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Identity And Regulatory Status — Explained

By Editorial Desk · published 2026-04-24 · last reviewed 2026-05-25 · Blog

The short version of GW501516 fits in a sentence. The long version — which is the one that helps — is below.

Reviewed 2026-05-25. Anything still debated is marked as such rather than presented as settled.

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.

Regulation and Analytical Detection

Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.

Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.

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

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.

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Mechanism and Detection Methods

Detection of GW501516 in biological samples generally relies on liquid chromatography coupled with tandem mass spectrometry. Urine is a common matrix in anti-doping analysis, while blood or plasma may be used in research settings. Sample preparation can involve enzymatic hydrolysis, protein precipitation, or solid-phase extraction before instrumental analysis. Because the compound undergoes metabolism, assays may target the parent molecule, one or more metabolites, or both. Detection windows are not fixed; they depend on factors such as dose, route, individual metabolism, and assay sensitivity. Reference standards are required for accurate identification and quantification.

Handling and quality assessment of cardarine reference material follow general laboratory practices for poorly characterized compounds. It typically appears as a white to off-white powder and is sparingly soluble in water but soluble in organic solvents such as dimethyl sulfoxide and ethanol. Storage recommendations usually specify a cool, dry, dark place, with long-term storage at low temperature and desiccation. Purity may be checked by high-performance liquid chromatography with ultraviolet detection, while identity is confirmed by mass spectrometry and nuclear magnetic resonance. No pharmacopeial monograph exists, so reported purity and stability depend on the supplier’s methods.

GW501516 acts as a selective agonist at PPARδ, a nuclear receptor that regulates transcription of genes involved in lipid handling and energy metabolism. Activation of PPARδ in preclinical models increases fatty acid oxidation, mitochondrial biogenesis, and exercise endurance in rodents. These effects have made the compound a subject of metabolic research and also a target for sport anti-doping rules. In humans, however, controlled studies are limited, and whether similar endurance or metabolic changes occur at tolerated exposures remains an open question. The receptor’s broad tissue distribution also means downstream effects may vary by organ and condition.

Background from the literature

Deep learning uses several layers of neurons between the network's inputs and outputs. The multiple layers can progressively extract higher-level features from the raw input. For example, in image processing, lower layers may identify edges, while higher layers may identify the concepts relevant to a human such as digits, letters, or faces. Deep learning has been used to improve the performance of programs in subfields of artificial intelligence including computer vision, speech recognition, natural language processing, image classification and others. Deep neural networks and backpropagation had been in development since 1950. Starting in 2012, the speed of deep learning was increased one hundred-fold by switching to GPUs, and there were enormous amounts of data available on the internet (called at the time "big data") as well as curated datasets used for benchmark testing, such as ImageNet. Usage of deep learning increased in 2012–2015 due to these improvements. In 2025, Geoffrey Hinton said that, until the 2010s, "We couldn't do anything very impressive because we didn’t have enough data and we didn't have enough computation."

Following the end of the Chadian-Libyan conflict, relations with Libya were normalised in 1994. Starting in the mid-1990s, the AAT started to grow slowly but steadily. In 1995, two second-hand Aérospatiale Alouette IIIs were bought from the Netherlands. Two Mil Mi-24Ds and one Mil Mi-17 were also purchased in the late 1990s. Libya donated two Antonov An-26s in the same period, and two SIAI-Marchetti SF.260s in 2006. Two Mi-24Vs were delivered from Ukraine in 2000, as well as four Mi-17s in 2001 and 2006. Four more Mi-24Vs were delivered from the same source in 2007–2008. The expansion of the AAT in this period was fuelled by royalties from oil exports that started in the mid-2000s. In 2005, one of the two PC-7s donated by France in the 1980s was overhauled by the company Griffon Aerospace, which also bought another on the civilian market in the United States. The same company then purchased a single Pilatus PC-9 directly from Swiss manufacturer Pilatus Aircraft, and contracted around 50 French, Algerian and Mexican personnel to serve in the AAT. Griffon Aerospace then proceeded to modify one Mi-17V-5, three Mi-24Vs and the PC-9 with hardpoints allowing them to carry Mark 81 and Mark 82 bombs, sourced from Pakistan. The three Mi-24Vs were also made compatible with night-vision goggles. The weaponisation of the PC-9 caused a scandal in Switzerland, as the Chadian government had promised it would not be used in a combat role. This affair marked the end of Griffon Aerospace's work in Chad, and all of its employees left the country by March 2008.

