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Cardarine As Investigational Pparδ Agonist — Reference Sheet

By Editorial Desk · published 2025-12-13 · last reviewed 2026-02-01 · Guide

A practical reference on GW501516: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

Reviewed 2026-02-01. Anything still debated is marked as such rather than presented as settled.

Cardarine as Investigational PPARδ Agonist

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.

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.

Identity and Pharmacological Mechanism

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.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516, GW-501516, GW 501516, endurobolNames vary in research and anti-doping documents.
Chemical classSynthetic PPARδ agonistSmall-molecule nuclear receptor ligand.
CAS Registry Number317318-70-0Identifier commonly associated with GW501516.
AppearanceWhite to off-white powderTypical for purified research material.
SolubilityLow in water; soluble in DMSO and ethanolOrganic solvents are common for laboratory stock solutions.

Mechanism and Detection

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.

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.

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Identity and Regulatory Status

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.

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.

Supporting material

== Recalls and safety corrections == In 2014, Tandem recalled selected lots of t:slim cartridges because leaks could cause too much or too little insulin to be delivered. In 2024, the FDA classified a correction of version 2.7 of the iOS t:connect app as a Class I recall. Repeated app crashes and automatic relaunches could increase Bluetooth communication, drain a connected t:slim X2 battery and interrupt insulin delivery. The action covered 85,863 distributed app installations; the FDA reported 224 injuries and no deaths as of April 15, 2024. Tandem released updated app versions and advised users to monitor pump batteries. In April 2025, the FDA classified a correction of Control-IQ+ software version 7.9 as a Class I recall. A defect affecting 85 pumps could incorrectly interpolate glucose values after gaps in CGM data and cause too much or too little insulin to be delivered. Tandem instructed affected users to turn off Control-IQ+ until the software was corrected. Later in 2025, Tandem issued two further corrections that the FDA classified as Class I recalls. One covered 171,750 t:slim X2 pumps whose speakers could fail and stop insulin delivery; the company reported 59 injuries and no deaths. The other covered 17,745 Mobi pumps that could falsely detect vibration-motor failure and enter a non-operational state, stopping insulin delivery and CGM sessions. Tandem directed users to install corrected pump software.

This problem however was resolved with the use of so-called self-polishing paints, in which the biocide was released at a slower rate as the seawater reacted with the surface layer of the paint. More recently, copper-based anti-fouling paints have been used because they are less toxic than TBT in aquatic environments, but are only effective against marine animal life, and not so much weed growth. Non-stick coatings contain no biocide but have extremely slippery surfaces which prevents most fouling and makes it easier to clean any fouling that occurs. Natural biocides are found on marine organisms such as coral and sponges and also prevent fouling if applied to a vessel. Creating a difference in electrical charge between the hull and seawater is a common practice in the prevention of fouling. This technology has proven to be effective, but is easily damaged and may be expensive. Finally, microscopic prickles can be added to a coating, and depending on length and distribution have shown the ability to prevent the attachment of most biofouling.

The rationale for establishing emission standards for non-road engines is that they are a significant source of pollution. The engines of on-road vehicles have advanced emission controls which are not found on those non-road engines. The non-road engines also emit air pollution particles at much higher rates. The emission standards are based on the engine classifications and vary in various jurisdictions. The main model regulations that are used by many countries are the United States Environmental Protection Agency through the section 213 of the Clean Air Act (42 U.S.C. 7547) and the directive of the European Commission (the "mother" Directive 97/68/EC, the amendments Directive 2002/88/EC, Directive 2004/26/EC, Directive 2006/105/EC, Directive 2011/88/EU and the last amendment Directive 2012/46/EU). The directives cover diesel engines, spark-ignition engines, constant-speed engines, railcars, locomotives and inland waterway vessels. In Europe, the term "non-road mobile machinery" (NRMM) is used to clarify that the definition refers to non-road engines that are capable of self-propulsion. In the European Union, in 2023, the Commission and the Council proposed to harmonize road safety requirements to ease non-road mobile machinery (such as lawn mowers, harvesters or bulldozers) to circulate on public roads and replace local European union member states regulations. This would only apply to machine with maximum speed greater than 6 km/hour (around 4 miles per hour). Next legislative step would be in the European parliament.

== Health aspects == Fruits that are rich in polyphenol oxidase activity may affect the polyphenol content of other fruits consumed in the same meal. In particular mixed fruit juices and smoothies are at risk, as different fruits (and their cellular content) are mixed long time before digestion enzymes can inactivate the polyphenol oxidase. Thus, these beverages contain considerably less bioactive polyphenoles compared to fruit juices made entirely of low-PPO fruits or whole fruits.

Sources: en.wikipedia.org

Supporting material

Single workplaces may have multiple unions, and in such cases an employer may apply to the FWC for an order that bargaining representatives meet to elect one to represent all of them if "the bargaining process is not proceeding efficiently or fairly because there are multiple bargaining representatives for the agreement."

