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Identity And Regulatory Status — 2026 Update

By Editorial Desk · published 2025-07-29 · last reviewed 2025-09-02 · News

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

Reviewed 2025-09-02. Anything still debated is marked as such rather than presented as settled.

Identity and Regulatory Status

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.

Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.

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.

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.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516; GW-1516; endurobolGW501516 is the research code
Drug classPPARδ agonistNot a selective androgen receptor modulator
Molecular formulaC21H18F3NO3S2Established chemical formula
Molar mass453.5 g/molCalculated from the formula
Regulatory statusProhibited in sport; not approved as medicineStatus varies by country

Identity and Pharmacological Mechanism

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.

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.

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Cardarine as Investigational PPARδ Agonist

The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.

Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.

Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.

Detection, Regulation, and Quality Context

Cardarine can be detected in biological samples and product materials using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The method separates compounds by chromatography and identifies them by mass-to-charge transitions, allowing low-level detection in urine or blood. Sample preparation often involves enzymatic hydrolysis, solid-phase extraction, or protein precipitation. Certified reference materials and isotope-labeled internal standards improve quantification. Detection windows depend on metabolism, matrix, and assay sensitivity, so no single universal window applies.

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.

Supporting material

February 20: Decrees enacting the Conventions on the night work of women and of children in industry, drawn up in Washington by the International Labor Conference and signed in Paris on January 24, 1921, by France and Belgium, along with their annexed protocol. August 10: Nationality law. December 6: Decree on the regulations of the École nationale supérieure de céramique in Sèvres, reserved for boys. 1928

=== Skeletal muscle === Sarcopenia (loss of skeletal muscle mass associated with aging) Polymyositis (chronic inflammation) Dermatomyositis (chronic inflammation with skin rash) Inclusion body myositis (common age-related inflammatory disease)

ATSDR - Toxicity of Polycyclic Aromatic Hydrocarbons (PAHs) Archived 30 May 2020 at the Wayback Machine U.S. Department of Health and Human Services Fused Ring and Bridged Fused Ring Nomenclature Database of PAH structures Cagliari PAH Theoretical Database NASA Ames PAH IR Spectroscopic Database National Pollutant Inventory: Polycyclic Aromatic Hydrocarbon Fact Sheet Understanding Polycyclic Aromatic Hydrocarbons NASA Spitzer Space Telescope "The Aromatic World: An Interview with Professor Pascale Ehrenfreund" from Astrobiology Magazine Oregon State University Superfund Research Center focused on new technologies and emerging health risks of Polycyclic Aromatic Hydrocarbons (PAHs) Polycyclic Aromatic Hydrocarbons (PAHs)--EPA Fact Sheet. U.S. Environmental Protection Agency, Office of Solid Waste, January 2008.

On 7 April, Hikmat al-Hijri dissolved the Supreme Legal Committee in Suwayda, the judge Shadi Fayez Murshid was tasked with forming the Administrative Council of Jabal Bashan. On 11 April, people went to the streets at al-Karama Square to show their support for Hikmat al-Hijri. On 12 April 2026, clashes occurred between the Syrian Armed Forces and the National Guard along Maghdal–Mazraa. The next day, clashes took place between the Syrian Armed Forces and the National Guard along the Tel Hadid–industrial area. On 13 April, clashes between the Syrian Armed Forces and the National Guard took place along the Tel Hadid–industrial area. Also an assassination attempt was made against Anad Makarem, after he threatened the National Guard with a "popular uprising", Makarem was left in critical condition. On 15 April, the rival Druze leader Munir Najib al-Bahri was killed by unknown assailants. On 27 April, it was reported that the car of commander Basel al-Shaer was targeted. On 28 April, it was reported that the home of Rawad Abdul Khaleq, commander of the “Rapid Intervention” battalion in the National Guard, was attacked with gunfire and that the car of commander Farouk al-Naddaf was targeted with a Molotov cocktail.

