willis is a supporter of Aston Villa. In August 2019, Willis obtained a qualification as a maternity care assistant following her experience on the W series Delivering Babies. During the COVID-19 pandemic in March 2021, Willis and her husband completed training with St John Ambulance to act as vaccination volunteers. In May 2023, Willis was featured in the documentary, Matt Willis: Fighting Addiction. The documentary, which aired on the BBC on 17 May 2023, followed Willis and her husband as they spoke about the latter's addiction issues.

The discovery posed a problem, since sales of enalapril were strong for Merck, and the company did not want to diminish those sales. Merck ended up entering into an agreement with Zeneca under which Zeneca received the right to co-market lisinopril, and Merck received the exclusive rights to an earlier stage aldose reductase inhibitor drug candidate, a potential diabetes treatment. Zeneca's marketing and brand name, "Zestril", turned out to be stronger than Merck's effort. The drug became a blockbuster for AstraZeneca (formed in 1998), with annual sales in 1999 of $1.2B. The US patents expired in 2002. Since then, lisinopril has been available under many brand names worldwide; it is also available in combination drugs with diuretic hydrochlorothiazide (as lisinopril/hydrochlorothiazide), and with calcium channel blocker amlodipine (as lisinopril/amlodipine).

Technology companies have built electricity and artificial intelligence infrastructure to facilitate the AI boom of the 2020s. A 2025 report from the consulting firm McKinsey & Company estimated that by 2030, $2.7 trillion would be invested into AI infrastructure and data centres in the US, surpassing World War II's Manhattan Project every month. In January 2024, the International Energy Agency (IEA) released Electricity 2024, Analysis and Forecast to 2026. This is the first IEA report to make projections for data centres and power consumption by AI and cryptocurrency. The report states that power demand for these uses might double by 2026, with the additional power consumption equaling that of Japan. Power consumption by AI is responsible for an increase in fossil fuel use, and has delayed closings of obsolete, carbon-emitting coal energy facilities. A ChatGPT search involves 10 times as much electrical energy as a Google search. A 2024 Goldman Sachs research paper, AI Data Centers and the Coming US Power Demand Surge, found "US power demand (is) likely to experience growth not seen in a generation...." and forecasts that, by 2030, US data centres will consume 8% of US power, as opposed to 3% in 2022, presaging growth for the electrical power generation industry by a variety of means. Data centres' need for more and more electrical power is such that they might max out the electrical grid. The Big Tech companies counter that AI can be used to maximise the utilisation of the grid by all.

The army command coordinated with a multitude of spontaneous groupings to form the Defense of the Nation (Obrana národa, ON) with branches in Britain and France. Czechoslovak units and formations with Czechs (c. 65–70%), and Slovaks (c. 30%) served with the Polish Army (Czechoslovak Legion), the French Army, the Royal Air Force, the British Army (the 1st Czechoslovak Armoured Brigade), and the Red Army (I Czechoslovak Corps). Two thousand eighty-eight Czechs and 401 Slovaks fought in 11th Infantry Battalion-East alongside the British during the war in areas such as North Africa and Palestine. Among others, Czech fighter pilot, Sergeant Josef František was one of the most successful fighter pilots in the Battle of Britain. Beneš's collaborators, led by Prokop Drtina, created the Political Center (Politické ústředí, PÚ). The PÚ was nearly destroyed by arrests in November 1939, after which younger politicians took control. Social democrats and leftist intellectuals, in association with such groups as trade unions and educational institutions, constituted the Committee of the Petition that We Remain Faithful (Petiční výbor Věrni zůstaneme, PVVZ). The Communist Party of Czechoslovakia (KSČ) was the fourth major resistance group. The KSČ had been one of over 20 political parties in the democratic First Republic, but it had never gained sufficient votes to unsettle the democratic government. After the Munich Agreement, the leadership of the KSČ moved to Moscow and the party went underground. Until 1943, however, KSČ resistance was weak.

