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Background And Regulatory Status — Background and Details

By Editorial Desk · published 2026-04-07 · last reviewed 2026-04-23 · Data

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

Last reviewed on 2026-04-23. Where a claim depends on a specific study, the study is described rather than over-claimed.

Background and Regulatory Status

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.

Identity and Pharmacological Classification

Cardarine is a common name for GW501516, also GW-1516, a synthetic compound developed as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. It belongs to a class of agents that modulate gene transcription related to lipid and energy metabolism. The compound was studied in preclinical and early clinical research for metabolic and cardiovascular conditions, but it did not progress to approved therapeutic use. Its name appears in fitness and sports contexts despite not being approved as a drug.

PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.

Published studies have examined GW501516 in animal models of obesity, insulin resistance, and exercise endurance. Early human trials reportedly ended, and development was discontinued after preclinical findings raised concerns about cancer in some rodent studies. Regulatory agencies have not approved cardarine for any medical use. Its availability through non-pharmaceutical channels raises questions about identity, purity, and legal status that are separate from its laboratory pharmacology. Those questions are often addressed through analytical testing rather than assumptions about product labels.

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

Mechanism and Detection 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.

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.

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Regulation and Analytical Detection

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.

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.

Mechanism and Laboratory Detection

GW501516 binds and activates PPARδ, a nuclear receptor that influences transcription of genes involved in fatty acid oxidation and energy use. Activation shifts some metabolic pathways in preclinical models, which is why the compound has been studied for lipid disorders and exercise-related endpoints. The exact downstream effects in humans are incompletely mapped. PPARδ is expressed in many tissues, including skeletal muscle, liver, and adipose tissue, so broad activation may have varied consequences. Researchers continue to examine how selective or partial activation might alter the balance between benefits and risks.

Published human data are sparse and mostly come from early-phase trials. Those studies examined short-term changes in lipids, glucose, and exercise capacity, but they were not large enough to establish efficacy or long-term safety. Some animal experiments reported increased running endurance, yet such findings do not prove a performance benefit in people. Anti-doping laboratories detect GW501516 and its metabolites in urine or blood using liquid chromatography-tandem mass spectrometry. Detection windows depend on dose, sample type, and individual metabolism. The method is sensitive enough to identify trace residues in tested samples.

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.

Background from the literature

Autoimmune diseases represent a vast and diverse category of disorders that, despite their differences, share some common symptomatic threads. These shared symptoms occur as a result of the body's immune system mistakenly attacking its own cells and tissues, causing inflammation and damage. However, due to the broad range of autoimmune diseases, the specific presentation of symptoms can significantly vary based on the type of disease, the organ systems affected, and individual factors such as age, sex, hormonal status, and environmental influences. An individual may simultaneously have more than one autoimmune disease (known as polyautoimmunity), further complicating the symptomatology.

The first use of radioluminescence was in luminous paint containing radium, a natural radioisotope. Beginning in 1908, luminous paint containing a mixture of radium and copper-doped zinc sulfide was used to paint watch faces and instrument dials, giving a greenish glow. Phosphors containing copper-doped zinc sulfide (ZnS:Cu) yield blue-green light; copper and manganese-doped zinc sulfide (ZnS:Cu,Mn), yielding yellow-orange light are also used. Radium-based luminescent paint is no longer used due to the radiation hazard posed to persons manufacturing the dials. These phosphors are not suitable for use in layers thicker than 25 mg/cm2, as the self-absorption of the light then becomes a problem. Zinc sulfide undergoes degradation of its crystal lattice structure, leading to gradual loss of brightness significantly faster than the depletion of radium. ZnS:Ag coated spinthariscope screens were used by Ernest Rutherford in his experiments discovering the atomic nucleus. Radium was used in luminous paint until the 1960s, when it was replaced with the other radioisotopes mentioned above due to health concerns. In addition to alpha and beta particles, radium emits penetrating gamma rays, which can pass through the metal and glass of a watch dial, and skin. A typical older radium wristwatch dial has a radioactivity of 3–10 kBq and could expose its wearer to an annual dose of 24 millisieverts if worn continuously. Another health hazard is its decay product, the radioactive gas radon, which constitutes a significant risk even at extremely low concentrations when inhaled.

