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Background And Regulatory Status — What the Evidence Shows

By Editorial Desk · published 2026-04-07 · last reviewed 2026-04-25 · Faq

LC-MS/MS comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.

Updated 2026-04-25. Numbers and descriptions here follow the published literature rather than marketing material.

Background and Regulatory Status

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.

Cardarine is a common name for GW501516, a synthetic compound first described in the 1990s as a selective agonist of the peroxisome proliferator-activated receptor delta. It was studied in preclinical models for metabolic and cardiovascular conditions, but it has not been approved as a medicine in the United States, Europe, or other major jurisdictions. Retail products labeled as cardarine are generally research chemicals or supplements, not pharmaceutical formulations. Because human safety and efficacy data remain limited, regulatory agencies treat it as an unapproved substance rather than a therapeutic product.

Mechanism and Safety Research

Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.

GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.

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

Regulation and Detection

Anti-doping laboratories identify GW501516 and related metabolites using liquid chromatography coupled with tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be analyzed. The method targets the parent compound and phase I and phase II metabolites, which extend the detection window. Because the substance is prohibited at all times, athletes can be tested outside competition. Detection limits and windows depend on the assay, sample type, and individual metabolism.

Cardarine is frequently described as a fat-burning or endurance-enhancing supplement, but these claims exceed the available evidence. The compound is not a hormone, steroid, or selective androgen receptor modulator. Research articles discuss it as a tool compound for studying PPARδ biology, while anti-doping literature focuses on its abuse and detection. Quality of unapproved products is uncertain, and independent analyses have found impurities or incorrect labeling. Open questions include whether human cancer risk resembles that seen in rodents and how often non-athletes use the substance.

Cardarine has no approved therapeutic indication and is not marketed as a medicine. The World Anti-Doping Agency lists GW501516 as a prohibited substance at all times, covering both in-competition and out-of-competition periods. National laws vary: some countries treat it as an unapproved drug subject to import controls, while others have specific restrictions on sale for human consumption. It is often sold as a research chemical, a label that does not imply safety or legality. Enforcement actions have targeted online vendors and shipments.

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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.

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.

Identity and Pharmacological Mechanism

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 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.

Background from the literature

== Hyperfibrinogenemia == Levels of functionally normal fibrinogen increase in pregnancy to an average of 4.5 gram/liter (g/L) compared to an average of 3 g/L in non-pregnant people. They may also increase in various forms of cancer, particularly gastric, lung, prostate, and ovarian cancers. In these cases, the hyperfibrinogenemia may contribute to the development of pathological thrombosis. A particular pattern of migratory superficial vein thrombosis, termed trousseau's syndrome, occurs in, and may precede all other signs and symptoms of, these cancers. Hyperfibrinogenemia has also been linked as a cause of persistent pulmonary hypertension of the newborn and post-operative thrombosis. High fibrinogen levels had been proposed as a predictor of hemorrhagic complications during catheter-directed thrombolysis for acute or subacute peripheral native artery and arterial bypass occlusions. However, a systematic review of the available literature until January 2016 found that the predictive value of plasma fibrinogen level for predicting hemorrhagic complications after catheter-directed thrombolysis is unproven.

== Composition == The prepreg matrix consists of a mixture of resin and hardener, in some cases an accelerator. Freezing at -20 °C prevents the resin from reacting with the hardener. If the cold chain is interrupted, the reaction starts and the prepreg becomes unusable. There are also high-temperature prepregs which can be stored for a certain time at room temperature. These prepregs can then be cured only in an autoclave at elevated temperature.