Sources: en.wikipedia.org

Further detail

Quinteiro, Javier; Baibai, Tarik; Oukhattar, Laila; Soukri, Abdelaziz; Seixas, Pablo; Rey-Méndez, Manuel (2011). "Multiple paternity in the common octopus Octopus vulgaris (Cuvier, 1797), as revealed by microsatellite DNA analysis" (PDF). Molluscan Research. 31 (1): 15–20. Bibcode:2011MollR..311.1.2Q. CiteSeerX 10.1.1.363.8342. doi:10.11646/mr.31.1.2. {{cite journal}}: Cite uses deprecated parameter |citeseerx= (help) "CephBase: Common octopus". Archived from the original on 17 August 2005. Photos of Common octopus in the Sealife Collection

Stalin's plans for the city included a network of broad avenues and roadways, some of them more than ten lanes wide, which—while significantly simplifying movement through the city—were constructed at the expense of many historical buildings and districts. Among the many losses from Stalin's demolitions were the Sukharev Tower, an old city landmark, as well as mansions and commercial buildings. The city's new status as the capital of a strongly secular nation made religiously significant buildings particularly vulnerable to demolition. Many of the city's churches—in most cases some of Moscow's oldest and most prominent buildings—were destroyed. Notable examples of this destruction include Kazan Cathedral and the Cathedral of Christ the Saviour. During the 1990s, both cathedrals were rebuilt. Many smaller churches, however, were lost.

Antioxidant vitamins are found in vegetables, fruits, eggs, legumes and nuts. Vitamins A, C, and E can be destroyed by long-term storage or prolonged cooking. The effects of cooking and food processing are complex, as these processes can also increase the bioavailability of antioxidants, such as some carotenoids in vegetables. Processed food contains fewer antioxidant vitamins than fresh and uncooked foods, as preparation exposes food to heat and oxygen.

Cligosiban (INNTooltip International Nonproprietary Name; developmental code names IX-01 and PF-3274167) is an oxytocin receptor antagonist which is or was under development for the treatment of premature ejaculation. It is taken orally. The drug is a small molecule or non-peptide and is a potent, highly selective, and brain-penetrant antagonist of the oxytocin receptor. Cligosiban was originated by Pfizer and is under development by Ixchelsis and Chorus Group. As of December 2019, it is in phase 2 clinical trials. However, another source lists the drug's development as having been discontinued. The drug failed to show effectiveness in a phase 2b trial.

=== Prior experiments === From the earliest days of radio technology, signals had been used for navigation using the radio direction finding (RDF) technique. RDF can determine the bearing to a radio transmitter, and several such measurements can be combined to produce a radio fix, allowing the receiver's position to be calculated. Given some basic changes to the broadcast signal, it was possible for the receiver to determine its location using a single station. The UK pioneered one such service in the form of the Orfordness Beacon. Through the early period of radio development it was widely known that certain materials, especially metal, reflected radio signals. This led to the possibility of determining the location of objects by broadcasting a signal and then using RDF to measure the bearing of any reflections. Such a system saw patents issued to Germany's Christian Hülsmeyer in 1904, and widespread experimentation with the basic concept was carried out from then on. These systems revealed only the bearing to the target, not the range, and due to the low power of radio equipment of that era, they were useful only for short-range detection. This led to their use for iceberg and collision warning in fog or bad weather, where all that was required was the rough bearing of nearby objects. The use of radio detection specifically against aircraft was first considered in the early 1930s. Teams in the UK, US, Japan, Germany and others had all considered this concept and put at least some amount of effort into developing it.

Sources: en.wikipedia.org

Background from the literature

=== Dry infusion === Dry infusion is the combination of partial dehydration and osmotic dehydration using a humectant. The food product is first dehydrated and then the resultant product is added to a humectant solution to reach the desired water activity. This method is desirable because it results in a higher quality and more appealing product. However, more energy is used for this method because it is two processing steps combined. Dry infusion is primarily employed by the U.S military and NASA for production of IMF to produce safe, palatable food that can be consumed much later than it is produced.

DKA is common in type 1 diabetes as this form of diabetes is associated with an absolute lack of insulin production by the islets of Langerhans. In type 2 diabetes, insulin production is present but is insufficient to meet the body's requirements as a result of end-organ insulin resistance. Usually, these amounts of insulin are sufficient to suppress ketogenesis. If DKA occurs in someone with type 2 diabetes, their condition is called "ketosis-prone type 2 diabetes". The exact mechanism for this phenomenon is unclear, but there is evidence both of impaired insulin secretion and insulin action. Once the condition has been treated, insulin production resumes and often the person may be able to resume diet or tablet treatment as normally recommended in type 2 diabetes. The clinical state of DKA is associated, in addition to the above, with the release of various counterregulatory hormones such as glucagon and adrenaline, as well as cytokines, the latter of which leads to increased markers of inflammation, even in the absence of infection. Cerebral edema, which is the most dangerous DKA complication, is probably the result of a number of factors. Some authorities suggest that it is the result of overvigorous fluid replacement, but the complication may develop before treatment has been commenced. It is more likely in those with more severe DKA, and in the first episode of DKA.

Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as a hormone, neurotransmitter and neuromodulator. The name "norepinephrine" (from Ancient Greek ἐπῐ́ (epí), "upon", and νεφρός (nephrós), "kidney") is usually preferred in the United States, whereas "noradrenaline" (from Latin ad, "near", and ren, "kidney") is more commonly used in the United Kingdom and the rest of the world. "Norepinephrine" is also the international nonproprietary name given to the drug. Regardless of which name is used for the substance itself, parts of the body that produce or are affected by it are referred to as noradrenergic. The general function of norepinephrine is to mobilize the brain and body for action. Norepinephrine release is lowest during sleep, rises during wakefulness, and reaches much higher levels during situations of stress or danger, in the so-called fight-or-flight response. In the brain, norepinephrine increases arousal and alertness, promotes vigilance, enhances formation and retrieval of memory, and focuses attention; it also increases restlessness and anxiety. In the rest of the body, norepinephrine increases heart rate and blood pressure, triggers the release of glucose from energy stores, increases blood flow to skeletal muscle, reduces blood flow to the gastrointestinal system, and inhibits voiding of the bladder and gastrointestinal motility. In the brain, noradrenaline is produced in nuclei that are small yet exert powerful effects on other brain areas.

Sildenafil protects cyclic guanosine monophosphate (cGMP) from degradation by cGMP-specific phosphodiesterase type 5 (PDE5) in the corpus cavernosum. Nitric oxide (NO) in the corpus cavernosum of the penis binds to guanylate cyclase receptors, which results in increased levels of cGMP, leading to smooth muscle relaxation (vasodilation) of the intimal cushions of the helicine arteries. This smooth muscle relaxation leads to vasodilation and increased inflow of blood into the spongy tissue of the penis, causing an erection. Robert F. Furchgott, Ferid Murad, and Louis Ignarro won the Nobel Prize in Physiology or Medicine in 1998 for their independent study of the metabolic pathway of nitric oxide in smooth muscle vasodilation. The molecular mechanism of smooth muscle relaxation involves the enzyme CGMP-dependent protein kinase, also known as PKG. This kinase is activated by cGMP and it phosphorylates multiple targets in the smooth muscle cells, namely myosin light chain phosphatase, RhoA, IP3 receptor, phospholipase C, and others. Overall, this results in a decrease in intracellular calcium and desensitizing proteins to the effects of calcium, engendering smooth muscle relaxation. Sildenafil is a potent and selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP in the corpus cavernosum. The molecular structure of sildenafil is similar to that of cGMP and acts as a competitive binding agent of PDE5 in the corpus cavernosum, resulting in more cGMP and increased penile response to sexual stimulation.

MacDonald et al. (1990) has described four general community types. These are communities dominated by Vestimentiferan tube worms (Lamellibrachia c.f. barhami and Escarpia spp.), mytilid mussels (Seep Mytilid Ia, Ib, and III, and others), vesicomyid clams (Vesicomya cordata and Calyptogena ponderosa), and infaunal lucinid or thyasirid clams (Lucinoma sp. or Thyasira sp.). Bacterial mats are present at all sites visited to date. These faunal groups tend to display distinctive characteristics in terms of how they aggregate, the size of aggregations, the geological and chemical properties of the habitats in which they occur, and, to some degree, the heterotrophic fauna that occur with them. Many of the species found at these cold seep communities in the Gulf of Mexico are new to science and remain undescribed. Individual lamellibrachid tube worms, the longer of two taxa found at seeps, can reach lengths of 3 metres (9.8 feet) and live hundreds of years (Fisher et al., 1997; Bergquist et al., 2000). Growth rates determined from recovered marked tube worms have been variable, ranging from no growth of 13 individuals measured one year to a maximum growth of 9.6 cm/yr (3.8 in/yr) in a Lamellibrachia individual (MacDonald, 2002). Average growth rate was 2.19 cm/yr (0.86 in/yr) for the Escarpia-like species and 2.92 cm/yr (1.15 in/yr) for lamellibrachids. These are slower growth rates than those of their hydrothermal vent relatives, but Lamellibrachia individuals can reach lengths 2–3 times that of the largest known hydrothermal vent species. Individuals of Lamellibrachia sp.

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 a common name for GW501516, a synthetic PPARδ agonist developed for research. It has not been approved as a medication in any country. It is classified as an unapproved drug and a prohibited substance in sport.

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