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Identity And Regulatory Status — Background and Details

By Editorial Desk · published 2026-02-06 · last reviewed 2026-03-13 · Topic

Cardarine 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.

Updated 2026-03-13. Numbers and descriptions here follow the published literature rather than marketing material.

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.

Cardarine Identity and Mechanism

At the molecular level, GW501516 binds and activates PPARδ, a nuclear receptor that regulates transcription. Activation shifts expression of genes involved in fatty acid oxidation, energy expenditure, and lipid transport in skeletal muscle and liver. Animal studies report increased endurance and altered lipid profiles after exposure. Human data are limited to small trials and do not establish long-term safety or efficacy. PPARδ also has roles in cell proliferation, so the relationship between activation and cancer risk remains an open question.

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 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

Further detail

Cytochrome-b5 reductase is a NADH-dependent enzyme that converts ferricytochrome from a Fe3+ form to a Fe2+ form. It contains FAD and catalyzes the reaction: In its b5-reducing capacity, this enzyme is involved in desaturation and elongation of fatty acids, cholesterol biosynthesis, and drug metabolism. This enzyme can also reduce methemoglobin to normal hemoglobin, gaining it the inaccurate synonym methemoglobin reductase. Isoforms expressed in erythrocytes (CYB5R1, CYB5R3) perform this function in vivo. Ferricyanide is another substrate in vitro.

In 1958, scientists at Lawrence Berkeley National Laboratory claimed the discovery of element 102, now called nobelium. At the same time, they also tried to synthesize element 103 by bombarding the same curium target used with 14N ions. Eighteen tracks were noted, with decay energy around 9±1 MeV and half-life around 0.25 s; the Berkeley team noted that while the cause could be the production of an isotope of element 103, other possibilities could not be ruled out. While the data agrees reasonably with that later discovered for 257Lr (alpha decay energy 8.87 MeV, half-life 0.6 s), the evidence obtained in this experiment fell far short of the strength required to conclusively demonstrate synthesis of element 103. A follow-up on this experiment was not done, as the target was destroyed. Later, in 1960, the Lawrence Berkeley Laboratory attempted to synthesize the element by bombarding 252Cf with 10B and 11B. The results of this experiment were not conclusive. The first important work on element 103 was done at Berkeley by the nuclear-physics team of Albert Ghiorso, Torbjørn Sikkeland, Almon Larsh, Robert M. Latimer, and their co-workers on February 14, 1961. The first atoms of lawrencium were reportedly made by bombarding a three-milligram target consisting of three isotopes of californium with boron-10 and boron-11 nuclei from the Heavy Ion Linear Accelerator (HILAC). The Berkeley team reported that the isotope 257Lr was detected in this manner, and that it decayed by emitting an 8.6 MeV alpha particle with a half-life of 8±2 s.

Apelin (also known as APLN) is a peptide that in humans is encoded by the APLN gene. Apelin is one of two endogenous ligands for the G-protein-coupled APJ receptor that is expressed at the surface of some cell types. It is widely expressed in various organs such as the heart, lung, kidney, liver, adipose tissue, gastrointestinal tract, brain, adrenal glands, endothelium, and human plasma.

=== Sport === Donough O'Brien (1879–1953), was a Welsh-born Irish cricketer. Ray Williams (born 1959), is a weightlifting Commonwealth Games gold medallist. Tony Roberts (born 1969), is Welsh international footballer with 614 club caps Gareth Evans (born 1986), weightlifter, Commonwealth gold medalist and 2012 Summer Olympics, lives in the town. Alex Lynch (born in 1995), a footballer with over 100 club caps, educated in Ysgol Uwchradd Caergybi.

Sources: en.wikipedia.org

Related pages on this site

Background from the literature

Western Region (Vancouver, Seattle, San Francisco Bay Area, Los Angeles) Central Region (Guadalajara, Mexico City, Monterrey, Houston, Dallas, Kansas City) Eastern Region (Atlanta, Miami, Toronto, Boston, Philadelphia, New York/New Jersey) However, even during the group stage, about half of the teams had to play matches in two different regions.

