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Identity And Pharmacological Classification — Reference Sheet

By Editorial Desk · published 2026-05-02 · last reviewed 2026-06-06 · Data

PPARδ agonist is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.

Updated 2026-06-06. Numbers and descriptions here follow the published literature rather than marketing material.

Identity and Pharmacological Classification

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 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.

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.

Cardarine at a glance

PropertyValueNotes
Chemical classPPARδ agonistNot an anabolic steroid.
Common synonymsGW501516, GW-1516Cardarine is an informal name.
AppearanceWhite to off-white powderTypical for research-grade solid.
Solubility classPoorly soluble in water; soluble in some organic solventsSuch as DMSO or ethanol in laboratory settings.
Typical storage temperatureCool, dry, protected from lightSpecific conditions vary by supplier and form.

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.

Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.

Related pages on this site

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.

Regulation and Detection

Cardarine is frequently described as a fat-burning or endurance-enhancing supplement, but these claims exceed the available evidence. The compound is not a hormone, steroid, or selective androgen receptor modulator. Research articles discuss it as a tool compound for studying PPARδ biology, while anti-doping literature focuses on its abuse and detection. Quality of unapproved products is uncertain, and independent analyses have found impurities or incorrect labeling. Open questions include whether human cancer risk resembles that seen in rodents and how often non-athletes use the substance.

Cardarine has no approved therapeutic indication and is not marketed as a medicine. The World Anti-Doping Agency lists GW501516 as a prohibited substance at all times, covering both in-competition and out-of-competition periods. National laws vary: some countries treat it as an unapproved drug subject to import controls, while others have specific restrictions on sale for human consumption. It is often sold as a research chemical, a label that does not imply safety or legality. Enforcement actions have targeted online vendors and shipments.

Anti-doping laboratories identify GW501516 and related metabolites using liquid chromatography coupled with tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be analyzed. The method targets the parent compound and phase I and phase II metabolites, which extend the detection window. Because the substance is prohibited at all times, athletes can be tested outside competition. Detection limits and windows depend on the assay, sample type, and individual metabolism.

Further detail

Pakistani military claimed to have killed 34 TTP militants in engagement throughout Khyber Pakhtunkhwa and Balochistan, with three killed in Lakki Marwat district, 10 killed in Bannu district and 13 killed in North Waziristan as well as eight killed in Zhob district. A police constable was killed in a militant attack in Wana while six police personnel including a DSP were killed and three were wounded in an insurgent ambush in Kohat District. An ex-Police officer and a militant were killed while another militant was injured in an engagement in Peshawar District. On 25 February, local sources reported that further skirmishes took place in Maqbal area in Dand Aw Patan District of Paktia province between Taliban and Pakistani forces. Light clashes took place in Mohmand and Kurram Districts whereas heavy fighting occurred in Khyber District between Pakistani security forces and Pakistani Taliban. Pakistani military claimed to have killed 10 TTP militants in a follow-up operation in Zhob District. Unidentified militants attacked a police patrol in Bajaur killing four and wounding two police personnel and also killed a constable and his son in South Waziristan. On 26 February, at around 20:00 local time (15:30 GMT), Taliban-led Afghanistan's officials announced the launch of what they described as a "retaliatory operation", directed by Defence Minister Mullah Yaqoob and Army Chief Fasihuddin Fitrat, along the border in the provinces of Nangarhar, Nuristan, Kunar, Khost, Paktia, and Paktika.

=== System IV === Four membrane proteins are necessary for the attachment of a heme in cytochrome b6. A major difference to systems I-III is that the heme attachment occurs at the opposite side of the lipid bilayer compared to the other systems.

== History == In February 2003, Nabil Seidah and Jae Byun, a scientist at the Clinical Research Institute of Montreal in Canada, discovered a novel human proprotein convertase, the gene for which was located on the short arm of chromosome 1. Meanwhile, a lab led by Catherine Boileau at the Necker–Enfants Malades Hospital in Paris had been following families with familial hypercholesterolaemia, a genetic condition that, in 90% of cases causes coronary artery disease (FRAMINGHAM study) and in 60% of cases may lead to an early death; they had identified a mutation on chromosome 1 carried by some of these families, but had been unable to identify the relevant gene. The labs got together and by the end of the year published their work, linking mutations in the gene, now identified as PCSK9, to the condition. In their paper, they speculated that the mutations might make the gene overactive. In that same year, investigators at Rockefeller University and University of Texas Southwestern had discovered the same protein in mice, and had worked out the novel pathway that regulates LDL cholesterol in which PCSK9 is involved, and it soon became clear that the mutations identified in France led to excessive PCSK9 activity, and thus excessive removal of the LDL receptor, leaving people carrying the mutations with too much LDL cholesterol. Meanwhile, Helen H. Hobbs and Jonathan Cohen at UT-Southwestern had been studying people with very high and very low cholesterol, and had been collecting DNA samples.

Sources: en.wikipedia.org

Background from the literature

=== Environmental === Environmental biotechnology includes various disciplines that play an essential role in reducing environmental waste and providing environmentally safe processes, such as biofiltration and biodegradation. The environment can be affected by biotechnologies, both positively and adversely. Vallero and others have argued that the difference between beneficial biotechnology (e.g., bioremediation is to clean up an oil spill or hazard chemical leak) versus the adverse effects stemming from biotechnological enterprises (e.g., flow of genetic material from transgenic organisms into wild strains) can be seen as applications and implications, respectively. Cleaning up environmental wastes is an example of an application of environmental biotechnology; whereas loss of biodiversity or loss of containment of a harmful microbe are examples of environmental implications of biotechnology. Many cities have installed CityTrees, which use biotechnology to filter pollutants from urban atmospheres.

