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Background And Regulatory Status — Reference Sheet

By Editorial Desk · published 2026-06-10 · last reviewed 2026-06-24 · News

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

Last reviewed on 2026-06-24. Where a claim depends on a specific study, the study is described rather than over-claimed.

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.

Detection, Regulation, and Quality Context

Regulatory treatment of cardarine differs by context and jurisdiction. In competitive sport, the World Anti-Doping Agency lists PPARδ agonists, including GW501516, as prohibited at all times. Outside sport, it lacks approval as a prescription medicine in major drug markets, and products sold for human consumption may be treated as unapproved drugs. Some countries also restrict importation or sale through general consumer protection and medicines laws. These classifications affect availability, testing, and legal risk without establishing therapeutic value.

Because cardarine is not an approved medicine, no pharmacopeial monograph defines its identity, purity, or storage requirements. Laboratories typically rely on in-house methods and reference standards when testing materials labeled as GW501516. Certificates of analysis may report purity and identity for a specific batch, but their scope varies and they do not guarantee safety or legal status. Independent verification can include high-performance liquid chromatography, mass spectrometry, nuclear magnetic resonance, and elemental analysis. The distinction between research chemical labeling and human use is significant because quality standards and oversight differ.

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 Analytical Detection

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 is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.

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Mechanism and Safety Research

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.

Background and Research Context

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.

Regulatory Status and Detection Context

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.

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.

Supporting material

=== Pharmacodynamics === Isoergine shows affinity for serotonin receptors labeled with serotonin or LSD in rat brain membranes. It has about 10- to 25-fold lower affinity for these receptors than serotonin or LSD and has the same affinity as ergine and iso-LSD (IC50Tooltip half-maximal inhibitory concentration = 100–200 nM for isoergine, 200 nM for ergine and iso-LSD, and 8–10 nM for LSD). No other receptor interaction data are available for isoergine as of 2020. However, computer-predicted receptor affinities are available for ergine/isoergine (stereochemistry not taken into account). The drug is said to have about 4.3% of LSD's antiserotonergic potency in vitro. It is 5- to 33-fold less potent than LSD in producing behavioral changes in the conditioned avoidance test in rodents.

In particular, Maricopa County has been targeted by conspiracy theorists for alleged irregularities in how the county voted in the 2020 presidential election; the county's ballots were audited by Republicans in 2021, finding no such claims of voter fraud. Ahead of the 2023 Philadelphia mayoral election and the Pennsylvania primary election, the account for the Philadelphia City Commissioners was unverified, leading to several verified accounts impersonating the commissioners. On May 22, an account aligned with the QAnon conspiracy theory posted an image generated by artificial intelligence that seemingly depicted an explosion near the Pentagon. The fake image was amplified by the Russian propaganda television network RT and the far-right blog Zero Hedge. A verified account posing as Bloomberg News then posted the claim accompanied by several other verified accounts. The S&P 500 fell sharply as a result of the news before rebounding. Several Indian news outlets, including Zee News and Republic TV, aired false reports about the supposed explosion.

Layne Staley – lead and backing vocals, rhythm guitar on "Hate to Feel" and "Angry Chair"; sun logo/icons Jerry Cantrell – guitars, backing vocals, co-lead vocals on "Down in a Hole" and "Would?" Mike Starr – bass Sean Kinney – drums Additional personnel

=== GLUT 1 === Every carrier protein, especially within the same cell membrane, is specific to one type or family of molecules. GLUT1 is a named carrier protein found in almost all animal cell membranes that transports glucose across the bilayer. This protein is a uniporter, meaning it transports glucose along its concentration in a singular direction. It is an integral membrane protein carrier with a hydrophilic interior, which allows it to bind to glucose. As GLUT 1 is a type of carrier protein, it will undergo a conformational change to allow glucose to enter the other side of the plasma membrane. GLUT 1 is commonly found in the red blood cell membranes of mammals.

Sources: en.wikipedia.org

Notes from published material

7 CH2=CH2 + 6 O2 → 6 (CH2CH2)O + 2 CO2 + 2 H2O and the maximum degree of conversion of ethylene to ethylene oxide is theoretically predicted to be 6/7 or 85.7%, although higher yields are achieved in practice. The catalyst for the reaction is metallic silver deposited on various matrixes, including pumice, silica gel, various silicates and aluminosilicates, alumina, and silicon carbide, and activated by certain additives (antimony, bismuth, barium peroxide, etc.). The process temperature was optimized as 220–280 °C (430–540 °F). Lower temperatures reduce the activity of the catalyst, and higher temperatures promote the complete oxidation of ethylene thereby reducing the yield of ethylene oxide. Elevated pressure of 1–3 MPa (150–440 psi) increases the productivity of the catalyst and facilitates absorption of ethylene oxide from the reacting gases. Whereas oxidation by air is still being used, oxygen (> 95% purity) is preferred for several reasons, such as higher molar yield of ethylene oxide (75–82% for oxygen vs. 63–75% for air), higher reaction rate (no gas dilution) and no need of separating nitrogen in the reaction products.