Provisioning for sea was crucial in the 19th century due to the lack of modern conveniences such as refrigeration, freeze-drying and canning. Most foodstuffs and liquids such as spirits, molasses, vinegar, and water, were shipped in casks, the balance in wooden crates and other suitable packing materials. It was also commonplace to carry live chickens, both for their eggs and meat, and some small livestock such as sheep, which were butchered when their feed ran out, providing fresh meat before barreled stores such as beef and salt pork were consumed. The fare for officers and rations for the crew were distinct, as were dining accommodations, with each reflecting their relative stations in society and the navy. Due to the inability to maintain water fresh for extended periods of time prior to the advent of modern hygiene, shipboard plumbing, and disinfectants, it was common to ship large quantities of beer to provide both hydration and nourishment in times when water aboard fouled. The beer's alcoholic content served as a preservative. In contrast, grog, a mix of rum and water, was provided and consumed daily (with officers provided their rum straight). The rum allotment per man was retained in the United States Navy until the latter part of the 19th century, and all the way until 1970 in the British Royal Navy.

1945 In the US, the Gerontological Society of America is formed. The founder is Edmund Vincent Cowdry. 1950 Largely thanks to the collaborative efforts of Korenchevsky and Cowdry, the International Association of Gerontology is formed, later renamed to the International Association of Gerontology and Geriatrics (IAGG). The organization was registered in Belgium, and that is where its first conference took place. Slowly, gradually, the ideas began to spread that the problems of aging cannot be solved within the framework and efforts of one nation – therefore the international interaction is necessary. 1952 Peter Medawar proposed the mutation accumulation theory to explain how the aging process could have evolved. 1954 Vladimir Dilman formulated the hypothesis of aging that at first become known only in the USSR, as the elevation hypothesis. In 1968 it took the form and became known as the neuroendocrine theory of aging. 1956 Denham Harman proposed the free-radical theory of aging and demonstrated that free radical reactions contribute to the degradation of biological systems. The theory is based on the ideas of Rebeca Gerschman and her colleagues put forward in 1945. 1957 George Williams proposed the antagonistic pleiotropy hypothesis for the explanation of the emergence of aging. 1958 Physicist Gioacchino Failla proposed the hypothesis that aging is caused by the accumulation of DNA damage. The next year the hypothesis was developed by the physicist Leo Szilard, resulting in a number of related theories under the general name DNA damage theory of aging.

X chromosome One of two sex chromosomes present in organisms which use the XY sex-determination system, and the only sex chromosome in the X0 system. The X chromosome is found in both males and females and typically contains much more gene content than its counterpart, the Y chromosome.

Sources: en.wikipedia.org

Reference notes

=== Biomedical applications === Because of their relatively large surface area, CNTs are capable of interacting with a wide variety of therapeutic and diagnostic agents (drugs, genes, vaccines, antibodies, biosensors, etc.). This can be utilized to assist in drug delivery directly into cells. In addition, CNTs have recently been used as reinforcements in implants and scaffolds due to their suitable reaction area, high elastic modulus, and load transfer capability.

=== Absolute specificity === Absolute specificity can be thought of as being exclusive, in which an enzyme acts upon one specific substrate. Absolute specific enzymes will only catalyze one reaction with its specific substrate. For example, lactase is an enzyme specific for the degradation of lactose into two sugar monosaccharides, glucose and galactose. Another example is Glucokinase, which is an enzyme involved in the phosphorylation of glucose to glucose-6-phosphate. It is primarily active in the liver and is the main isozyme of Hexokinase. Its absolute specificity refers to glucose being the only hexose that is able to be its substrate, as opposed to hexokinase, which accommodates many hexoses as its substrate.

==== Transparency ==== Neural networks have often been described as black boxes, meaning that it is difficult to understand why they make the decisions they do as a result of the massive number of computations they perform. This makes it challenging to anticipate failures. In 2018, a self-driving car killed a pedestrian after failing to identify them. Due to the black box nature of the AI software, the reason for the failure remains unclear. It also raises debates in healthcare over whether statistically efficient but opaque models should be used. One critical benefit of transparency is explainability. It is sometimes a legal requirement to provide an explanation for why a decision was made in order to ensure fairness, for example for automatically filtering job applications or credit score assignment. Another benefit is to reveal the cause of failures. At the beginning of the 2020 COVID-19 pandemic, researchers used transparency tools to show that medical image classifiers were 'paying attention' to irrelevant hospital labels. Transparency techniques can also be used to correct errors. For example, in the paper "Locating and Editing Factual Associations in GPT", the authors were able to identify model parameters that influenced how it answered questions about the location of the Eiffel tower. They were then able to 'edit' this knowledge to make the model respond to questions as if it believed the tower was in Rome instead of France. Though in this case, the authors induced an error, these methods could potentially be used to efficiently fix them.