The increase of activity is due to the interlocking labyrinth of the basal lamina creating a crosscurrent activity similar to the mitochondrial-rich cells found in teleost marine fish. The lacuna-forming cells are characterized by contact to the basal lamina, but not reaching the apical rim of the associated epithelial cells and are located in the branchial heart epithelium. The shape varies widely and are occasionally more electron-dense than the epithelial cells, seen as a "diffused kidney" regulating ion concentrations. One adaptation that O. vulgaris has is some direct control over its kidneys. It is able to switch at will between the right or left kidney doing the bulk of the filtration, and can also regulate the filtration rate so that the rate does not increase when the animal's blood pressure goes up due to stress or exercise. Some species of octopuses, including O. vulgaris, also have a duct that runs from the gonadal space into the branchial pericardium. Wells theorized that this duct, which is highly vascularized and innervated, may enable the reabsorption of important metabolites from the ovisac fluid of pregnant females by directing this fluid into the renal appendages.

A nanodisc is a synthetic model membrane system which assists in the study of membrane proteins. Nanodiscs are discoidal proteins in which a lipid bilayer is surrounded by molecules that are amphipathic molecules including proteins, peptides, and synthetic polymers. It is composed of a lipid bilayer of phospholipids with the hydrophobic edge screened by two amphipathic proteins. These proteins are called membrane scaffolding proteins (MSP) and align in double belt formation. Nanodiscs are structurally very similar to discoidal high-density lipoproteins (HDL) and the MSPs are modified versions of apolipoprotein A1 (apoA1), the main constituent in HDL. Nanodiscs are useful in the study of membrane proteins because they can solubilise and stabilise membrane proteins and represent a more native environment than liposomes, detergent micelles, bicelles and amphipols. The art of making nanodiscs has progressed past using only the MSPs and lipids to make particles, leading to alternative strategies like peptide nanodiscs that use simpler proteins and synthetic nanodiscs that do not need any proteins for stabilization.

Sources: en.wikipedia.org

Reference notes

== Legality == Plant breeding is subject to a different set of rules and regulations, at times contradictory. The International Union for the Protection of New Varieties of Plants (UPOV Convention) grants limited proprietary rights to breeders over their seeds, under certain conditions. In parallel, and often in a conflicting way, a series of dispositions aiming to fight against biopiracy require breeders to prove that the free, prior and informed consent was obtained from the communities (often Indigenous peoples or peasant communities) from where the seeds used to breed the new variety originates. This is the case in particular of the Nagoya Protocol, a treaty complementing the Convention on Biological Diversity, in force since 2014 (2017 in the European Union). In 2024, the GRATK Treaty was adopted, preventing national patent offices from granting patents based on biopiracy. Patent applicants relying on Cannabis strains will have to disclose the origin of the variety, which often entails compliance under the Nagoya protocol or other similar mechanisms of Access and Benefit Sharing Agreement.

facultative expression The transcription of a gene only as needed, as opposed to constitutive expression, in which a gene is transcribed continuously. A gene that is transcribed as needed is called a facultative gene.

