PPARδ agonist raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.
Reviewed 2026-06-10. Anything still debated is marked as such rather than presented as settled.
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.
Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.
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 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.
| Property | Value | Notes |
|---|---|---|
| Common synonyms | GW501516; GW-1516; endurobol | GW501516 is the research code |
| Drug class | PPARδ agonist | Not a selective androgen receptor modulator |
| Molecular formula | C21H18F3NO3S2 | Established chemical formula |
| Molar mass | 453.5 g/mol | Calculated from the formula |
| Regulatory status | Prohibited in sport; not approved as medicine | Status varies by country |
Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.
A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.
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.
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.
Human mitochondrial DNA encodes 13 proteins of the respiratory chain, while most of the estimated 1,500 proteins and components targeted to mitochondria are nuclear-encoded. Defects in nuclear-encoded mitochondrial genes are associated with hundreds of clinical disease phenotypes including anemia, dementia, hypertension, lymphoma, retinopathy, seizures, and neurodevelopmental disorders. A study by Yale University researchers (published in the February 12, 2004, issue of the New England Journal of Medicine) explored the role of mitochondria in insulin resistance among the offspring of patients with type 2 diabetes. Other studies have shown that the mechanism may involve the interruption of the mitochondrial signaling process in body cells (intramyocellular lipids). A study conducted at the Pennington Biomedical Research Center in Baton Rouge, Louisiana showed that this, in turn, partially disables the genes that produce mitochondria.
For services to the community in Banbury, Oxfordshire. Malcolm John Kightley. For services to the Holy Sepulchre Church, Northampton. Lorna Jean King. For services to Jersey Hospice Care. Alison Kinnaird, Clarsach player and teacher, and glass engraver. For services to Music and to Art. Inna Kirillova. For services to Anglo/Russian relations. Captain Alex Kirk, lately Honorary Secretary, Hartlepool Lifeboat Station, Royal National Lifeboat Institution. For services to the RNLI. Bernadette Ann Kirk, Diabetes Specialist Nurse, Nottingham City Hospital NHS Trust. For services to Health Care. Donald Henry Kirk. For services to the Royal London Aid Society. Wendy Patricia Knight. For services to the British Red Cross Society in Hampshire. Alan Keith Knowles. For services to Remploy in Norwich, Norfolk. Mildred Eveline Knowles. For services to disabled people in Berkshire. Luis Eric Rupert de la Torre. For services to The St. Nazaire Society. Thomas Percival Langridge, Founder, the Pahar Trust. For charitable services. David Stuart Large, Constable, Cheshire Constabulary. For services to the Police and to the community in Winsford. Margaret Elsie Ann Lawrance. For services to the community in Loughton, Essex. Iain William Lawrence, Managing Director, Thomas Smith & Company (Peterhead) Ltd. For services to the Textile Industry. R. Mary Lawrence, Caretaker, Irfon Valley County Primary School, Powys. For services to Education and to the community. Bernard Robert Lawson, Lord Mayor's Secretary, Manchester City Council. For services to Local Government.
== Medical uses == Spironolactone is used in the treatment of heart failure with reduced ejection fraction (HFrEF), where evidence shows that it reduces the risk of heart failure hospitalisation and mortality when added to standard therapy. Multiple studies show that spironolactone improves left ventricular diastolic function in patients with heart failure with preserved ejection fraction HFpEF, though without benefits in death from any cause or overall hospitalisation. One randomised controlled trial showed a modest reduction in hospitalisation due to heart failure. A secondary analysis of TOPCAT suggested possible benefit in patients with both HFpEF and resistant hypertension, but this has not been confirmed in a prospective trial designed for this subgroup. Spironolactone is an effective fourth-line add-on therapy for lowering blood pressure in resistant hypertension that remains uncontrolled despite an ACE inhibitor or ARB, calcium channel blocker, and diuretic. It is also used to treat edematous conditions such as nephrotic syndrome or ascites in people with liver disease, essential hypertension, low blood levels of potassium, secondary hyperaldosteronism (such as occurs with liver cirrhosis), and Conn's syndrome (primary hyperaldosteronism). The most common use of spironolactone is in the treatment of heart failure. On its own, spironolactone is only a weak diuretic because it primarily targets the distal nephron (collecting tubule), where only small amounts of sodium are reabsorbed, but it can be combined with other diuretics to increase efficacy.
