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Background And Research Context — Quick Reference

By Editorial Desk · published 2026-04-16 · last reviewed 2026-05-21 · Wiki

PPARδ agonist raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.

This page was last updated on 2026-05-21 and is reviewed periodically as new material appears.

Background and Research Context

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.

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.

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.

Cardarine at a glance

PropertyValueNotes
CAS Registry Number317318-70-0Unique identifier for the compound.
Chemical classPPARδ agonistSynthetic ligand for peroxisome proliferator-activated receptor delta.
AppearanceWhite to off-white solidTypical form of research-grade material.
SolubilitySoluble in DMSO and ethanolPoorly soluble in water.
Typical storage-20°CRecommended for long-term storage of stock solutions.

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.

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.

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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.

Mechanism and Detection

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

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.

Background from the literature

Advanced product quality planning (APQP) is a framework of procedures and techniques used to develop products in industry, particularly in the automotive industry. It differs from Six Sigma in that the goal of Six Sigma is to reduce variation but has similarities to Design for Six Sigma (DFSS). According to the Automotive Industry Action Group (AIAG), the purpose of APQP is "to produce a product quality plan which will support development of a product or service that will satisfy the customer." It is a product development process employed by General Motors, Ford, Chrysler, and their suppliers.

The impact of this ~10 km asteroid massively altered the 187Os/188Os signature of marine sediments at that time - the average extraterrestrial 187Os/188Os of ~0.13 and the huge amount of Os this impact contributed (equivalent to 600,000 years of present-day riverine inputs) lowered the global marine 187Os/188Os value of ~0.45 to a minimum of ~0.2. Os isotope ratios may also be used as a signal of anthropogenic impact. The same 187Os/188Os ratios that are common in geological settings may be used to gauge the addition of anthropogenic Os through things like catalytic converters. While catalytic converters have been shown to drastically reduce the emission of NOx and CO, they are introducing platinum group elements (PGE) such as Os, to the environment. Other sources of anthropogenic Os include combustion of fossil fuels, smelting chromium ore, and smelting of some sulfide ores. In one study, the effect of automobile exhaust on the marine Os system was evaluated. Automobile exhaust 187Os/188Os has been recorded to be ~0.2 (similar to extraterrestrial and mantle derived inputs). The effect of anthropogenic Os can be seen best by comparing aquatic Os ratios and local sediments or deeper waters. Surface waters thought to be affected have depleted values compared to deep ocean and sediments by a ratio larger than can be explained by cosmic inputs. The alpha decay of 184Os into 180W (with a rate perhaps large enough for detection) has been proposed as a radiometric dating method for osmium-rich rocks or for differentiation of a planetary core.

females age 12 to 21 may have iron deficiency (27 June), researchers show how bird flu could mutate to overcome a human antiviral protein to start another pandemic (28 June), shortages of medications – including some against cancer – are reported across countries, articles in science outlets like Nature suggest contemporary viral concerns about hypothetical existential risk of AI "plays into the tech companies' agenda" – partly in the form of 'criti-hype' – and that this "hinders effective regulation of the societal harms AI is causing right now" and in the near-future. Promising results of therapeutic candidates are reported: first phase 3 trialed chikungunya vaccine (VLA1553) (12 June), mice-tested inoculation against a potential infectious contributor to endometriosis (14 June), new evidence regarding still-unclear vaginal seeding interventions (15 June), phase 2 trialed orforglipron against obesity (23 June), mice-tested gene-therapy against hearing loss (28 June).

