If you have been reading about PPARδ agonist 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.
Last reviewed on 2026-03-18. Where a claim depends on a specific study, the study is described rather than over-claimed.
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.
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.
At the molecular level, GW501516 binds and activates PPARδ, a nuclear receptor that regulates transcription. Activation shifts expression of genes involved in fatty acid oxidation, energy expenditure, and lipid transport in skeletal muscle and liver. Animal studies report increased endurance and altered lipid profiles after exposure. Human data are limited to small trials and do not establish long-term safety or efficacy. PPARδ also has roles in cell proliferation, so the relationship between activation and cancer risk remains an open question.
Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.
Cardarine is the common name for GW501516, a synthetic compound studied as a peroxisome proliferator-activated receptor delta agonist. Researchers developed it to explore treatments for lipid disorders and metabolic conditions. It is not an approved medicine in any country. Early clinical work examined changes in HDL cholesterol and triglycerides, but development was discontinued after animal studies raised concerns about cancer. The compound remains available as a research chemical and appears in discussions of performance enhancement.
| Property | Value | Notes |
|---|---|---|
| IUPAC name | {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid | Systematic name for GW501516 |
| CAS Registry Number | 317318-70-0 | Unique identifier for the parent compound |
| Molecular formula | C21H18F3NO3S2 | Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur |
| Molecular weight | 453.5 g/mol | Approximate value for the neutral form |
| Appearance | White to off-white powder | Typical description for purified laboratory material |
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.
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.
Stability of GW501516 depends on form, temperature, light exposure, and moisture. Solid reference material is typically stored frozen or refrigerated in a desiccator and protected from light. Solutions in organic solvents such as dimethyl sulfoxide are often kept frozen in aliquots to reduce freeze-thaw cycling. Aqueous solubility is low, so aqueous stock solutions can be difficult to prepare without cosolvents. Degradation may appear as changes in chromatographic purity or mass spectral signal. Stability studies are needed to establish shelf life for any specific preparation.
Quality assessment for cardarine samples usually combines identity, purity, and impurity testing. Nuclear magnetic resonance spectroscopy and mass spectrometry can confirm molecular structure, while high-performance liquid chromatography estimates purity. Certificates of analysis from testing laboratories may list these results, but they do not establish safety or legality. In the absence of approved manufacturing, products sold online may contain the wrong compound, variable amounts, or unlisted contaminants. Independent verification is therefore central to analytical work and to interpreting any reported biological activity.
The stabilisation of ununennium's valence electron and thus the contraction of the 8s orbital cause its atomic radius to be lowered to 240 pm, very close to that of rubidium (247 pm), so that the chemistry of ununennium in the +1 oxidation state should be more similar to the chemistry of rubidium than to that of francium. On the other hand, the ionic radius of the Uue+ ion is predicted to be larger than that of Rb+, because the 7p orbitals are destabilised and are thus larger than the p-orbitals of the lower shells. Ununennium may also show the +3 and +5 oxidation states, which are not seen in any other alkali metal, in addition to the +1 oxidation state that is characteristic of the other alkali metals and is also the main oxidation state of all the known alkali metals: this is because of the destabilisation and expansion of the 7p3/2 spinor, causing its outermost electrons to have a lower ionisation energy than what would otherwise be expected. Indeed, many ununennium compounds are expected to have a large covalent character, due to the involvement of the 7p3/2 electrons in the bonding.
== Discovery and synthesis == Djenkolic acid was first isolated by Van Veen and Hyman in 1933 from the urine of the natives of Java who had eaten the djenkol bean and were suffering from poisoning. They then isolated the djenkolic acid crystals by treating the djenkol beans with barium hydroxide at 30°C for a prolonged period. Du Vigneaud and Patterson managed to synthesize djenkolic acid by condensation of methylene chloride with 2 moles of L-cysteine in liquid ammonia. Later on, Armstrong and du Vigneaud prepared djenkolic acid by the direct combination of 1 mole of formaldehyde with 2 moles of L-cysteine in a strongly acidic solution.
=== Bioremediation === Some yeasts can find potential application in the field of bioremediation. One such yeast, Yarrowia lipolytica, is known to degrade palm oil mill effluent, TNT (an explosive material), and other hydrocarbons, such as alkanes, fatty acids, fats and oils. It can also tolerate high concentrations of salt and heavy metals, and is being investigated for its potential as a heavy metal biosorbent. Saccharomyces cerevisiae has potential to bioremediate toxic pollutants like arsenic from industrial effluent. Bronze statues are known to be degraded by certain species of yeast. Different yeasts from Brazilian gold mines bioaccumulate free and complexed silver ions.
== Endolithic fungi and algae in marine ecosystems == Although it is possible that endolithic fungi could play an important role in the health of coral reefs, only limited research has been conducted on the distribution and diversity of marine endolithic fungi. Endolithic fungi have been discovered in shells as early as the year 1889 by Edouard Bornet and Charles Flahault. These two French phycologists specifically provided descriptions for two fungi: Ostracoblabe implexis and Lithopythium gangliiforme. Discovery of endolithic fungi, such as Dodgella priscus and Conchyliastrum, has also been made in the beach sand of Australia by George Zembrowski. Findings have also been made in coral reefs and have been found to be, at times, beneficial to their coral hosts. In the wake of worldwide coral bleaching, studies have suggested that the endolithic algae located in the skeleton of the coral may be aiding the survival of coral species by providing an alternative source of energy. Although the role that endolithic fungi play is important in coral reefs, it is often overlooked because much research is focused on the effects of coral bleaching as well as the relationships between Coelenterate and endosymbiotic Symbiodinia. According to a study done by Astrid Gunther endoliths were also found in the island of Cozumel (Mexico). The endoliths found there not only included algae and fungi but also included cyanobacteria, sponges as well as many other microborers.
