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Background And Regulatory Status — Quick Reference

By Editorial Desk · published 2026-05-06 · last reviewed 2026-05-20 · Guide

If you have been reading about research chemical and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.

Updated 2026-05-20. Numbers and descriptions here follow the published literature rather than marketing material.

Background and Regulatory Status

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.

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.

Mechanism and Laboratory Detection

Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.

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.

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

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.

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Mechanism and Detection Methods

Handling and quality assessment of cardarine reference material follow general laboratory practices for poorly characterized compounds. It typically appears as a white to off-white powder and is sparingly soluble in water but soluble in organic solvents such as dimethyl sulfoxide and ethanol. Storage recommendations usually specify a cool, dry, dark place, with long-term storage at low temperature and desiccation. Purity may be checked by high-performance liquid chromatography with ultraviolet detection, while identity is confirmed by mass spectrometry and nuclear magnetic resonance. No pharmacopeial monograph exists, so reported purity and stability depend on the supplier’s 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.

Background and Research Context

In laboratory settings, cardarine is studied as a tool compound for probing PPARδ biology. Published experiments often use cell cultures, rodent models, or isolated tissues. Some investigations focus on metabolic effects, while others assess potential risks such as carcinogenicity observed in long-term animal studies. Because human trials are sparse, most knowledge comes from preclinical work and adverse event reports. Scientific literature frequently notes the gap between animal findings and human outcomes. The compound is not a dietary supplement and is not intended for human consumption.

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.

Background from the literature

=== Relationship === Rose's parents forbade their daughter from continuing to date Fred, but she defied their wishes, prompting them to visit Gloucestershire's social services agency to explain that their 15-year-old daughter was having a sexual relationship with an older man, and that they had heard rumours that she had begun to engage in prostitution at Fred's caravan. In response, Rose was placed in a home for troubled teenagers in Cheltenham in August 1969, and only permitted to leave under controlled conditions. When allowed to return home to visit her parents at weekends, Rose almost invariably took the opportunity to visit Fred. On her 16th birthday, Rose left the home for troubled teenagers to return to her parents while Fred was serving a thirty-day sentence for theft and unpaid fines. Upon his release, Rose left her parents' home to move into a flat in Cheltenham with Fred. Shortly thereafter, Fred collected Charmaine and Anne Marie from social services. Rose's father made one final effort to prevent his daughter from seeing Fred, and Rose was examined by a police surgeon in February 1970, who confirmed she was pregnant. In response, Rose was again placed into care but was discharged on 6 March on the understanding she would terminate her pregnancy and return to her family. Instead, Rose opted to live with Fred, resulting in her father forbidding his daughter from ever again setting foot in his household. Three months later Fred and Rose vacated the Cheltenham flat and moved to the ground-floor flat of a two-storey house at 25 Midland Road in Gloucester.

Although the office of the attorney general did not begin such an investigation, El Faro was subject to tax audits that Human Rights Watch's José Miguel Vivanco described as "selective and abusive". The audits were suspended in March 2021 after a Supreme Court order citing concerns about a risk to freedom of expression. In 2022, Amnesty International stated that at least 22 Salvadoran journalists (most of whom worked for El Faro) had their phones tapped by the Salvadoran government using the Israeli Pegasus spyware. El Faro moved its headquarters to San José, Costa Rica in April 2023, saying that it was trying to avoid "fabricated accusations" from Bukele's government. In 2025, Bukele claimed that most independent journalists and media outlets were part of a supposed "global money laundering operation" ("operación mundial de lavado de dinero"), referring to the United States Agency for International Development (USAID).

Former CIA official David Rush is accused of stealing $40 million of gold bars. CBS News editor-in-chief Bari Weiss appoints former New York Times journalist Nick Bilton as the executive director of 60 Minutes, following a series of firings on 60 Minutes staff amid pressure from the Trump administration. The White House launches aliens.gov, an extraterrestrial-themed website that lambasts illegal immigration in the U.S. May 29 Federal judge Leonie Brinkema blocks the distribution of the Trump administration's $1.8 billion anti-weaponization fund while lawsuits are being litigated. Federal judge Christopher R. Cooper orders the Trump administration to reopen the Kennedy Center and remove Trump's name from it, ruling that congressional approval is required. In ice hockey, the Carolina Hurricanes beat the Montreal Canadiens in five games during the Eastern Conference Finals to advance to the 2026 Stanley Cup finals, making it their first appearance in the Stanley Cup since 2006. May 30 The San Antonio Spurs defeat the defending champions, the Oklahoma City Thunder, in seven games to win the Western Conference finals and reach the NBA Finals for the first time since 2014, where they will face the New York Knicks. The U.S. Southern Command announces that it conducted a strike on a vessel in the eastern Pacific, killing three male "narco-terrorists".