== External links == Cluster and Nanocrystal Research Group, Technische Universität Berlin Molecular Diamond Technologies, Chevron Texaco Nanotechnology and the arrival of the Diamond Age Laser Raman Spectroscopy and Modelling of Diamondoids Electronic and Optical Properties of Diamondoids (free download) Diamondoid Molecules: With Applications in Biomedicine, Materials Science, Nanotechnology & Petroleum Science Diamondoid-functionalized gold nanogaps as sensors for natural, mutated, and epigenetically modified DNA nucleotides

== Monitoring == It is important to recognize that all described exercise programs were conducted by physicians or physiotherapists during the stable phase of the disease (except Painelli). Patients were monitored closely for indicators of deleterious effects, such as increases in serum creatine kinase, inflammation or weakness. Monitoring of this kind can only be done in conjunction with a medical team that is aware of the risks posed by increased inflammatory response in patients with IIM.

The Court of Justice held that the Directive could be relied on by her because equality was also a general principle of EU law. Fourth, if the defendant is an emanation of the state, even if not central government, it can still be bound by Directives. In Foster v British Gas plc the Court of Justice held that Mrs Foster was entitled to bring a sex discrimination claim against her employer, British Gas plc, which made women retire at age 60 and men at 65, if (1) pursuant to a state measure, (2) it provided a public service, and (3) had special powers. This could also be true if the enterprise is privatised, as it was held with a water company that was responsible for basic water provision. Fifth, national courts have a duty to interpret domestic law "as far as possible in the light of the wording and purpose of the directive". Textbooks (though not the Court itself) often called this "indirect effect". In Marleasing SA v La Comercial SA the Court of Justice held that a Spanish Court had to interpret its general Civil Code provisions, on contracts lacking cause or defrauding creditors, to conform with the First Company Law Directive article 11, that required incorporations would only be nullified for a fixed list of reasons. The Court of Justice quickly acknowledged that the duty of interpretation cannot contradict plain words in a national statute. But, if a member state has failed to implement a Directive, a citizen may not be able to bring claims against other non-state parties. It must instead sue the member state itself for failure to implement the law.

=== Childhood === Records suggest that his childhood was an active and happy one. His pastimes consisted of listening to music on the radio or records at home. Eastlack would also enjoy reading, playing with his sister, and going to the movies. Additionally, a seat was exclusively reserved for him at the center of the seventh row in Hamilton Theater, a musical theater, in Philadelphia. It has been claimed that ushers would not let anyone else sit there, as the spot was spacious enough to later allow Eastlack to stretch his immobile leg.

Sources: en.wikipedia.org

Notes from published material

==== Bretisilocin ==== In March 2026, bretisilocin entered European Medicines Agency's priority medicines (PRIME) scheme for major depressive disorder, while a phase 2 clinical trial was still ongoing.

The pastel shades of turquoise have endeared it to many great cultures of antiquity: it has adorned the rulers of Ancient Egypt, the Aztecs (and possibly other Pre-Columbian Mesoamericans), Persia, Mesopotamia, the Indus Valley, and to some extent in ancient China since at least the Shang dynasty. Despite being one of the oldest gems, probably first introduced to Europe (through Turkey) with other Silk Road novelties, turquoise did not become important as an ornamental stone in the West until the 14th century, following a decline in the Roman Catholic Church's influence which allowed the use of turquoise in secular jewellery. It was apparently unknown in India until the Mughal Empire period, and unknown in Japan until the 18th century. A common belief shared by many of these civilizations held that turquoise possessed certain prophylactic qualities; it was thought to change colour with the wearer's health and protect him or her from untoward forces. The Aztecs viewed turquoise as an embodiment of fire and gave it properties such as heat and smokiness. They inlaid turquoise, together with gold, quartz, malachite, jet, jade, coral, and shells, into provocative (and presumably ceremonial) mosaic objects such as masks (some with a human skull as their base), knives, and shields. Natural resins, bitumen and wax were used to bond the turquoise to the objects' base material; this was usually wood, but bone and shell were also used.

== Weak affinity chromatography == Weak affinity chromatography (WAC) is an affinity chromatography technique for affinity screening in drug development. WAC is an affinity-based liquid chromatographic technique that separates chemical compounds based on their different weak affinities to an immobilized target. The higher affinity a compound has towards the target, the longer it remains in the separation unit, and this will be expressed as a longer retention time. The affinity measure and ranking of affinity can be achieved by processing the obtained retention times of analyzed compounds. Affinity chromatography is part of a larger suite of techniques used in chemoproteomics based drug target identification. The WAC technology is demonstrated against a number of different protein targets – proteases, kinases, chaperones and protein–protein interaction (PPI) targets. WAC has been shown to be more effective than established methods for fragment based screening.

===== Finland ===== In Finland, semaglutide is included in the national price regulation scheme and is available by prescription. For people with type 2 diabetes and a BMI over 27, part of the cost is covered by Kela, the Finnish social insurance institution.

=== Apodization in digital audio === An apodizing filter can be used in digital audio processing instead of the more common brick-wall filters, in order to reduce the pre- and post-ringing that the latter introduces.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.

Is cardarine a steroid?

No. Cardarine is not a steroid hormone; it targets the nuclear receptor PPARδ. Its classification in anti-doping rules differs from anabolic steroids, though it remains prohibited in sport.

Why was cardarine not developed further?

Early rodent studies reported tumor formation at multiple sites, which raised safety concerns. Sponsors stopped clinical development, and no approved human product exists.

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.

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