Secondary amino acids, amino acids containing a secondary amine group are sometimes named imino acids, though this usage is obsolescent. The only proteinogenic amino acid of this type is proline, although the related non-proteinogenic amino acids hydroxyproline and pipecolic acid have often been included in studies of this class of compounds. The term imino acid is also the obsolete term for imidic acids, structures containing the -C(=NH)-OH group, and should not be used for them.

== Diagnostic == Dozens of congenital metabolic diseases are now detectable by newborn screening tests, especially expanded testing using mass spectrometry. Gas chromatography–mass spectrometry-based technology with an integrated analytics system has now made it possible to test a newborn for over 100 mm genetic metabolic disorders. Because of the multiplicity of conditions, many different diagnostic tests are used for screening. An abnormal result is often followed by a subsequent "definitive test" to confirm the suspected diagnosis.

==== Outdoor areas with elevated concentrations ==== Local concentrations of carbon dioxide can reach high values near strong sources, especially those that are isolated by surrounding terrain. At the Bossoleto hot spring near Rapolano Terme in Tuscany, Italy, situated in a bowl-shaped depression about 100 m (330 ft) in diameter, concentrations of CO2 rise to above 75% overnight, sufficient to kill insects and small animals. After sunrise the gas is dispersed by convection. High concentrations of CO2 produced by disturbance of deep lake water saturated with CO2 are thought to have caused 37 fatalities at Lake Monoun, Cameroon in 1984 and 1700 casualties at Lake Nyos, Cameroon in 1986.

HGF/c-MET has also been implicated in β-cell regeneration, which suggests that HGF/c-MET may help increase β-cell mass to compensate for insulin needs during pregnancy. Recent studies support that loss of HGF/c-MET signaling results in aberrant β-cell adaptation. c-MET is a receptor tyrosine kinase (RTK) that is activated by its ligand, hepatocyte growth factor (HGF), and is involved in the activation of several cellular processes. When HGF binds c-MET, the receptor homodimerizes and self-phosphorylates to form an SH2 recognition domain. The downstream pathways activated include common signaling molecules such as RAS and MAPK, which affect cell motility and cell cycle progression. Studies have shown that HGF is an important signaling molecule in stress-related situations where more insulin is needed. Pregnancy causes increased insulin resistance and a higher insulin demand. The β-cells must compensate for this by either increasing insulin production or proliferating. If neither of the processes occurs, then markers for gestational diabetes are observed. It has been observed that pregnancy increases HGF levels, showing a correlation that suggests a connection between the signaling pathway and increased insulin needs. When no signaling is present, gestational diabetes is more likely to occur. The exact mechanism of HGF/c-MET regulated β-cell adaptation is not yet known. Several hypotheses about how the signaling molecules contribute to insulin levels during pregnancy have been proposed.

Sources: en.wikipedia.org

Background from the literature

Many industries other than the health industry have used antimicrobial surfaces to keep surfaces clean. The physical nature of the surface or its chemical makeup can be manipulated to create an inhospitable environment for micro-organisms. Photocatalytic materials have been used for their ability to kill many micro-organisms and therefore can be used for self-cleaning surfaces as well as air cleaning, water purification, and antitumor activity.

At that point, the ice is able to safely support the heavier equipment required for that phase, which mostly consists of artificial thickening using a pump or a spraying system. The aim is to bring the thickness up to what is required for the heaviest vehicles that are anticipated when the ice road opens.

== Background == Found in several fungal species such as Fusarium graminearum NRRL 2903 (formerly misidentified as Dactylium dendroides), and other species of Fusarium and Aspergillus genera, galactose oxidase was first isolated in 1959. This enzyme is secreted by fungi to function in extracellular space. Although the oxidation reaction of D-galactose gives galactose oxidase its name, the coupled reduction of dioxygen to hydrogen peroxide is believed to have greater physiological significance in yeasts. Hydrogen peroxide which can be produced by yeasts in this way is possibly a bacteriostatic agent.

A nanoparticle or ultrafine particle is a particle of matter 1 to 100 nanometres (nm) in diameter. The term is sometimes used for larger particles, up to 500 nm, or fibers and tubes that are less than 100 nm in only two directions. At the lowest range, metal particles smaller than 1 nm are usually called atom clusters instead. Nanoparticles are distinguished from microparticles (1–1000 μm), "fine particles" (sized between 100 and 2500 nm), and "coarse particles" (ranging from 2500 to 10,000 nm), because their smaller size drives very different physical or chemical properties, like colloidal properties and ultrafast optical effects or electric properties. Being more subject to the Brownian motion, they usually do not sediment, like colloidal particles that conversely are usually understood to range from 1 to 1000 nm. Being much smaller than the wavelengths of visible light (400–700 nm), nanoparticles cannot be seen with ordinary optical microscopes, requiring the use of electron microscopes or microscopes with laser. For the same reason, dispersions of nanoparticles in transparent media can be transparent, whereas suspensions of larger particles usually scatter some or all visible light incident on them. Nanoparticles also easily pass through common filters, such as common ceramic candles, so that separation from liquids requires special nanofiltration techniques.

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.

How is cardarine detected in anti-doping tests?

Anti-doping laboratories typically use LC-MS/MS to detect GW501516 and its metabolites in urine. The method is sensitive and can identify the compound at low concentrations. Detection depends on sample timing, metabolism, and the specific assay.

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