Adenomatous polyposis coli protein 2 is a protein that in humans is encoded by the APC2 gene. This is a dual-functional protein which is especially prevalant in the developing brain, and involved in cell signaling (specifically Wnt signaling) and stabilizing the cytoskeleton. Frizzled receptors are a type of cell receptor involved in a variety of functions including embryonic development and cell proliferation. These receptors trigger a cascade of reactions called the Wnt signaling pathway that eventually leads to interaction with the DNA via the protein beta-catenin, which affects which proteins get produced by the cell. The APC2 protein promotes the formation of a protein complex which is involved in breaking down the protein beta-catenin. The APC2 protein stabilizes microtubules, which are part of the cell cytoskeleton. It may also be involved in the regulation of actin fibers my means of GTPase activation (specifically the Rho family).

Selective microfluidics-based ligand enrichment followed by sequencing (SMiLE-seq) is a technique developed for the rapid identification of DNA binding specificities and affinities of full length monomeric and dimeric transcription factors in a fast and semi-high-throughput fashion. SMiLE-seq works by loading in vitro transcribed and translated “bait” transcription factors into a microfluidic device in combination with DNA molecules. Bound transcription factor-DNA complexes are then isolated from the device, which is followed by sequencing and then sequence data analysis to characterize binding motifs. Specialized software is used to determine the DNA binding properties of monomeric or dimeric transcription factors to help predict their in vivo DNA binding activity. SMiLE-seq combines three important functions differing from existing techniques: (1) The use of capillary pumps to optimize the loading of samples, (2) Trapping molecular interactions on the surface of the microfluidic device through immunocapture of target transcription factors, (3) Enabling the selection of DNA that is specifically bound to transcription factors from a pool of random DNA sequences.

Sources: en.wikipedia.org

Reference notes

=== Marketing authorization === In 2011, the European Medicines Agency (EMA) granted a marketing authorisation for a buccal application form of midazolam, sold under the brand name Buccolam. Buccolam was initially approved for the treatment of prolonged, acute, convulsive seizures in people from three months to less than 18 years of age. This is the first application of a paediatric-use marketing authorisation by the EMA.

=== 2026 Iran war === Following the assassination of Ali Khamenei during the 2026 Iran war, Badr Organization leader Hadi al-Amiri pledged allegiance to the new supreme leader of Iran, Mojtaba Khamenei.

In more recent years, the party has attempted to win votes from Black South Africans and as a result, Black support for the DA has risen over the past several years, going from 1% to 6%. The DA is a liberal party that favours free-market policies. The DA was allotted 89 seats in parliament after the 2014 general election, but the party's seat total decreased to 84 seats following the 2019 general election. The DA has been part of the government of South Africa since the 2024 general election, having joined the Government of National Unity (GNU), and President Cyril Ramaphosa's Third Cabinet. The DA stated that one of its main aims for joining the GNU was keeping rival parties EFF and MK out of the government; a goal which was achieved as per the eventual composition of the GNU. As of May 2025, the party holds 6 ministry seats, and 6 deputy ministry seats in parliament. Economic Freedom Fighters The EFF emerged eight months before the 2014 general election and won 25 seats in parliament. After the 2019 general elections, the EFF increased their seats in parliament to 44, the only party of the top three parties that achieved an increase of members in parliament. The EFF is a far-left revolutionary socialist political party, advocating for land expropriation and for an end to corruption within parliament. Inkatha Freedom Party The IFP, which was formed in 1990 was the successor to the former government in the now-defunct Kwazulu Bantustan, traditionally draws its support from the Zulu people. It has however made inroads into the minority electorate of Whites and Indians.

== Contraindications == Artesunate is typically a well tolerated medicine. Known contraindications include a previous severe allergic reaction to artesunate. Drugs that should be avoided while on artesunate are the drugs that inhibit the liver enzyme CYP2A6. These drugs include amiodarone, desipramine, isoniazid, ketoconazole, letrozole, methoxsalen and tranylcypromine.

Sources: en.wikipedia.org

Reference notes

== Synthesis and transport == GIP is derived from a 153-amino acid proprotein encoded by the GIP gene and circulates as a biologically active 42-amino acid peptide. It is synthesized by K cells, which are found in the mucosa of the duodenum and the jejunum of the gastrointestinal tract. Like all endocrine hormones, it is transported by the blood. Gastric inhibitory polypeptide receptors are seven-transmembrane protein (GPCRs) found in beta cells in the pancreas.