== Later life and death == Schoenheimer had married Salome Glucksohn, a noted zoologist and geneticist, in 1937. They emigrated to the United States together, and they had no children. They later divorced. Schoenheimer was invited to conduct lectures detailing his scientific work and findings. In 1937, he conducted his Harvey Lecture and in 1941 his Dunham Lecture was conducted by his colleagues in his behalf. At the height of his career he committed suicide by ingesting potassium cyanide at his home in Yonkers, having struggled with depression for multiple years.

The bacteria Pseudomonas putida CBB5 can live on pure caffeine and can cleave caffeine into carbon dioxide and ammonia. Caffeine is toxic to birds and to dogs and cats, and has a pronounced adverse effect on mollusks, various insects, and spiders. This is at least partly due to a poor ability to metabolize the compound, causing higher levels for a given dose per unit weight. Caffeine has also been found to enhance the reward memory of honey bees.

Sources: en.wikipedia.org

Reference notes

=== Imaging studies === In some cases, imaging studies may be used to assess the extent of organ involvement and damage. For example, chest x-rays or CT scans can identify lung involvement in diseases like rheumatoid arthritis or systemic lupus erythematosus, while an MRI can reveal inflammation or damage in the brain and spinal cord in multiple sclerosis.

Cancellous bone, spongy bone, or trabecular bone is the internal tissue of the skeletal bone and is an open-cell porous network that follows the material properties of biofoams. Cancellous bone has a higher surface-area-to-volume ratio than cortical bone and it is less dense. This makes it weaker and more flexible. The greater surface area also makes it suitable for metabolic activities such as the exchange of calcium ions. Cancellous bone is typically found at the ends of long bones, near joints, and in the interior of vertebrae. Cancellous bone is highly vascular and often contains red bone marrow where hematopoiesis, the production of blood cells, occurs. The primary anatomical and functional unit of cancellous bone is the trabecula. The trabeculae are aligned towards the mechanical load distribution that a bone experiences within long bones such as the femur. As far as short bones are concerned, trabecular alignment has been studied in the vertebral pedicle. Thin formations of osteoblasts covered in endosteum create an irregular network of spaces, known as trabeculae. Within these spaces are bone marrow and hematopoietic stem cells that give rise to platelets, red blood cells and white blood cells. Trabecular marrow is composed of a network of rod- and plate-like elements that make the overall organ lighter and allow room for blood vessels and marrow. Trabecular bone accounts for the remaining 20% of total bone mass but has nearly ten times the surface area of compact bone.

Scar revision is a process of cutting the scar tissue out. After the excision, the new wound is usually closed up to heal by primary intention, instead of secondary intention. Deeper cuts need a multilayered closure to heal optimally, otherwise depressed or dented scars can result. Surgical excision of hypertrophic or keloid scars is often associated to other methods, such as pressotherapy or silicone gel sheeting. Lone excision of keloid scars, however, shows a recurrence rate close to 45%. A clinical study is currently ongoing to assess the benefits of a treatment combining surgery and laser-assisted healing in hypertrophic or keloid scars. Subcision is a process used to treat deep rolling scars left behind by acne or other skin diseases. It is also used to lessen the appearance of severe glabella lines, though its effectiveness in this application is debatable. Essentially the process involves separating the skin tissue in the affected area from the deeper scar tissue. This allows the blood to pool under the affected area, eventually causing the deep rolling scar to level off with the rest of the skin area. Once the skin has leveled, treatments such as laser resurfacing, microdermabrasion or chemical peels can be used to smooth out the scarred tissue.

=== HANAC syndrome === Mutations in COL4A1 exons 24 and 25 are associated with HANAC (autosomal dominant hereditary angiopathy with nephropathy, aneurysms, and muscle cramps). It has also been confirmed that mutations in the COL4A1 gene occur in some patients with porencephaly and schizencephaly.

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 the investigational compound GW501516. It acts as a PPARδ agonist and is not approved for human use. It is prohibited in sport.

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