=== The production of amino acids from inorganic molecules === Sidney Fox based his experiments off of the information found in the Miller–Urey experiment. The Miller–Urey experiment was performed by scientist Stanley Miller under the guidance of Harold Urey in the early 1950s. In the Miller–Urey experiment, water was boiled in a flask with the gases hydrogen, ammonia, and methane. The gases flowed through the apparatus past two electrodes that produced an electrical charge that acted as the lightning that would have been in the atmosphere before life on Earth. When the gases condensed after being cooled down, they fell back into the boiling flask. What Stanley Miller found in the flask when he observed the water were acids and amino acids. Amino acids are the necessary "building block" molecules for proteins. Stanley Miller and Harold Urey's experiment suggests that life formed from the presence of inorganic molecules, water, and electrical charge. These conditions are assumed to be similar to those of primordial earth. In 1964, Fox and Kaoru Harada performed an experiment yielding similar results. In this experiment, methane flowed through a concentrated solution of ammonium hydroxide and then into a hot tube containing silica sand at about 1000 °C. Fox indicated that silica gel, volcanic lava, and alumina could be used in place of silica sand. The gas was then absorbed in cold, aqueous ammonia.

Sources: en.wikipedia.org

Reference notes

Drug-related violence remained at previous levels during the first months of López Obrador's presidency. In October 2019, a National Guard operation in Culiacán, Sinaloa to capture Ovidio Guzmán López, responding to a U.S. extradition request, failed after cartel gunmen took hostages and forced his release. Guzmán was released after approximately 700 cartel enforcers took multiple hostages, including the housing unit where military families live in Culiacán. López Obrador defended the decision to release Guzmán López, arguing it prevented further loss of life, and insisted that he wanted to avoid more massacres, and that even though they underestimated the cartel's forces and ability to respond, the criminal process against Ovidio is still ongoing. Guzmán López was captured in a 2023 operation and extradited to the U.S. The strategy of avoiding armed confrontations while drug organizations have continued violent altercations has been controversial. The Jalisco New Generation Cartel (CJNG) expanded aggressively during López Obrador's presidency, and its territorial disputes were linked to significant increases in homicide rates in Colima, Zacatecas, Guanajuato, and Jalisco. In July 2022, authorities captured Rafael Caro-Quintero, a former leader of the Guadalajara Cartel. Despite his campaign promises, military deployments and expenditures have risen, with troop levels 76% higher and defense spending up 87% between 2012 and 2022.

The protecting group is abbreviated Cbz or, in honour of Zervas, simply Z. The typical route for deprotection involves hydrogenolysis under mild conditions e.g. with hydrogen gas and a catalyst such as palladium on charcoal. The discovery of the Bergmann-Zervas synthesis has been characterised as "epoch-making" as it allowed the advent of controlled synthetic peptide chemistry, completing the work started in the early 20th century by Bergmann's mentor Emil Fischer. Previously impossible to synthesise oligopeptides with a highly specific sequence and reactive side chains were consequently produced in the 1930s by Bergmann and Zervas. The ability of Z-protection to prevent racemization of activated derivatives of the protected amino acids and the importance thereof were also noted by the two chemists. Indeed, their method became the standard in the field for the following two decades until further developments in the early 1950s with the introduction of mixed anhydrides (e.g. the Boc group).

Spondyloepiphyseal dysplasia congenita (SEDc, also known as Spranger-Wiedemann disease) is a type of autosomal dominant dwarfism caused by mutations in the COL2A1 gene. Spondyloepiphyseal dysplasia congenita is present in 1 in 100,000 births, though many children are stillborn, premature, or die shortly after birth. This disorder is characterized by delayed ossification, particularly of the spine and the proximal ends of long bones (epiphyses).

=== Otospondylomegaepiphyseal dysplasia === Approximately 10 mutations identified in the COL11A2 gene are responsible for otospondylomegaepiphyseal dysplasia (OSMED). Most of these mutations result in a complete lack of pro-alpha2(XI) chains, which leads to a loss of function of type XI collagen. Some mutations affect the production of the pro-alpha2(XI) chain and disrupt normal collagen assembly. Because this type of collagen is an important component of cartilage and other connective tissues, these mutations result in the characteristic signs and symptoms of OSMED.

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 legal to buy?

Legal status varies by country, but cardarine is not approved as a medicine in major jurisdictions. It is often sold as a research chemical, a category that may not be lawful for human use. Buyers should check local laws and product labels carefully.

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