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Identity And Regulatory Status — Beginner to Advanced

By Editorial Desk · published 2026-02-26 · last reviewed 2026-03-29 · Faq

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.

Updated 2026-03-29. Numbers and descriptions here follow the published literature rather than marketing material.

Identity and Regulatory Status

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.

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.

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 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

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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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.

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

Supporting material

=== Mixed === In mixed inhibition the inhibitor may bind to the enzyme whether or not the substrate has already bound. Hence mixed inhibition is a combination of competitive and noncompetitive inhibition. Furthermore, the affinity of the inhibitor for the free enzyme and the enzyme-substrate complex may differ. By increasing concentrations of substrate [S], this type of inhibition can be reduced (due to the competitive contribution), but not entirely overcome (due to the noncompetitive component). Although it is possible for mixed-type inhibitors to bind in the active site, this type of inhibition generally results from an allosteric effect where the inhibitor binds to a different site on an enzyme. Inhibitor binding to this allosteric site changes the conformation (that is, the tertiary structure or three-dimensional shape) of the enzyme so that the affinity of the substrate for the active site is reduced. These four types of inhibition can also be distinguished by the effect of increasing the substrate concentration [S] on the degree of inhibition caused by a given amount of inhibitor. For competitive inhibition the degree of inhibition is reduced by increasing [S], for noncompetitive inhibition the degree of inhibition is unchanged, and for uncompetitive (also called anticompetitive) inhibition the degree of inhibition increases with [S].

Chinese cuisine exhibits an immense amount of regional diversity. A number of different styles contribute to Chinese cuisine but perhaps the best known and most influential are Cantonese cuisine, Shandong cuisine, Jiangsu cuisine (specifically Huaiyang cuisine) and Sichuan cuisine. These styles are distinctive from one another due to factors such as availability of resources, climate, geography, history, cooking techniques and lifestyle. One style may favour the use of garlic and shallots over chili and spices, while another may favour preparing seafood over other meats and fowl. Jiangsu cuisine favours cooking techniques such as braising and stewing, while Sichuan cuisine employs baking. Zhejiang cuisine focuses more on serving fresh food, Fujian cuisine is famous for its seafood and soups and the use of spices, Hunan cuisine is famous for its hot and salty taste, Anhui cuisine incorporates wild ingredients for an unusual taste. Based on the raw materials and ingredients used, the method of preparation and cultural differences, a variety of foods with different flavors and textures are prepared in different regions of the country. Many traditional regional cuisines rely on basic methods of preservation such as drying, salting, pickling and fermentation. In addition, the "rice theory" attempts to describe cultural differences between north and south China; in the north, noodles are more consumed due to wheat being widely grown whereas in the south, rice is more preferred as it has historically been more cultivated there.

Nutty Professor II: The Klumps at IMDb Nutty Professor II: The Klumps at the TCM Movie Database (archived) Nutty Professor II: The Klumps at the AFI Catalog of Feature Films Nutty Professor II: The Klumps at Box Office Mojo Nutty Professor II: The Klumps at Rotten Tomatoes Nutty Professor II: The Klumps at Metacritic

Li2CO3 + CO2 + H2O ⇌ 2 LiHCO3 The extraction of lithium carbonate at high pressures of CO2 and its precipitation upon depressurizing is the basis of the Quebec process. Lithium carbonate can also be purified by exploiting its diminished solubility in hot water. Thus, heating a saturated aqueous solution causes crystallization of Li2CO3. Lithium carbonate, and other carbonates of group 1, do not decarboxylate readily. Li2CO3 decomposes at temperatures around 1300 °C.

Sources: en.wikipedia.org

Notes from published material

=== Public awareness === Public awareness of the disease, which is spread through the exchange of bodily fluids, is not as high as it is for HIV and AIDS. In some rural areas, doctors have reused syringes and unknowingly spread the disease, particularly among children.

"Fentanyl". U.S. Drug Enforcement Administration (DEA). "Fentanyl". European Union Drugs Agency (EUDA). "Fentanyl". National Institute on Drug Abuse (NIDA). 21 December 2021. Archived from the original on 6 June 2022. Fentanyl (Report). National Institute for Occupational Safety and Health (NIOSH). 8 July 2021.

The argument for keeping the term "atomic weight" was primarily that it was a well understood term to those in the field, that the term "atomic mass" was already in use (as it is currently defined) and that the term "relative atomic mass" might be easily confused with relative isotopic mass (the mass of a single atom of a given nuclide, expressed dimensionlessly relative to 1/12 of the mass of carbon-12; see section above). In 1979, as a compromise, the term "relative atomic mass" was introduced as a secondary synonym for atomic weight. Twenty years later the primacy of these synonyms was reversed, and the term "relative atomic mass" is now the preferred term. However, the term "standard atomic weights" (referring to the standardized expectation atomic weights of differing samples) has not been changed, because simple replacement of "atomic weight" with "relative atomic mass" would have resulted in the term "standard relative atomic mass".

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.

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.

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