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Background And Regulatory Status — Evidence Review

By Editorial Desk · published 2025-08-11 · last reviewed 2025-08-26 · Wiki

This is a working overview of research chemical, written for readers who want more than a one-paragraph summary but less than a textbook.

Reviewed 2025-08-26. Anything still debated is marked as such rather than presented as settled.

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.

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.

Reference notes

van Krevelen, D.W. (1950). "Graphical-statistical method for the study of structure and reaction processes of coal", Fuel, 29, 269–84. van Krevelen, D.W. and Schuyer, J. (1957) Coal science. Elsevier publishing company. The chemistry and technology of petroleum

=== Pharmacokinetics === RO5203648 showed favorable pharmacokinetics orally and intravenously in mice, rats, and monkeys. However, it was found to be very rapidly metabolized in human hepatocytes in vitro.

Ciramadol (WY-15,705) is an opioid analgesic that was developed in the late 1970s and is related to phencyclidine, tramadol, tapentadol and venlafaxine. It is a mixed agonist-antagonist for the μ-opioid receptor with relatively low abuse potential and a ceiling on respiratory depression which makes it a relatively safe drug. It has a slightly higher potency and effectiveness as an analgesic than codeine, but is weaker than morphine. Other side effects include sedation and nausea but these are generally less severe than with other similar drugs.

Carcinoma: Cancers derived from epithelial cells. This group includes many of the most common cancers that occur in older adults. Nearly all cancers developing in the breast, prostate, lung, pancreas, and colon are carcinomas. Sarcoma: Cancers arising from connective tissue (i.e. bone, cartilage, fat, nerve), each of which develop from cells originating in mesenchymal cells outside of the bone marrow. Lymphoma and leukemia: These two classes of cancer arise from immature cells that originate in the bone marrow, and are intended to fully differentiate and mature into normal components of the immune system and the blood, respectively. Acute lymphoblastic leukemia is the most common type of cancer in children, accounting for ~30% of cases. However, far more adults than children develop lymphoma and leukemia. Germ cell tumor: Cancers derived from pluripotent cells, most often presenting in the testicle or the ovary (seminoma and dysgerminoma, respectively). Blastoma: Cancers derived from immature "precursor" cells or embryonic tissue. Blastomas are generally more common in children (e.g. neuroblastoma, retinoblastoma, nephroblastoma, hepatoblastoma, medulloblastoma, etc.) than in older adults.

Sources: en.wikipedia.org

Reference notes

In prokaryotic cells, such as bacteria, which lack mitochondria, the citric acid cycle reaction sequence is performed in the cytosol with the proton gradient for ATP production being across the cell's surface (plasma membrane) rather than the inner membrane of the mitochondrion. For each pyruvate molecule (from glycolysis), the overall yield of energy-containing compounds from the citric acid cycle is three NADH, one FADH2, and one GTP or ATP.

The 1st Infantry Division's Task Force 2–16 Infantry cleared four lanes simultaneously through an enemy fortified trench system while inflicting heavy casualties on Iraqi forces. Task Force 2–16 continued the attack clearing over 21 km (13 mi) of entrenched enemy positions resulting in the capture and destruction of numerous enemy vehicles, equipment, personnel and command bunkers.

== Distribution and migration == The cabbage looper can be found across North America and Eurasia, as far south as Florida and as far north as British Columbia. Cabbage looper populations in North America migrate from Mexico to Canada, depending on the seasons. It generally overwinters in Mexico or southern California, where temperatures are above 16 °C (61 °F) even during winter. It used to be frequently found in Florida, but this has lessened due to fewer cabbage crops. As northern regions of North America grow warmer, the cabbage looper gradually moves upward, only migrating if the region is above 16 °C (61 °F). During summer, it is less commonly found in southern regions, due to high temperatures. Similar to the monarch butterfly, populations presumably migrate in groups, as there is little genetic difference between source and migrating populations. Similar seasonal distributions were found in Europe. There, the cabbage looper can be found from England to southeastern Europe.

== Human use == Different parts of the plant are used as traditional remedies for disease and skin afflictions. Juice from the leaves is used to treat warts and snakebite, and the flower is applied to burns. This species has been used as indigenous traditional medicine in Asia for rheumatism, fractures, and other ailments. In Korean folk medicine, this impatiens species is used as a medicine called bongseonhwa dae (봉선화대) for the treatment of constipation and gastritis. Chinese people used the plant to treat those bitten by snakes or who ingested poisonous fish. Juice from the stalk, pulverised dried stalks, and pastes from the flowers were also used to treat a variety of ailments. Vietnamese wash their hair with an extract of the plant to stimulate hair growth. One in vitro study found extracts of this impatiens species, especially of the seed pod, to be active against antibiotic-resistant strains of Helicobacter pylori. It is also an inhibitor of 5α-reductases, enzymes that converts testosterone to dihydrotestosterone (active form of testosterone), thus reducing action of testosterone in our body. In Nepal, the balsam leaves are crushed to dye fingernails on the day of Shrawan Sakranti (Shrawan 1). The day is also observed as Luto Faalne Deen (Go Away-Itch Day). Similarly, in China and Korea, the flowers are crushed and mixed with alum to produce an orange dye that can be used to dye fingernails. Unlike common nail varnish, the dye is semi-permanent, requiring dyed nails to grow off over time in order to remove any traces of color.

Narrated by Bill Paterson, directed by Paul Sen, produced by Rosalind Arden, made by McDougall Craig 22 September Non-lethal Weapon, about non-lethal weapons; Steven Metz of the US Army War College; Ride of the Valkyries with sticky foam guns; a net gun made by Foster-Miller; sonic weapons; Jonathan Rosenhead of the LSE; seventeen people had been killed by plastic bullets in Northern Ireland; Lenore Anderson; in the Gulf War air campaign of 1991, Tomahawk missiles discharged BLU-114/B wire over Iraq electrical substations, and crippled 85% of the country's electrical network, so effectively switching off the country's air defence radar; Julian Perry Robinson of the Science Policy Research Unit at the University of Sussex. Produced by David Frank, directed by Martin Durkin, made by RDF Television with Discovery Communications

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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