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Background And Regulatory Status — Questions and Answers

By Editorial Desk · published 2026-03-23 · last reviewed 2026-04-12 · News

If you have been reading about Cardarine and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.

Last reviewed on 2026-04-12. Where a claim depends on a specific study, the study is described rather than over-claimed.

Background and Regulatory Status

Sporting authorities added GW501516 to prohibited lists after it appeared in athlete samples and online markets. The World Anti-Doping Agency classifies it as a hormone and metabolic modulator, and its use can lead to an anti-doping rule violation. Some early laboratory work suggested effects on fatty acid oxidation and endurance-related metabolism in animals, but those findings do not establish safe or effective use in people. Reports of adverse events in humans are scarce and often anecdotal, which complicates risk assessment.

Legal status varies by country. In some places, cardarine is controlled under medicines or psychoactive substances laws; in others, it may be sold with minimal oversight as a research chemical. Customs agencies have intercepted shipments, and several national health agencies have issued warnings about products marketed for bodybuilding or performance enhancement. The lack of a standardized pharmaceutical supply means identity, purity, and contamination levels can differ widely between samples. These factors make cardarine a regulatory and public health concern rather than a conventional prescription drug.

Identity and Pharmacological Mechanism

Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.

Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.

The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.

Cardarine at a glance

PropertyValueNotes
IUPAC name{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acidSystematic name for GW501516
CAS Registry Number317318-70-0Unique identifier for the parent compound
Molecular formulaC21H18F3NO3S2Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur
Molecular weight453.5 g/molApproximate value for the neutral form
AppearanceWhite to off-white powderTypical description for purified laboratory material

Background and Regulatory History

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.

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.

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Regulatory Status and Detection Context

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.

Reference notes

=== Carbonyl compounds === There are five types of carbonyl compounds, including aldehydes, ketones, carboxylic acids and esters. The principal fragmentation modes are described as follows: Alpha-cleavage can occur on either side of the carbonyl functional group since an oxygen lone pair can stabilize the positive charge.

In September 2008, Aboitiz Equity Ventures decided to quit the shipping business to focus on its core businesses, namely power and financial services, and announced the sale of its controlling 77% stake in Aboitiz Transport System to KGLI‑NM Holdings, a joint venture between Negros Navigation and Dutch investors, with plans to acquire the remaining shares and potentially delist the company, but due to financing difficulties during the global financial crisis, KGLI‑NM was unable to complete the full buyout, paid only a P100 million option fee, and eventually withdrew its offer in May 2009, terminating the agreement. On December 1, 2010, Aboitiz Equity Ventures sold its transport business to Negros Navigation Co. Inc. (NENACO) for US$105 million, transferring all logistics and shipping operations under new ownership. At the same time, the China–ASEAN Investment Cooperation Fund, a Netherlands-based private equity firm owned by the Government of the People's Republic of China, acquired a controlling stake in NENACO through an equity infusion. In 2012, the company was reorganized and rebranded as 2GO Group Inc. with its brands SuperFerry, SuperCat, and Cebu Ferries merged with Negros Navigation to form 2GO Travel. In 2016, SM Investments Corporation (SMIC) and Chelsea Logistics and Infrastructure Holdings Corp. (owned by Dennis Uy) jointly acquired a major stake in 2GO Group Inc. In 2021, Chelsea Logistics sold its shares to SMIC, making 2GO a full subsidiary of SM Investments Corporation.

November 14, 2008: Eurozone Taken as a whole the Eurozone officially slips under, pushed down by recessions in Germany and Italy for its first recession since its creation in 1999. These 15 countries are: Austria, Belgium, Cyprus, Finland, France, Germany, Greece, Ireland, Italy, Luxembourg, Malta, Netherlands, Portugal, Slovenia, Spain. On January 1, 2009, Slovakia adopted the euro, and so is now part of the Eurozone. Though the Eurozone suffers from recession as a whole, Belgium, France, Greece, and Slovakia still have better growth.

Sources: en.wikipedia.org

Notes from published material

During the process of creating new queens, the workers construct special queen cells. The larvae in these cells are fed with copious amounts of royal jelly. This type of feeding in part triggers the development of queen morphology, including the fully developed ovaries needed to lay eggs. Note however that some newer research shows it is not solely the presence of royal jelly that develops the queen but rather the absence of certain other nutrients fed to worker bees. Royal jelly is sometimes used in alternative medicine under the category apitherapy. It is often sold as a dietary supplement for humans, but the European Food Safety Authority concluded in 2011 that evidence does not support the claim that consuming royal jelly offers health benefits to humans. In the United States, the Food and Drug Administration has taken legal action against companies that have marketed royal jelly products using unfounded claims of health benefits.

== Research == Both acute and chronic stress are under preliminary research for the potential to participate in insulin resistance. Experimental approaches for insulin resistance are under investigation, including stem cell-based therapies, extracellular vesicles such as exosomes, pharmacological combinations, and tissue-engineering platforms; however, these strategies remain primarily in the research stage and are not established standard treatments.

=== Circadian rhythm sleep disorders === Melatonin may be useful in the treatment of delayed sleep phase syndrome. Melatonin is known to reduce jet lag, especially in eastward travel. However, if it is not taken at the correct time, it can instead delay adaptation. Melatonin appears to have limited use against the sleep problems of people who work shift work. Tentative evidence suggests that it increases the length of time people are able to sleep. Meta-analyses, published between 2005 and 2017, appear to show different results as to whether melatonin is effective for circadian rhythm sleep disorders or not. Some found that it was effective, while others found no evidence of effectiveness. Meta-analyses of melatonin for delayed sleep phase syndrome that found it effective have reported that it improves time to sleep onset by about 40 minutes (0.67 hours) and advances onset of endogenous melatonin secretion by about 1.2 hours (72 minutes). One meta-analysis found that melatonin was notably more effective in improving sleep onset latency in people with delayed sleep phase syndrome than in people with insomnia (improvement of 39 minutes vs. 7 minutes, respectively). One meta-analysis found that melatonin was probably effective for jet lag syndrome.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine approved for human use?

No. Major drug regulators have not approved GW501516 for treating any medical condition. Products sold as cardarine are typically unapproved research chemicals or supplements, so their contents and safety are not assured.

Why is cardarine banned in sport?

It is prohibited by the World Anti-Doping Agency as a hormone and metabolic modulator. Athletes who test positive for GW501516 can face sanctions, including suspensions and loss of results.

What is the difference between cardarine and GW501516?

Cardarine is a common or trade-style name, while GW501516 is the research code for the same chemical entity. Some sources also use Endurobol or GSK-516. The names refer to the same compound, not distinct drugs.

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.

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