=== Advertisements === Being the product of a Chicago company, Ferrara Pan was a prominent sponsor of The Bozo Show on WGN-TV (along with its national superstation feed), with Lemonhead specifically promoted, and a gift package of various Ferrara Pan candies often being given as a close-bucket prize during the "Grand Prize Game". In the 1980s, Lemonhead candy advertisements were mostly centered around sports. The commercials followed a similar pattern and featured a children's sports team; the player who made a mistake would be labeled the "lemonhead". In the 2010s, Lemonhead candy commercials featured athletes as well as the Lemonhead mascot. The mascot was pictured alongside popular athletes scoring in games or otherwise achieving athletic success. In 2014, the company rebranded the mascot to feature a more mature figure as the face of Lemonhead candies.

A group or series of case reports involving patients who were given similar treatment. Reports of case series usually contain detailed information about the individual patients. This includes demographic information (for example, age, gender, ethnic origin) and information on diagnosis, treatment, response to treatment, and follow-up after treatment. (NCI) Case-control study

Sources: en.wikipedia.org

Reference notes

== Treatment == Standard intravenous preparations of potassium phosphate are available and are routinely used in malnourished people and people who consume excessive amounts of alcohol. Supplementation by mouth is also useful where no intravenous treatment are available. Historically one of the first demonstrations of this was in people in concentration camp who died soon after being re-fed: it was observed that those given milk (high in phosphate) had a higher survival rate than those who did not get milk. Monitoring parameters during correction with IV phosphate

In Plaumann & Co v Commission the Court of Justice held that a clementine importer was not individually concerned when the Commission refused permission to Germany to stop import custom duties. This kept it more expensive for Mr Plaumann to import clementines, but it was equally expensive for everyone else. This decision heavily restricted the number of people who could claim for judicial review. In Unión de Pequeños Agricultores, Advocate General Jacobs propose a broader test of allowing anyone to claim if there was a "substantial adverse effect" on the claimant's interests. Here, a group of Spanish olive oil producers challenged Council Regulation No 1638/98, which withdrew subsidies. Because Regulations are not implemented in national law, but have direct effect, they argued the requirement for individual concern would deny them effective judicial protection. The Court of Justice held that direct actions were still not allowed: if this was unsatisfactory the member states would have to change the treaties. Individual concern is not needed, however under article 263(4), if an act is not legislation, but just a "regulatory act". In Inuit Tapiriit Kanatami v Parliament and Council the Court of Justice affirmed that a Regulation does not count as a "regulatory act" within the Treaty's meaning: it is only meant for acts of lesser importance. Here, a Canadian group representing the Inuit wished to challenge a Regulation on seal products, but were not allowed. They would have to show both direct and individual concern as normal.

== Theca externa == The theca externa is the outer layer of the theca in the follicle. It is derived from connective tissue, the cells resemble fibroblasts, and contain abundant collagen. During ovulation, the surge in luteinizing hormone (LH surge) increases cAMP which increases progesterone and PGF2α production. PGF2α induces the contraction of the smooth muscle cells of the theca externa, increasing intrafollicular pressure. This aids in rupture of the mature oocyte, or immature oocyte at the germinal vesicle stage in the canine, along with plasmin and collagenase degradation of the follicle wall.

Some meteorologists prefer the hectopascal (hPa) for atmospheric air pressure, which is equivalent to the older unit millibar (mbar). Similar pressures are given in kilopascals (kPa) in most other fields, except aviation where the hecto- prefix is commonly used. The inch of mercury is still used in the United States. Oceanographers usually measure underwater pressure in decibars (dbar) because pressure in the ocean increases by approximately one decibar per metre depth. The standard atmosphere (atm) is an established constant. It is approximately equal to typical air pressure at Earth mean sea level and is defined as 101325 Pa (IUPAC recommends the value 100000 Pa, but prior to 1982 the value 101325 Pa (= 1 atm) was usually used). Because pressure is commonly measured by its ability to displace a column of liquid in a manometer, pressures are often expressed as a depth of a particular fluid (e.g., centimetres of water, millimetres of mercury or inches of mercury). The most common choices are mercury (Hg) and water; water is nontoxic and readily available, while mercury's high density allows a shorter column (and so a smaller manometer) to be used to measure a given pressure. The pressure exerted by a column of liquid of height h and density ρ is given by the hydrostatic pressure equation p = ρgh, where g is the gravitational acceleration. Fluid density and local gravity can vary from one reading to another depending on local factors, so the height of a fluid column does not define pressure precisely.

Sources: en.wikipedia.org

Frequently asked questions

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.

Is cardarine a steroid?

No, cardarine is not a steroid. It is classified as a PPARδ agonist. Its structure and receptor target differ from anabolic steroids.

Has cardarine been approved for human use?

No regulatory agency has approved cardarine as a medicine. It was investigated in early research but development was discontinued. It is not available as a prescription drug.

Is cardarine legal to buy?

Legal status varies by country, but cardarine is not approved as a medicine in major jurisdictions. It is often sold as a research chemical, a category that may not be lawful for human use. Buyers should check local laws and product labels carefully.

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