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Background And Regulatory Status — Deep Dive

By Editorial Desk · published 2026-05-16 · last reviewed 2026-06-06 · News

PPARδ raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.

Reviewed 2026-06-06. Anything still debated is marked as such rather than presented as settled.

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.

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

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.

Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.

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.

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

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.

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.

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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.

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.

Supporting material

In enzymology, an aromatic 2-oxoacid reductase (EC 1.1.1.110, previously indolelactate dehydrogenase) is an enzyme that catalyzes the reversible oxidation and reduction of aryllactate compounds to arylpyruvate compounds using the redox cofactor nicotinamide adenine dinucleotide or the similar nicotinamide adenine dinucleotide phosphate. For example, the enzyme may oxidize (R)-3-(4-hydroxyphenyl)lactate to 3-(4-hydroxyphenyl)pyruvic acid.

About 75% can be found in the dorsal area. Most of the congenital type-III cysts can be found posteriorly to the spinal cord, as opposed to those caused by trauma which can be found anteriorly to the spinal cord.Post traumatic inflammation induces cavitation and cystic formation and leads to greater secondary CNS injury. Cellular migration causing these cyst cavities was observed both in vitro and in vivo and cavitation was observed to be prevented with the use of an anti-inflammatory. Further more migration inflammatory cells into traumatized tissue has been observed with inflammation.

Absorption spectroscopy techniques (e.g., FTIR, ultraviolet-visible ("UV-vis") spectroscopy) measure how much light a sample absorbs at each wavelength. The most straightforward way to do this, the "dispersive spectroscopy" technique, is to shine a monochromatic light beam at a sample, measure how much of the light is absorbed, and repeat for each different wavelength. The dispersive spectroscopy technique is used by some UV–vis spectrometers to take measurements. Fourier transform spectroscopy is a less intuitive way to obtain the same information. Rather than shining a monochromatic beam of light (a beam composed of only a single wavelength) at the sample, this technique shines a beam containing many frequencies of light at once and measures how much of that beam is absorbed by the sample. Next, the beam is modified to contain a different combination of frequencies, giving a second data point. This process is rapidly repeated many times over a short time span. Afterwards, a computer takes all this data and works backward to infer what the absorption is at each wavelength. The beam described above is generated by starting with a broadband light source—one containing the full spectrum of wavelengths to be measured. The light shines into a Michelson interferometer—a certain configuration of mirrors, one of which is moved by a motor. As this mirror moves, each wavelength of light in the beam is periodically blocked, transmitted, blocked, transmitted, by the interferometer, due to wave interference.

Sources: en.wikipedia.org

Notes from published material

== Osmium isotopes in radiometric dating == The isotopic ratio of osmium-187 and osmium-188 (187Os/188Os) can be used as a window into geochemical changes throughout the ocean's history. The average marine 187Os/188Os ratio in oceans is 1.06. This value represents a balance of the continental riverine inputs of Os with a 187Os/188Os ratio of ~1.3, and the mantle/extraterrestrial inputs with a 187Os/188Os ratio of ~0.13. The lighter isotope, 187Os, is produced by beta decay of 187Re. This decay has actually increased the 187Os/188Os ratio of the bulk silicate earth (Earth less the core) by 33%. The difference between crust and mantle ratios is explained this way: crustal rocks have a much higher level of rhenium. Re is concentrated in the crust relative to the mantle due to partial melting of the mantle (differentiation). Because Re is partitioned into the melt more than other PGEs, it increases in the crust over time.}, which produces an excess of 187Os. The combined input of the two sources to the marine environment results in the observed ratio in the oceans, and has fluctuated over the geologic history. These changes in the isotopic values of marine Os can be observed in the marine sediment that is deposited, and eventually lithified in that time period. This allows for researchers to estimate weathering fluxes, flood basalt volcanism, and impact events that may have caused some of our largest mass extinctions. The marine sediment Os isotope record has corroborated the K-T boundary impact, for example.

3 August – Dogxim, the now-dead first known hybrid of a fox and a domesticated dog, discovered in the wild in Brazil in 2021, is reported. 8 August Walking more than 3,967 steps each day is shown to reduce the risk of dying prematurely of any cause, based on a study of 226,000 people around the world. This is considerably less than previous recommendations, which have sometimes cited a figure of 10,000+ steps being needed each day. A study shows activating astrocyte cells in mice with a novel technique makes them stay awake for much longer without making them sleepier or impacting cognition-associated EEG markers. 10 August – Scientists at Fermilab report the most precise measurement yet of the magnetic moment of the muon. The particles are shown to wobble faster than predicted by the Standard Model, hinting at a possible fifth fundamental force. 11 August The rise in photosynthesis rates around the world caused by the increase of carbon dioxide is found to have slowed dramatically in the 21st century, as the atmosphere has grown drier. A global consortium releases two studies and a database on DNA methylation profiles across 348 mammalian species for use in epigenetic clocks. They provide various new results relating to human aging and animal experiments as well as predictive models that can estimate mammalian tissue age or risk with high accuracy. On 16 August, a study indicates chest radiographs evaluated using AI could be a performant biomarker for aging clocks.

The education system is divided into three parts: basic education, secondary cycle, and tertiary education. "Basic education" lasts 11 years (ages 4‒15). It is divided into kindergarten (two years), primary school (two modules of three years) and junior high (three years). Junior high school ends with the Basic Education Certificate Examination. Once certified, the pupil can proceed to the secondary cycle. Hence, the pupil has the choice between general education (offered by the senior high school) and vocational education (offered by the technical senior high school or the technical and vocational institutes). Senior high school lasts three years and leads to the West African Senior School Certificate Examination, which is a prerequisite for enrollment in a university bachelor's degree programme. Polytechnics are open to vocational students. A bachelor's degree requires four years of study. It can be followed by a one- or two-year master's degree programme, which can be followed by a PhD programme of at least three years. A polytechnic programme lasts two or three years. Ghana possesses colleges of education. Some of the universities are the University of Ghana, Kwame Nkrumah University of Science and Technology, and University of Cape Coast. There are more than 95% of children in school. The literacy rate of youth ages 15 to 24 years old was 81% in 2010, with males at 82%, and females at 80%. The education system annually attracts foreign students, particularly in the university sector.

Sources: en.wikipedia.org

Background from the literature

== Pathogenesis == Micrococcus is generally thought to be a saprotrophic or commensal organism, though it can be an opportunistic pathogen, particularly in hosts with compromised immune systems, such as HIV patients. It can be difficult to identify Micrococcus as the cause of an infection, since the organism is normally present in skin microflora, and the genus is seldom linked to disease. In rare cases, death of immunocompromised patients has occurred from pulmonary infections caused by Micrococcus. Micrococci may be involved in other infections, including recurrent bacteremia, septic shock, septic arthritis, endocarditis, meningitis, and cavitating pneumonia (immunosuppressed patients).

An insulin pump allows the replacement of slow-acting insulin for basal needs with a continuous infusion of rapid-acting insulin. The insulin pump delivers a single type of rapid-acting insulin in two ways:

=== China === In China, the use of IUDs by state health services was part of the government's efforts to limit birth rates. From 1980 to 2014, 324 million women were inserted with IUDs, in addition to the 107 million who had tubal ligation. Until the mid-1990s, the state-preferred IUD was a stainless steel ring, which had a higher rate of complications compared to other types of IUD. It gave rise to the idiom shànghuán (上环), meaning "insert a loop". Since then, IUDs include T and V shapes, the former being the most common and easiest to remove.

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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