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Identity And Regulatory Status — Research Overview

By Editorial Desk · published 2026-01-12 · last reviewed 2026-02-18 · Blog

A practical reference on Anti-doping testing: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

This page was last updated on 2026-02-18 and is reviewed periodically as new material appears.

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.

Detection, Stability, and Quality

Stability of GW501516 depends on form, temperature, light exposure, and moisture. Solid reference material is typically stored frozen or refrigerated in a desiccator and protected from light. Solutions in organic solvents such as dimethyl sulfoxide are often kept frozen in aliquots to reduce freeze-thaw cycling. Aqueous solubility is low, so aqueous stock solutions can be difficult to prepare without cosolvents. Degradation may appear as changes in chromatographic purity or mass spectral signal. Stability studies are needed to establish shelf life for any specific preparation.

Quality assessment for cardarine samples usually combines identity, purity, and impurity testing. Nuclear magnetic resonance spectroscopy and mass spectrometry can confirm molecular structure, while high-performance liquid chromatography estimates purity. Certificates of analysis from testing laboratories may list these results, but they do not establish safety or legality. In the absence of approved manufacturing, products sold online may contain the wrong compound, variable amounts, or unlisted contaminants. Independent verification is therefore central to analytical work and to interpreting any reported biological activity.

Laboratory detection of GW501516 commonly uses liquid chromatography coupled with tandem mass spectrometry. The method can identify the parent compound or its metabolites in urine and blood after sample cleanup. Protein precipitation, solid-phase extraction, or enzymatic hydrolysis may precede analysis, depending on the matrix. Reference standards are required for accurate quantification and confirmation. Because the compound is not approved, testing often occurs in anti-doping, forensic, or research settings rather than routine clinical care. Results are reported with limits of detection and quantification.

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

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.

A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.

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Preclinical Findings and Safety Signals

Safety concerns emerged from long-term animal studies. In rodents given the compound for extended periods, researchers found an increased incidence of certain cancers, including liver and bladder tumors. These findings contributed to the discontinuation of clinical development. Whether similar risks apply to short-term or low-level exposure in humans is not established, and controlled human safety data are limited. The relevance of high-dose rodent carcinogenicity findings to human use remains a subject of debate.

Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.

Laboratory studies indicate that GW501516 activates PPARδ, a nuclear receptor involved in fatty acid oxidation and energy metabolism. In rodent experiments, treated animals often showed increased endurance and reduced fat mass. These effects were observed under controlled conditions and do not establish safe or effective use in humans. The exact dose-response relationship in humans remains poorly characterized. Species differences in metabolism can affect how results translate across animals and people.

Notes from published material

Liquefied gases, such as liquid nitrogen and liquid helium, are used in many cryogenic applications. Liquid nitrogen is the most commonly used element in cryogenics and is legally purchasable around the world. Liquid helium is also commonly used and allows for the lowest attainable temperatures to be reached. These liquids may be stored in Dewar flasks, which are double-walled containers with a high vacuum between the walls to reduce heat transfer into the liquid. Typical laboratory Dewar flasks are spherical, made of glass and protected in a metal outer container. Dewar flasks for extremely cold liquids such as liquid helium have another double-walled container filled with liquid nitrogen. Dewar flasks are named after their inventor, James Dewar, the man who first liquefied hydrogen. Thermos bottles are smaller vacuum flasks fitted in a protective casing. Cryogenic barcode labels are used to mark Dewar flasks containing these liquids, and will not frost over down to −195 degrees Celsius. Cryogenic transfer pumps are the pumps used on LNG piers to transfer liquefied natural gas from LNG carriers to LNG storage tanks, as are cryogenic valves.

Opioids by themselves put older people at risk of respiratory depression and impaired ability to operate vehicles and other machinery. Combining these two drugs together not only increases a person's risk of the aforementioned adverse effects, but can increase a person's risk of overdose and death. Benzodiazepines are also the second leading cause of teen overdose death after fentanyl. They killed 152 people in 2021, less than a fifth of fentanyl's death toll. Hydrocodone was declared the most widely prescribed opioid between 2007 and 2016, and in 2015 the International Narcotics Control Board reported that greater than 98% of the hydrocodone consumed in the entire world was consumed by Americans.

==== NIH Interagency Pain Research Coordinating Committee ==== On February 13, 2012, the National Institutes of Health (NIH) announced a new group of individuals assigned to research pain. This committee is composed of researchers from different organizations and will focus to "coordinate pain research activities across the federal government with the goals of stimulating pain research collaboration… and providing an important avenue for public involvement" ("Members of new", 2012). With a committee such as this research will not be conducted by each individual organization or person but instead a collaborating group which will increase the information available. With this hopefully more pain management will be available including techniques for those with arthritis. In 2020 Beth Darnall, American scientist and pain psychologist, was appointed as scientific member of the group.

JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR). JDTic is a 4-phenylpiperidine derivative, distantly related structurally to analgesics such as pethidine and ketobemidone, and more closely to the MOR antagonist alvimopan. In addition, it is structurally distinct from other KOR antagonists such as norbinaltorphimine. JDTic has been used to create crystal structures of KOR [ PDB: 4DJH, 6VI4​].

Sources: en.wikipedia.org

Further detail

== Background == Scientists have debated whether umami was a basic taste since Kikunae Ikeda first proposed its existence in 1908. In 1985, the term umami was recognized as the scientific term to describe the taste of glutamates and nucleotides at the first Umami International Symposium in Hawaii. Umami represents the taste of the amino acid L-glutamate and 5'-ribonucleotides such as "inosinate and guanylate". (guanosine monophosphate, GMP, and inosine monophosphate, IMP). It can be described as a pleasant "brothy" or "meaty" taste with a long-lasting, mouthwatering, and coating sensation over the tongue. Umami enhances the palatability of a wide variety of foods. Studies in genetically engineered mice in which individual TAS1R genes have been deleted indicate that the TAS1R1/TAS1R3 complex is solely responsible for umami taste, whereas TAS1R2/TAS1R3 is solely responsible for sweet taste. As expected, a genetic knockout of TAS1R1 selectively abolishes umami taste, a knockout of TAS1R2 specifically abolishes sweet taste, while a knockout of TAS1R3 eliminates both sweet and umami taste. Specialized taste bud cells detect the chemical species perceived as umami by humans. Glutamate in acid form (glutamic acid) imparts little umami taste, whereas the salts of glutamic acid, known as glutamates, give the characteristic umami taste due to their ionized state. GMP and IMP amplify the taste intensity of glutamate. Adding salt to the free acids also enhances the umami taste.

==== Oligoarticular arthritis (Oligoarthritis) ==== Oligoarticular (or pauciarticular) JIA is the most common JIA subtype, and occurs when there are up to four joints involved during the first six months of disease. Two subtypes of oligoarticular arthritis exist: persistent oligoarthritis, where no more than four joints are affected throughout the whole disease course; and extended oligoarthritis, where more than four joints are affected after the first six months of disease. Patients in this subtype are often young, typically aged between 1 and 5 years, and are female preponderant. The most commonly involved joint is the knee, but other affected joints may include the ankles, wrists, elbows, and others. 50% of cases involve mono-arthritis, only involving the knee. The anti-nuclear antigen (ANA) is positive in up to 80% of patients with oligoarthritis and is associated with a higher risk of associated eye disease (uveitis), particularly in younger patients. There is no adult counterpart disease to oligoarticular JIA. The prefixes oligo- and pauci- mean 'few'.

A nitrogen atom has seven electrons. In the ground state, they are arranged in the electron configuration 1s22s22p1x2p1y2p1z. It, therefore, has five valence electrons in the 2s and 2p orbitals, three of which (the p-electrons) are unpaired. It has one of the highest electronegativities among the elements (3.04 on the Pauling scale), exceeded only by chlorine (3.16), oxygen (3.44), and fluorine (3.98). (The light noble gases, helium, neon, and argon, would presumably also be more electronegative, and in fact are on the Allen scale.) Following periodic trends, its single-bond covalent radius of 71 pm is smaller than those of boron (84 pm) and carbon (76 pm), while it is larger than those of oxygen (66 pm) and fluorine (57 pm). The nitride anion, N3−, is much larger at 146 pm, similar to that of the oxide (O2−: 140 pm) and fluoride (F−: 133 pm) anions. The first three ionisation energies of nitrogen are 1.402, 2.856, and 4.577 MJ·mol−1, and the sum of the fourth and fifth is 16.920 MJ·mol−1. Due to these very high figures, nitrogen has no simple cationic chemistry. The lack of radial nodes in the 2p subshell is directly responsible for many of the anomalous properties of the first row of the p-block, especially in nitrogen, oxygen, and fluorine. The 2p subshell is very small and has a very similar radius to the 2s shell, facilitating orbital hybridisation. It also results in very large electrostatic forces of attraction between the nucleus and the valence electrons in the 2s and 2p shells, resulting in very high electronegativities.

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.

How is cardarine measured in biological samples?

LC-MS/MS is common, often after sample cleanup. The assay targets GW501516 or its metabolites.

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