=== Central & East Indo-Pacific === 2024 Vietnamese export of pangasius maw has increased to about US$58,000,000, with 38% going to China and the rest to Thailand, Malaysia, Singapore and the USA. The Vietnam News Agency claims that the falling totoaba population has incentivized Chinese import of alternative maw. The island and seas of New Guinea see significant fish maw production. Since 2012, in and around the Kikori River delta of Papua New Guinea, the scaly croaker Nibea squamosa has been targeted in gillnetting for its extremely high-priced maw, selling for as much as US$15,615 per kilogram.

Benzodiazepines have robust efficacy in the short-term management of generalized anxiety disorder (GAD) when standardized measures of anxiety are used as the outcome variable, but did not demonstrate a favorable dropout rate compared to placebo in one meta-analysis. A newer meta-analysis showed that benzodiazepines are significantly more effective than serotonergic agents, regardless of treatment length. More research is needed, but unfortunately, newer randomized controlled trials are scarce for the off patent benzodiazepines. According to National Institute for Health and Clinical Excellence (NICE), benzodiazepines can be used in the immediate management of GAD, if necessary. However, they should not usually be given for longer than 2–4 weeks. The only medications NICE recommends for the longer-term management of GAD are antidepressants. Likewise, the Canadian Psychiatric Association (CPA) recommends benzodiazepines alprazolam, bromazepam, lorazepam, and diazepam only as a second-line choice, if the treatment with two different antidepressants was unsuccessful. Although they are second-line agents, benzodiazepines can be used for a limited time to relieve severe anxiety and agitation. CPA guidelines state that after 4–6 weeks the effect of benzodiazepines may decrease to the level of placebo, and that benzodiazepines are less effective than antidepressants in alleviating ruminative worry, the core symptom of GAD, but that in some cases, a prolonged treatment with benzodiazepines as the add-on to an antidepressant may be justified.

On March 7, 2025, Duterte left for Hong Kong alongside Honeylet Avanceña, his daughter Veronica and his entourage. Although his lawyer Salvador Panelo said that his purpose of travel was to attend a KOJC-organized campaign sortie for Partido Demokratiko Pilipino among overseas Filipino workers, his departure coincided with reports that the release of an arrest warrant for Duterte from the International Criminal Court (ICC) was imminent. Others who attended the event include Duterte's daughter, Vice President Sara Duterte, Senators Ronald dela Rosa and Bong Go, and senatorial candidates Rodante Marcoleta and Vic Rodriguez. On March 11, 2025, upon his return from Hong Kong on a commercial flight, Duterte was arrested at Ninoy Aquino International Airport for crimes against humanity of murder, torture, and rape. The warrant was issued by the ICC, but coursed through Interpol. A top official of the Marcos administration earlier said that the government would honor its commitments to Interpol if an arrest warrant was issued, despite its policy of not cooperating with the ICC. Duterte questioned the warrant's legitimacy, asserting that the arrest did not follow standard procedures and that any prosecution should occur within the Philippines. His supporters rallied in major cities condemning the arrest, while activists hailed the arrest as a pivotal moment for justice. He was soon surrendered to the ICC in The Hague, Netherlands, where he was being held as of 11 March 2025.

== Pathophysiology == The liver plays a vital role in many metabolic processes in the body, including protein synthesis, detoxification, nutrient storage (such as glycogen), platelet production, and clearance of bilirubin. With progressive liver damage, hepatocyte death, and replacement of functional liver tissue with fibrosis in cirrhosis, these processes are disrupted. This leads to many of the metabolic derangements and symptoms seen in cirrhosis. Cirrhosis is often preceded by hepatitis and fatty liver (steatosis), independent of the cause. If the cause is removed at this stage, the changes are fully reversible. The pathological hallmark of cirrhosis is the development of scar tissue that replaces normal tissue, which is normally organized into lobules. This scar tissue blocks the portal flow of blood through the organ, raising the blood pressure. This manifests as portal hypertension in which the pressure gradient between the portal circulation as compared to the systemic circulation is elevated. This portal hypertension leads to decreased sinusoidal flow from liver cells to nearby sinusoids in the liver, and increased lymph production with extravasation of lymph to the extracellular space, causing ascites. This also causes reduced cardiac return and central blood volume, which activates the renin-angiotensin system (RAAS), which causes kidneys to reabsorb sodium and water, causing water retention and further ascites. Activation of the RAAS also causes kidney vasoconstriction and may cause kidney injury.

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 samples?

Anti-doping and clinical laboratories commonly use liquid chromatography-tandem mass spectrometry. The method can identify GW501516 and its metabolites in urine or blood. Detection depends on sample timing and the amount present.

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