== Adverse effects == Acitretin is highly teratogenic and noted for the possibility of severe birth defects, such as abnormal development in the face and skull, as well as spinal, hip, forearm, and ear deformations. It should not be used by pregnant women or women planning to get pregnant within 3 years following the use of acitretin. Sexually active women of childbearing age who use acitretin should also use at least two forms of birth control concurrently. Men and women who use it should not donate blood for three years after using it, because of the possibility that the blood might be used in a pregnant patient and cause birth defects. In addition, it may cause nausea, headache, itching, dry, red or flaky skin, dry or red eyes, dry or chapped lips, swollen lips, dry mouth, thirst, cystic acne or hair loss.

Sources: en.wikipedia.org

Reference notes

== Contraindications == Use of verapamil is generally avoided in people with severe left ventricular dysfunction, hypotension (systolic blood pressure less than 90 mm Hg), cardiogenic shock, and hypersensitivity to verapamil. It is also contraindicated in people with atrial flutter or fibrillation and an existing accessory tract such as in Wolff-Parkinson-White syndrome.

Writer G. Pascal Zachary argues in a Wired essay that legalizing performance-enhancing substances, as well as genetic enhancements once they became available, would satisfy society's need for übermenschen and reverse the decline in public interest in sports. Sports scholar Verner Moller argues that society is hypocritical when it holds athletes to moral standards, but do not conform to those morals themselves. Fox Sports writer Jen Floyd Engel stated in an article, "We live in a pharmacological society. We live in a society of short cuts, of fake this and enhanced that, and somehow we keep trying to sell the line that sports has become this evil empire of cheating. The reality is athletes are merely doing what so many of us do and celebrate and watch every single day of our lives." Sociologist Ellis Cashmore argues that what is considered doping is too arbitrary: transfusing blood cells is not allowed, but other methods of boosting blood cell count, such as hypobaric chambers, are allowed. Other scholars have advanced similar arguments. In 2023, Australian businessman Aron D'Souza announced the Enhanced Games, a sports event permitting doping. British academic Byron Hyde criticized the Games for coercing retired athletes on low salaries into participating with large financial incentives, but observed that many other sports also coerce athletes into harming themselves for fame or money, including the Olympics. He observed that athletes increasingly face an "enhance or retire" dynamic.

In the diagram below, consider the amino-acids as single aliphatic monomers reacting with identical molecules to form a polyamide, focusing on solely the amine and acid groups. Ignore the substituent R groups – under the assumption the difference between the R groups are negligible:

While acknowledging the Marxist influence on Gaddafi's thought, Bearman stated that the Libyan leader rejected Marxism's core tenet, that of class struggle as the main engine of social development. Instead of embracing the Marxist idea that a socialist society emerged from class struggle between the proletariat and bourgeoisie, Gaddafi believed that socialism would be achieved through overturning "unnatural" capitalism and returning society to its "natural equilibrium". In this, he sought to replace a capitalist economy with one based on his own romanticized ideas of a traditional, pre-capitalist past. This owed much to the Islamic belief in God's natural law providing order to the universe.

=== Other === An engineer replaced a woodpecker-damaged feed horn of a high-power microwave antenna, a 15-meter dish at an Earth station of a television network, using a cherry picker. After finishing, he sent his technician to power up the transmitter, and attempted to lower the cherry picker down. The engine failed and the engineer was stuck next to the antenna, outside of its main lobe but well within the first sidelobe. The technician, unaware that the engineer was still close to the antenna, powered it up. The engineer was exposed to an intense microwave field for about three minutes, until the error was realized. There were no immediate symptoms; the next morning the engineer detected blood and solid matter in his urine, and visited a doctor, who found blood in stool and massive bowel adhesions. The engineer's medical problems lasted for many years.

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 the main molecular target of cardarine?

It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.

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