Sources: en.wikipedia.org

Notes from published material

=== Name === Within the INN, USAN, BAN, and AAN naming systems this drug is known as butorphanol, while within JAN it is named torbugesic. As the tartrate salt, butorphanol is known as butorphanol tartrate (USAN, BAN).

=== SARS-CoV-2 === Rapamycin has been proposed as a treatment for severe acute respiratory syndrome coronavirus 2 insofar as its immunosuppressive effects could prevent or reduce the cytokine storm seen in very serious cases of COVID-19. Moreover, inhibition of cell proliferation by rapamycin could reduce viral replication.

=== Market === The global instant coffee market was valued at US$34.16 Billion in 2026. In 2025, Asia-Pacific accounted for 39% of the instant coffee market, Europe 28%, North America 24% and Middle East and Africa 9%. A 2014 article said that as a percentage of coffee sold, instant coffee accounted for 1% of the market in Italy, 4% in France, 7% in the US, and 77% in the UK. The high proportion in the UK was attributed to coffee, a novelty to a tea-drinking nation, being introduced in the form of instant coffee by US troops in Britain during World War II.

Sources: en.wikipedia.org

Further detail

=== International agencies === The European Food Safety Authority (EFSA) warned that children who ate large amounts of confectionery and biscuits with high milk content could theoretically be consuming melamine at more than three times above prescribed EU safety limits (0.5 mg/kg of body weight). The EFSA said children with a mean consumption of products such as milk toffee, biscuits and chocolate containing contaminated powdered milk would not be at risk, and adults would not be at risk even in the worst-case scenarios. The World Health Organization, which was only notified on 11 September, asked Beijing why it took so many months for the scandal to become public, and to establish whether failure was deliberate or due to ignorance. WHO's representative in China, Hans Troedsson, said the issue of who knew what and when was critical, because knowledge would be the distinction between ignorance and neglect. WHO and UNICEF jointly decried the "deliberate contamination of foods intended for ... vulnerable infants and young children." Following a spate of mass national bans, the WHO urged national food safety authorities on 25 September to test Chinese dairy products for health risks before placing import bans or recalls. On 26 September, the WHO warned health officials to look out for tainted dairy products imported from China. International Food Safety Authorities (INFOSAN), a network organized by WHO and the Food and Agriculture Organization, suggested that countries should focus on smuggled formula.

DNA sequencing is the process of determining the nucleic acid sequence – the order of nucleotides in DNA. It includes any method or technology that is used to determine the order of the four bases: adenine, thymine, cytosine, and guanine. The advent of rapid DNA sequencing methods has greatly accelerated biological and medical research and discovery.

== Synthesis and reactions == Industrially, L-serine is produced from glycine and methanol catalyzed by hydroxymethyltransferase. Racemic serine can be prepared in the laboratory from methyl acrylate in several steps:

The renovated park featured a great lawn, as well as hedges and later an iron fence that separated the park from the surrounding city streets. Two entrances each were added from 40th and 42nd Streets. As part of the project, 270 trees were placed around the park. Moses also placed the park's statues along 40th and 42nd Streets so as to block sight lines from these streets. To save money, the project hired workers from the Civil Works Administration, an unemployment relief program. The renovation was complete by late 1934, and after a short postponement, the park reopened that September 15. Parts of the park were closed in the late 1930s due to transit changes on Sixth Avenue; the elevated was torn down in 1938, and the construction of the underground Sixth Avenue subway line occurred around the same time. The Sixth Avenue subway opened in 1940. A New Yorker article remarked in 1936 that during the prior 14 years, "Bryant Park has been closed to the public [...] for half that time."

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a SARM?

No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.

Is cardarine approved for human use?

No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.

Why was its development discontinued?

Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.

How does cardarine work in the body?

It binds to and activates PPAR delta, a nuclear receptor that controls expression of genes related to fatty acid oxidation. This mechanism can alter energy metabolism in animal models. It is not a direct stimulant or fat-burning enzyme.

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