=== Keith Jackson === A 1989 Washington Post investigative story accused the administration of setting up an 18-year-old black man from Baltimore in a sting operation to showcase the drug problem close to home. The DEA, using an undercover agent, pushed a black 18-year-old high school student, Keith Jackson, to make a sale of crack outside the White House. (Jackson had already sold cocaine to agents on four other occasions.) In a recorded conversation with the agents, Jackson can be heard saying "Where the [Expletive] is the White House?" The agents set up a buy with Jackson in Lafayette Park, just across the street from the White House. Jackson was arrested and convicted of felony possession of crack cocaine with intent to distribute. He had no prior convictions but was sentenced to 10 years in prison based on the mandatory minimum laws of 1988. After his conviction, Jackson was visibly in tears. U.S. District Judge Stanley Sporkin told Jackson at his sentencing, "Bush used you, in the sense of making a big drug speech. But he's a decent man, a man of great compassion. Maybe he can find a way to reduce at least some of that sentence." Bush, when asked about the story, told the Washington Post, "The man went there and sold drugs in front of the White House, didn't he?... I can't feel sorry for this fellow."

Sources: en.wikipedia.org

Further detail

Moscow has a humid continental climate (Köppen climate classification: Dfb) with long, cold winters usually lasting from mid-November to the end of March, along with warm summers. More extreme continental climates at the same latitude—such as parts of Eastern Canada or Siberia—have much colder winters than Moscow does, suggesting that Moscow receives significant moderation from the Atlantic Ocean, even though the city is distant from it. Weather in Moscow can fluctuate widely: in the winter, temperatures range from −25 °C (−13 °F) in the city and −30 °C (−22 °F) in the suburbs to above 5 °C (41 °F); in the summer, temperatures range from 10 to 35 °C (50 to 95 °F).

As with the chemical antioxidants, cells are protected against oxidative stress by an interacting network of antioxidant enzymes. Here, the superoxide released by processes such as oxidative phosphorylation is first converted to hydrogen peroxide and then further reduced to give water. This detoxification pathway is the result of multiple enzymes, with superoxide dismutases catalysing the first step and then catalases and various peroxidases removing hydrogen peroxide. As with antioxidant metabolites, the contributions of these enzymes to antioxidant defenses can be hard to separate from one another, but the generation of transgenic mice lacking just one antioxidant enzyme can be informative.

Inhibition of the activity of tyrosinase: The catalytic action of tyrosinase is inhibited by the skin whitening agent. Inhibition of the expression or activation of tyrosinase: The anti melanogenic agent causes less tyrosinase to be generated or prevents tyrosinase from being activated to its functional form. Scavenging of the intermediate products of melanin synthesis. Preventing the transfer of melanosomes to keratinocytes. Directly destroying existing melanin. Destroying melanocytes.

Sources: en.wikipedia.org

Supporting material

In January 2017, Dutch Bros purchased a vacant shopping center in downtown Grants Pass, where their original push cart was located. The company converted 20,000 square feet of the shopping center's interior into futsal courts for local youth soccer teams and workout space for its employees. In March of that same year, the company bought the Washington Federal bank building across the street from the shopping center, to move its headquarters and 150 employees into the bank building the following fall.

One new technology that is being introduced starting with the Japanese Navy's eleventh Sōryū-class submarine (JS Ōryū) is a more modern battery, the lithium-ion battery. These batteries have about double the electric storage of traditional batteries, and by changing out the lead-acid batteries in their normal storage areas plus filling up the large hull space normally devoted to AIP engine and fuel tanks with many tons of lithium-ion batteries, modern submarines can actually return to a "pure" diesel–electric configuration yet have the added underwater range and power normally associated with AIP equipped submarines.

Cervical drug delivery serves as a route for compounds to prevent and treat sexually transmitted diseases (STDs). Prevention of STDs for women can be achieved by administering preventative compounds into the vaginal canal prior to intercourse. One method researched is the use of a CAP technology that remains stable in the vaginal environment, but breaks down in the presence of human semen, releasing a drug to destroy STDs. This application of cervical drug delivery would be useful for prevention of STDs in women without interfering with the bodily environment until there is potential for infection. STDs can also be treated through cervical drug delivery methods. Antibiotics for STD treatment are often administered into the vagina in the form of creams or gels.

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 cardarine also known as?

Cardarine is commonly known as GW501516 or GW-1516. These names refer to the same synthetic compound. It is not a brand-name approved medicine.

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