Sources: en.wikipedia.org
=== Alkylation of carboxylic acids and their salts === Trimethyloxonium tetrafluoroborate can be used for esterification of carboxylic acids under conditions where acid-catalyzed reactions are infeasible:
Since breasts are an external organ and do not contain muscle, exercise cannot improve their shape. They are not protected from external forces and are subject to gravity. Many women mistakenly believe that breasts cannot anatomically support themselves and that wearing a brassiere will prevent their breasts from sagging later in life. Researchers, bra manufacturers, and health professionals have not found any evidence to support the idea that wearing a bra for any amount of time slows breast ptosis. Bra manufacturers are careful to claim that bras only affect the shape of breasts while they are being worn. There is some evidence that bra use reduces the development of Cooper's ligaments, connective tissue that supports breast shape. That atrophy from bra-wearing may therefore lead to more breast sag in the long run, much as the connective tissue in a limb weakens while it is in a cast and must be re-strengthened afterward. Studies have actually documented that, after an initial period of adjustment, women experienced a significant increase in comfort and breast firmness after forgoing bras.
== Variants == A common variant is Lillie's trichrome, which uses aniline blue instead of a green dye. It is often erroneously called Masson's trichrome. It differs in the dyes used, their concentrations, and the immersion times. Another common variant is the Masson trichrome & Verhoeff stain, which combines the Masson trichrome stain and Verhoeff's stain. This combination is useful for the examination of blood vessels; the Verhoeff stain highlights elastin (black) and allows one to easily differentiate small arteries (which typically have at least two elastic laminae) and veins (which have one elastic lamina).
=== Chemistry === Like the other noble gases, krypton is chemically highly unreactive. The rather restricted chemistry of krypton in the +2 oxidation state parallels that of the neighboring element bromine in the +1 oxidation state; due to the scandide contraction it is difficult to oxidize the 4p elements to their group oxidation states. Until the 1960s no noble gas compounds had been synthesized. Following the first successful synthesis of xenon compounds in 1962, synthesis of krypton difluoride (KrF2) was reported in 1963. In the same year, KrF4 was reported by Grosse, et al., but was subsequently shown to be a mistaken identification. Under extreme conditions, krypton reacts with fluorine to form KrF2 according to the following equation:
Sources: en.wikipedia.org
=== Rule in Xikang prior to 1933 === Liu Wenhui maintained a tense relationship with the Nanjing government. In 1928, when the central government announced the creation of Suiyuan and Chahar provinces, it also announced plans for a new Xikang province. However, Liu protested this move and claimed that the resources of the proposed Xikang would be insufficient, because more than half of the counties were under Tibetan occupation. He attempted to lobby Nanjing for control of more eight counties in neighboring Sichuan, Yunnan, and Qinghai, and also asked for more funds to develop Xikang and defeat Tibet; both requests were ignored by the central government. Around this time, an attempt by Nanjing to create Xikang Province on its own terms under the auspices of Kesang Tsering (唐柯三) was thwarted by Liu, who instead set up his own administrative committee in parallel with the central government's one. The Chinese authorities finally gave up after Liu started executing members of the government's committee. According to Leibold, Chiang Kai-shek backed down from asserting control over Xikang because of the tenuous situation of the Kuomintang's rule over China at the time. While in Xikang, he took a vigorous role in spearheading the development of the capital Kangding in particular, establishing several schools and agricultural experimental stations, as well as constructing a road from Kangding to Rongxian in Sichuan.
==== Nucleic acid-based molecules ==== Nanogels are advantageous carriers of small, nucleic-acid based molecules that can be employed to treat a variety of diseases. Examples of three different types of molecules that fall into this category, oligonucleotides, miRNA, and nucleoside analogs, are discussed here. In one study, cationic synthetic nanogels modified with insulin and transferrin were synthesized to transport oligonucleotides, a possible therapeutic and diagnostic tool for neurodegenerative disorders, to the brain. These nanogels successfully localized through an in vitro model of the blood-brain barrier and accumulated in the brain in a mouse model. With the treatment of cardiovascular diseases in mind, polysaccharide-based nanogels have been functionalized with fucoidan to target overexpressed P-selectin receptors on platelets and endothelial cells. After loading with miRNA, these nanogels bound to platelets and became internalized by an endothelial cell line. Nanogels have also been used to encapsulate phosphorylated nucleoside analogs, or active forms of anticancer therapeutics. In one study, nanogels loaded with nucleoside 5'-triphosphates underwent surface modifications and successfully bound to overexpressed folate receptors on breast cancer cells. These nanogels were then internalized by the cells and produced a significant increase in cytotoxicity compared to control groups.
== Life == Vital Brazil Mineiro da Campanha was born on April 28, 1865, in the town of Campanha, in the state of Minas Gerais, Southeastern of the Empire of Brazil. His father gave him this curious name in homage to the country, the state and the city where he was born, as well as from the date, St. Vital’s Day. He graduated from the Rio de Janeiro School of Medicine in 1891, working as a technical assistant in the chair of Physiology in order to pay for his tuition and living expenses. After graduating, he began work in public health, initially as a sanitary inspector in São Paulo (1892–1895), where he acquired experience in the prevalent epidemic diseases of the time (smallpox, typhoid fever, yellow fever and cholera), and then as a private practitioner in the city of Botucatu, from 1895 to 1896.
Sources: en.wikipedia.org
No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.
No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.
Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.
No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.