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Background And Regulatory Status — Worked Examples

By Editorial Desk · published 2026-06-17 · last reviewed 2026-07-04 · Topic

If you have been reading about Carcinogenicity 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.

Updated 2026-07-04. Numbers and descriptions here follow the published literature rather than marketing material.

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

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.

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.

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.

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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.

Further detail

where Ra, Rb, Rc, Rd are the radii in the circles externally tangent to the sides a, b, c, d respectively and the extensions of the adjacent two sides for each side. Several more characterizations are known in the four subtriangles formed by the diagonals.

== Books == Duttaroy, Asim K.; Spener, Friedrich (October 2003). Cellular Proteins and Their Fatty Acids in Health and Disease. Wiley-VCH, Germany. pp. 1–478. ISBN 978-3-527-60528-6. Duttaroy, Asim K.; Basak, Sanjay (October 2016). Human Placental Trophoblasts: Impact of Maternal Nutrition. CRC Press, USA. pp. 1–437. ISBN 978-1-4822-5428-0. Duttaroy, Asim K.; Basak, Sanjay (October 2017). Early Nutrition and Lifestyle Factors: Effects on First Trimester Placenta. Springer. pp. 1–159. doi:10.1007/978-3-319-38804-5. ISBN 978-3-319-38802-1. Duttaroy, Asim K. (June 2018). Nutraceuticals and Human Blood Platelet Function: Applications in Cardiovascular Health. Wiley. pp. 1–300. ISBN 978-1-119-37601-9.Duttaroy, Asim K. (July 2021). Evidence-Based Nutrition and Clinical Evidence of Bioactive Foods in Human Health and Disease. Elsevier. pp. 1–462. ISBN 978-0-128-22405-2.

== Early life and career == Natalie Paige Cochran (née Jessup; born November 1980) was born in Raleigh County, West Virginia. She pursued a career in pharmacy and married Michael Brandon Cochran in the early 2000s. The couple had two children and ran a contracting business during the 2010s, which later became central to her legal troubles.

This reconstituted organisation would bring the US and Canada, who were already OEEC observers, on board as full members, and the OEEC would set to work straight away on convincing Japan to join the organisation.

Magnesium has three stable isotopes: 24Mg, 25Mg and 26Mg. All are present in significant amounts in nature (see table of isotopes above). About 79% of Mg is 24Mg. The isotope 28Mg is radioactive and in the 1950s to 1970s was produced by several nuclear power plants for use in scientific experiments. This isotope has a relatively short half-life (21 hours) and its use was limited by shipping times. The nuclide 26Mg has found application in isotopic geology, similar to that of aluminium. 26Mg is a radiogenic daughter product of 26Al, which has a half-life of 717,000 years. Excessive quantities of stable 26Mg have been observed in the Ca-Al-rich inclusions of some carbonaceous chondrite meteorites. This anomalous abundance is attributed to the decay of its parent 26Al in the inclusions, and researchers conclude that such meteorites were formed in the solar nebula before the 26Al had decayed. These are among the oldest objects in the Solar System and contain preserved information about its early history. It is conventional to plot 26Mg/24Mg against an Al/Mg ratio. In an isochron dating plot, the Al/Mg ratio plotted is 27Al/24Mg. The slope of the isochron has no age significance, but indicates the initial 26Al/27Al ratio in the sample at the time when the systems were separated from a common reservoir.

Sources: en.wikipedia.org

Supporting material

In dispersive adhesion, also known as physisorption, two materials are held together by van der Waals forces: the attraction between two molecules, each of which has a region of slight positive and negative charge. In the simple case, such molecules are therefore polar with respect to average charge density, although in larger or more complex molecules, there may be multiple "poles" or regions of greater positive or negative charge. These positive and negative poles may be a permanent property of a molecule (Keesom forces) or a transient effect which can occur in any molecule, as the random movement of electrons within the molecules may result in a temporary concentration of electrons in one region (London forces).

== Personal life == For several years Dyson participated in Essendon's "On the Ball" program, which involved him and teammate Brent Prismall, as well as netball players Shelley O'Donnell and Bianca Chatfield, meeting with school groups and educating them on issues such as drug use and sports. Dyson took a year off from the program in 2008 to study and complete a personal training course.

=== Synthesis === The chemical synthesis of LSD has been described. It is commonly synthesized by reacting diethylamine with an activated form of lysergic acid. Activating reagents include phosphoryl chloride and peptide coupling reagents. Lysergic acid is made by alkaline hydrolysis of lysergamides like ergotamine, a substance usually derived from the ergot fungus on agar plate. Lysergic acid can also be produced synthetically, although these processes are not used in clandestine manufacture due to their low yields and high complexity. Albert Hofmann synthesized LSD in the following manner: (1) hydrazinolysis of ergotamine into D- and L-isolysergic acid hydrazide, (2) separation of the enantiomers with di-(p-toluyl)-D-tartaric acid to get D-isolysergic acid hydrazide, (3) enantiomerization into D-lysergic acid hydrazide, (4) substitution with HNO2 to D-lysergic acid azide and (5) finally substitution with diethylamine to form D-lysergic acid diethylamide. The precursor for LSD, lysergic acid, has been produced by GMO baker's yeast.

Synthetic Materials: Wennemers utilizes peptides to control the morphology of nanostructured materials for generation of ordered mesoscopic materials. She developed tripeptides for the size-controlled generation of mono-disperse, water-soluble silver-, palladium-, platinum-, and gold nanoparticles. Recently, she reported peptide‐stabilized platinum nanoparticles that have greater toxicity against hepatic cancer cells (HepG2) than against other cancer cells and non‐cancerous liver cells. Wennemers also explored conjugates of oligoprolines and π-conjugated systems that form hierarchical self-assemblies with diverse morphologies (e.g. nanofibers, nanorods, nanosheets). She used such a conjugate to prepare the first example of an extended triaxial supramolecular weave held together through the interplay of weak non-covalent interactions.

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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