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Background And Regulatory History — Background and Details

By Editorial Desk · published 2026-04-18 · last reviewed 2026-05-09 · Wiki

Everything below concerns research chemical. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Updated 2026-05-09. Numbers and descriptions here follow the published literature rather than marketing material.

Background and Regulatory History

Cardarine is a common name for the investigational chemical GW501516, also written GW-1516. It was developed as a peroxisome proliferator-activated receptor delta agonist for metabolic conditions such as dyslipidemia. Early research focused on lipid handling and energy use in skeletal muscle and other tissues. The compound was never approved as a medicine. In public discussion, it is often grouped with performance-enhancing substances, although its receptor target differs from that of anabolic steroids or selective androgen receptor modulators. Regulatory and health authorities have issued warnings about its use.

GW501516 acts on PPARδ, a nuclear receptor that helps regulate fatty acid oxidation and energy homeostasis. In animal studies, activation of this receptor was associated with increased endurance and changes in lipid metabolism. Human trials examined effects on blood lipids and other metabolic markers, but the compound did not advance to approval. Rodent studies later reported tumors in multiple tissues at doses used in those experiments. Whether those findings translate to human risk remains uncertain, and the clinical relevance of the animal data is still debated.

Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.

Identity and Pharmacological Mechanism

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.

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.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineCommon internet and media name.
Research codeGW501516Also written GW-1516.
Drug classPPARδ agonistNot a selective androgen receptor modulator.
Development statusDiscontinuedClinical development halted after rodent cancer findings.
Regulatory statusProhibited in sportListed by WADA; not approved as medicine.

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.

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.

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Regulatory Status and Detection Context

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.

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.

Reference notes

=== Historical taxonomy === The taxonomy of Parmotrema perlatum has a rich history marked by periods of confusion and clarification that typify the dynamic nature of botanical classification. It was originally described as Lichen perlatus by William Hudson in his 1762 work Flora Anglica. Hudson described it as a foliaceous (leafy) lichen with creeping, lobed, and smooth characteristics, having a pearly edge, a farinaceous (pruinose) texture, and a black underside, adorned with slightly scalloped, brown, stalked fruiting bodies. The taxon was later transferred to the genus Parmelia by Erik Acharius in 1803, becoming Parmelia perlata. The name was well-established in scientific literature, being cited extensively in works like Alexander Zahlbruckner's popular 1929 catalogue. In 1952, Maurice Choisy reclassified it under the current name, Parmotrema perlatum. The nomenclature of Parmotrema perlatum was revisited in the late 20th century, amid a broader effort to clarify the typification and application of early lichen names. Mason Hale, in 1961, undertook a detailed restudy of the species, selecting a lectotype from the Dillenian collections—the herbarium and associated works of Johann Jacob Dillenius housed at the University of Oxford. This solidified the application of Hudson's name and was part of a larger trend in lichenology to fix historical names to specific herbarium specimens to stabilise nomenclature. The name Parmelia perlata was widely accepted until Hale and Ahti (1986) encountered the designation Lichen chinensis, introduced by Pehr Osbeck in 1757.

=== Children === Prolonged use of prednisolone eye drops in children may lead to raised intraocular pressure. While this phenomenon is dose-dependent, it is shown to have a greater effect, especially in children under 6 years of age.

== Taxonomy == The maqui was first scientifically described by Juan Ignacio Molina in 1782, who named it Cornus chilensis. In 1914, Stephen Conrad Stuntz assigned it to the genus Aristotelia that had been erected by Charles Louis L'Héritier de Brutelle in 1786, and made the new combination A. chilensis.

== Clinical significance == A study on molecular markers in human aortic endothelial cells published that urolithin A aglycone stopped cell migration but not monocyte adhesion, which is the initial step of atherosclerotic plaque formation. Another study exploring the benefits of extra virgin olive oil consumption in preventing age-related neurodegenerative diseases found oleuropein aglycone greatly increased the cognitive performance of mice. The aglycone-fed mice displayed strong autophagic reactions, mTOR regulation, and reduced plaque deposits and β-amyloid levels.

Sources: en.wikipedia.org

Reference notes

=== Conciliation Service === The United States Conciliation Service, which had provided mediation for labor disputes as part of Department of Labor, was removed from that department and reconstituted as an independent agency, the Federal Mediation and Conciliation Service (United States). This was done in part because industry forces thought the existing service had been too "partial" to labor.

The contamination in the Ganga-Brahmaputra fluvial plains in India and Padma-Meghna fluvial plains in Bangladesh demonstrated adverse impacts on human health. Clare Luce, American ambassador to Italy from 1953 to 1956, suffered from arsenic poisoning. Its source was traced to flaking arsenic-laden paint on the ceiling of her bedroom. She may also have eaten food contaminated by arsenic in flaking ceiling paint in the embassy dining room. Arsenic poisoning from exposure to groundwater is believed to be responsible for the illness experienced by those that witnessed the 2007 Carancas impact event in Peru, as local residents inhaled steam which was contaminated with arsenic, produced from groundwater which boiled from the intense heat and pressure produced by a chondrite meteorite impacting the ground. Ground water contaminated by arsenic, as of 2014, "is still poisoning millions of people in Asia".