Sources: en.wikipedia.org

Reference notes

Tim Hortons' advertising slogans have included "You've Always Got Time for Tim Hortons" and starting in the mid-2000s, "Always Fresh. Always Tim Hortons." Canadian Business named Tim Hortons as the best-managed brand in Canada in 2004 and 2005. From 2005 to 2023, Tim Hortons was the title sponsor of the Brier, the annual Canadian men's curling championships, along with the Canadian Ringette Championships. In September 2006, Tim Hortons courted controversy by mandating that employees were not to wear red as part of the Red Fridays campaign by families of the military to show support for Canadian troops. Within a few hours, Tim Hortons partially reversed its position and has allowed staff in Ontario stores to wear red ribbons or pins to show support for the wear red on Fridays campaign. In June 2009, Tim Hortons USA created Twitter and Facebook pages to drive online traffic. After Tim Hortons had agreed to provide 250 cups of free coffee in 2009 for a "Marriage and Family Day" hosted by the National Organization for Marriage, the company removed its sponsorship after it was revealed that the NOM was an organization that campaigns against gay marriage. The company stated the sponsorship was a violation of the company's policy not to sponsor events "representing religious groups, political affiliates or lobby groups." On July 12, 2013, it was announced that Tim Hortons had acquired the naming rights to the stadium being built in Hamilton, Ontario. In 2014, Tim Hortons Field became the home stadium of the Hamilton Tiger-Cats.

Trump began a push for peace negotiations to end the Russia–Ukraine war. Trump's first foreign visit as president-elect was to Paris for the reopening of the Notre-Dame de Paris, during which he met with French president Emmanuel Macron and Ukrainian president Volodymyr Zelenskyy to discuss the war, and met with other European officials. In February 2025, Trump held phone calls with Russian president Vladimir Putin and with Zelenskyy that he said marked the beginning of negotiations. He threatened Ukraine with a suspension of U.S. military aid and Russia with sanctions and tariffs if he decided they were not negotiating in good faith. The U.S. sought a mineral resources agreement with Ukraine though was unwilling to offer postwar security guarantees for Ukraine in exchange. Negotiators reached a deal on the agreement but the agreement fell through after a contentious meeting between Trump and Zelenskyy in the Oval Office that ended when the Ukrainian delegation was abruptly asked to leave. Afterwards, the U.K. and France developed a proposal in which a "coalition of the willing" would provide security guarantees to Ukraine. The U.S. and Russia held a summit in Saudi Arabia for peace talks in February and U.S. held a summit with Ukraine the next month, during which Ukraine accepted a U.S.-proposed 30-day ceasefire. Putin did not accept the ceasefire, though on March 18 Russia agreed to a 30-day ceasefire only for strikes on energy infrastructure and in the Black Sea, which Ukraine agreed to.

=== Miscellaneous === Italian police sought bribery charges in May 2004, against 4,400 doctors and 273 GSK employees. GSK and its predecessor were accused of having spent £152m on physicians, pharmacists and others, giving them cameras, computers, holidays and cash. Doctors were alleged to have received cash based on the number of patients they treated with a cancer drug, topotecan (Hycamtin). The following month prosecutors in Munich accused 70–100 doctors of having accepted bribes from SmithKline Beecham between 1997 and 1999. The inquiry was opened over allegations that the company had given over 4,000 hospital doctors money and free trips. All charges were dismissed by the Verona court in January 2009. In 2006, in the United States GSK settled the largest tax dispute in IRS history, agreeing to pay US$3.1 billion. At issue were Zantac and other products sold in 1989 to 2005. The case revolved around intracompany transfer pricing—determining the share of profit attributable to the US subsidiaries of GSK and subject to tax by the IRS. The UK's Serious Fraud Office (SFO) opened a criminal inquiry in 2014 into GSK's sales practices, using powers granted by the Bribery Act 2010. The SFO said it was collaborating with Chinese authorities to investigate bringing charges in the UK related to GSK's activities in China, Europe and the Middle East. Also as of 2014, the US Department of Justice was investigating GSK with reference to the Foreign Corrupt Practices Act.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist developed for research. It has not been approved as a medication in any country. It is classified as an unapproved drug and a prohibited substance in sport.

Is cardarine a steroid?

No. Cardarine is not an anabolic steroid; it belongs to a different chemical class that targets PPARδ. Steroids act primarily through androgen receptors, while cardarine acts through a nuclear receptor involved in metabolism.

What did animal studies find?

Some rodent studies reported increased endurance and changes in fat metabolism after cardarine exposure. Long-term studies in animals also raised concerns about cancer in certain tissues. Human trial data are limited, so these findings cannot be directly translated to people.

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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