Sources: en.wikipedia.org
== Biosynthesis == Nystatin A1 (often called nystatin) is biosynthesized by a bacterial strain, Streptomyces noursei. The structure of this active compound is characterized as a polyene macrolide with a deoxysugar D-mycosamine, an aminoglycoside. The genomic sequence of nystatin reveals the presence of the polyketide loading module (nysA), six polyketide syntheses modules (nysB, nysC, nysI, nysJ, and nysK) and two thioesterase modules (nysK and nysE). It is evident that the biosynthesis of the macrolide functionality follows the polyketide synthase I pathway. Following the biosynthesis of the macrolide, the compound undergoes post-synthetic modifications, which are aided by the following enzymes: GDP-mannose dehydratase (nysIII), P450 monooxygenase (nysL and nysN), aminotransferase (nysDII), and glycosyltransferase (nysDI). The biosynthetic pathway is thought to proceed as shown to yield nystatin.
=== Ancient world === Prehistoric medicine incorporated plants (herbalism), animal parts, and minerals. In many cases these materials were used ritually as magical substances by priests, shamans, or medicine men. Well-known spiritual systems include animism (the notion of inanimate objects having spirits), spiritualism (an appeal to gods or communion with ancestor spirits); shamanism (the vesting of an individual with mystic powers); and divination (magically obtaining the truth). The field of medical anthropology examines the ways in which culture and society are organized around or impacted by issues of health, health care and related issues. The earliest known medical texts in the world were found in the ancient Syrian city of Ebla and date back to 2500 BCE. Other early records on medicine have been discovered from ancient Egyptian medicine, Babylonian Medicine, Ayurvedic medicine (in the Indian subcontinent), classical Chinese medicine (Alternative medicine) predecessor to the modern traditional Chinese medicine), and ancient Greek medicine and Roman medicine. In Egypt, Imhotep (3rd millennium BCE) is the first physician in history known by name. The oldest Egyptian medical text is the Kahun Gynaecological Papyrus from around 2000 BCE, which describes gynaecological diseases. The Edwin Smith Papyrus dating back to 1600 BCE is an early work on surgery, while the Ebers Papyrus dating back to 1500 BCE is akin to a textbook on medicine.
== Legal status == Dioxaphetyl butyrate is listed as an internationally controlled opioid under Schedule I of the 1961 Single Convention on Narcotic Drugs.[ref] In Australia, the Office of Drug Control lists it as a narcotic requiring import and export licensing and permits. In the United States it is a Schedule I Narcotic controlled substance with an ACSCN of 9621 and a 2013 annual aggregate manufacturing quota of zero.
Immune checkpoints affect the immune system function. Immune checkpoints can be stimulatory or inhibitory. Tumors can use these checkpoints to protect themselves from immune system attacks. Checkpoint therapies approved as of 2012 block inhibitory checkpoint receptors. Blockade of negative feedback signaling to immune cells thus results in an enhanced immune response against tumors. As of 2020, immune checkpoint blockade therapies have varied effectiveness. In Hodgkin lymphoma and natural killer T-cell lymphoma, response rates are high, at 50–60%. Response rates are quite low for breast and prostate cancers, however. A major challenge are the large variations in responses to immunocheckpoint inhibitors, some patients showing spectacular clinical responses while no positive effects are seen in others. A plethora of possible reasons for the absence of efficacy in many patients have been proposed, but the biomedical community has still to begin to find consensus in this respect. For instance, a recent paper documented that infection with Helicobacter pylori would negatively influence the effects of immunocheckpoint inhibitors in gastric cancer., but this notion was quickly challenged by others. One ligand-receptor interaction under investigation is the interaction between the transmembrane programmed cell death 1 protein (PDCD1, PD-1; also known as CD279) and its ligand, PD-1 ligand 1 (PD-L1, CD274). PD-L1 on the cell surface binds to PD1 on an immune cell surface, which inhibits immune cell activity. Among PD-L1 functions is a key regulatory role on T cell activities.
=== Planets === Though many other civilisations in the Culture books live on planets, the Culture as currently developed has little direct connection to on-planet existence. Banks has written that he presumes this to be an inherent consequence of space colonisation, and a foundation of the liberal nature of the Culture. A small number of home worlds of the founding member-species of the Culture receive a mention in passing, and a few hundred human-habitable worlds were colonised (some of them terraformed) before the Culture elected to turn towards artificial habitats, preferring to keep the planets it encounters wild. Since then, the Culture has come to look down on terraforming as inelegant, ecologically problematic and possibly even immoral. Less than one per cent of the population of the Culture lives on planets, and many find the very concept somewhat bizarre. This attitude is not absolute though; in Consider Phlebas, some Minds suggest testing a new technology on a "spare planet" (knowing that it could be destroyed in an antimatter explosion if unsuccessful). One could assume – from Minds' usual ethics – that such a planet would have been lifeless to start with. It is also quite possible, even probable, that the suggestion was not made in complete seriousness.
Sources: en.wikipedia.org
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.
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.
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.
Cardarine is a common name for the investigational compound GW501516. It acts as a PPARδ agonist and is not approved for human use. It is prohibited in sport.