James Windle notes that "prohibitions were enforced in Asian countries while the United States and Western Europe were routinely trading opium"; the "concept of prohibition being a distinctly American construct is, therefore, flawed". Collins concludes, "The United States was a key participant in the [International Drug Control System], albeit frequently an absent one, but hardly the sole force."

== Optical resolution in racemic amino acids == No theory explains the prevalence of L-amino acids. If one takes, for example, alanine, which has a small methyl group, and phenylalanine, which has a larger benzyl group, a simple question is in what aspect, L-alanine resembles L-phenylalanine more than D-phenylalanine, and what kind of mechanism causes the selection of all L-amino acids, because it might be possible that alanine was L and phenylalanine was D.

Cochlin is a protein that in humans is encoded by the COCH gene. It is an extracellular matrix (ECM) protein highly abundant in the cochlea and vestibule of the inner ear, constituting the major non-collagen component of the ECM of the inner ear. The protein is highly conserved in human, mouse, and chicken, showing 94% and 79% amino acid identity of human to mouse and chicken sequences, respectively.

Sources: en.wikipedia.org

Notes from published material

=== Others === It has also been used to prove that backpropagating action potentials invade dendritic spines without voltage attenuation, establishing a sound basis for future work on Long-term potentiation. Its use here was that it provided a way to accurately measure the voltage in the tiny dendritic spines with an accuracy unattainable with standard two-photon microscopy. Meanwhile, SHG can efficiently convert near-infrared light to visible light to enable imaging-guided photodynamic therapy, overcoming the penetration depth limitations.

== Diagnosis == In 1980, the American College of Rheumatology agreed on diagnostic criteria for scleroderma. Diagnosis is by clinical suspicion, presence of autoantibodies (specifically anticentromere and anti-Scl-70 antibodies), and occasionally by biopsy. Of the antibodies, 90% have a detectable antinuclear antibody. Anticentromere antibody is more common in the limited form (80–90%) than in the diffuse form (10%), and anti-Scl-70 is more common in the diffuse form (30–40%) and in African-American patients (who are more susceptible to the systemic form). Other conditions may mimic systemic sclerosis by causing hardening of the skin. Diagnostic hints that another disorder is responsible include the absence of Raynaud's phenomenon, a lack of abnormalities in the skin on the hands, a lack of internal organ involvement, and a normal antinuclear antibodies test result.

== Structure and mechanics == Fibrils are composed of linear biopolymers, and are characterized by rod-like structures with high length-to-diameter ratios. They often spontaneously arrange into helical structures. In biomechanics problems, fibrils can be characterized as classical beams with a roughly circular cross-sectional area on the nanometer scale. As such, simple beam bending equations can be applied to calculate flexural strength of fibrils under ultra-low loading conditions. Like most biopolymers, stress-strain relationships of fibrils tend to show a characteristic toe-heel region before a linear, elastic region. Unlike biopolymers, fibrils do not behave like homogeneous materials, as yield strength has been shown to vary with volume, indicating structural dependencies. Hydration has been shown to produce a noticeable effect in the mechanical properties of fibrillar materials. The presence of water (an aldehyde) has been shown to decrease the stiffness of collagen fibrils, as well as increase their rate of stress relaxation and strength. From a biological standpoint, water content acts as a toughening mechanism for fibril structures, allowing for higher energy absorption and greater straining capabilities. Fibrils mechanical strengthening properties originate at the molecular level. The forces distributed in the fiber are tensile load carried by the fibril and shear forces felt due to interaction with other fibril molecules. The fracture strength of individual collagen molecules is as a result controlled by covalent chemistry between molecules.

=== Voice acting === As an actor, French appeared on the 1996 NBC miniseries Pandora's Clock as a non-commissioned officer. He was best known for voice acting work in video games by Valve Corporation, most notably Father Grigori in Half-Life 2, Bill in Left 4 Dead and Left 4 Dead 2 and the Elder Titan in Dota 2. He additionally voiced the Scientist in Gunman Chronicles and the Fisherman in the tech demo Half-Life 2: Lost Coast.

Gliburnide is an endo-endo derivative made from camphor-3-carboxamide by borohydride reduction (exo approach), followed by Hofmann rearrangement to carbamate, followed by displacement with sodium tosylamide.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a selective androgen receptor modulator?

No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.

Why did clinical development stop?

Preclinical rodent studies reported cancers, including liver and bladder tumors, at tested doses. The human relevance of those findings is uncertain, but development was discontinued. No approved human product resulted.

Is cardarine approved for medical use?

No. It remains an investigational compound without approved therapeutic labeling. Sports regulators prohibit its use, and health agencies have warned against consuming it.

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.

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