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 2026-06-17 and is reviewed periodically as new material appears.
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.
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.
| 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 |
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.
Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.
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.
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.
=== Contamination === Any addition of carbon to a sample of a different age will cause the measured date to be inaccurate. Contamination with modern carbon causes a sample to appear to be younger than it really is: the effect is greater for older samples. If a sample that is 17,000 years old is contaminated so that 1% of the sample is modern carbon, it will appear to be 600 years younger; for a sample that is 34,000 years old, the same amount of contamination would cause an error of 4,000 years. Contamination with old carbon, with no remaining 14C, causes an error in the other direction independent of age – a sample contaminated with 1% old carbon will appear to be about 80 years older than it truly is, regardless of the date of the sample.
== Pharmacology == Saxagliptin is part of a class of diabetes medications called dipeptidyl peptidase-4 (DPP-4) inhibitors. DPP-4 is an enzyme that breaks down incretin hormones. As a DPP-4 inhibitor, saxagliptin slows down the breakdown of incretin hormones, increasing the level of these hormones in the body. It is this increase in incretin hormones that is responsible for the beneficial actions of saxagliptin, including increasing insulin production in response to meals and decreasing the rate of gluconeogenesis in the liver. Dipeptidyl peptidase-4's role in blood glucose regulation is thought to be through degradation of GIP and the degradation of GLP-1. Because incretin hormones are more active in response to higher blood sugar levels (and are less active in response to low blood sugar), the risk of dangerously low blood sugar (hypoglycemia) is low with saxagliptin monotherapy.
==== Russian preparations and invasion of Georgia ==== The commission noted, "the sum of actions undertaken by Russia by mid-2008 amounted to a threat of force vis-à-vis Georgia", and that Georgia felt "a substantial risk of Russian military intervention". The commission noted that "Russian military operations in Georgia in August 2008 appear to most analysts to have been well-planned and well-executed." The commission noted that many international experts "also believe that the massive Russian military action in August 2008 caught the Georgians off guard and unprepared both strategically and tactically." The commission noted that Russian military base Ugardanta in the Dzau District and Russian military rehabilitation centre in the north-west Tskhinvali were constructed before the August 2008 conflict. As far as legality of use of force by Russia was concerned, the report took a "differentiated" approach, dividing "the Russian reaction to the Georgian attack" into two phases – the one, which was "the immediate reaction in order to defend Russian peacekeepers" in Tskhinvali and the second one, "the invasion of Georgia by Russian armed forces reaching far beyond the administrative boundary of South Ossetia", which was "beyond the reasonable limits of defence".
From the late nineteenth century until the early 1930s, light therapy was considered an effective and mainstream medical therapy in the UK for conditions such as varicose ulcer, 'sickly children' and a wide range of other conditions. Controlled trials by the medical scientist Dora Colebrook, supported by the Medical Research Council, indicated that light therapy was not effective for such a wide range of conditions.
Each February, Tim Hortons holds a marketing campaign titled "Roll Up the Rim to Win". As of 2007, over 31 million prizes were distributed each year, including cars, televisions, and store products. Customers determine if they have won prizes by unrolling the rim on their paper cups when they have finished their drink, revealing the result underneath. Prizes are not distributed randomly country-wide; each of the company's distribution regions has distinct prize-winning odds. The idea for the campaign began in 1985 when Roger Wilson of one of Tim Hortons' supplier of cups, Lily Cup company, approached Tim Hortons with a new idea to increase their sales. Wilson explained his company had created a new cup design that allowed a message to be printed under the rim; the cup type cost no more than the current one and could enable a promotion or contest. Recognizing the opportunity to promote coffee in the normally weak sales period in the spring, the Roll Up the Rim to Win campaign was first held in 1986 when the biggest prize was a snack box of Timbits. In 2008, over 88% of major prizes were redeemed. The contest is popular enough that Paul Kind invented the Rimroller (as seen on Dragons' Den), a device for rolling up the rim mechanically. The contest has seen several controversies including the theft of unrolled cups. In March 2006, two families were fighting over a Toyota RAV4 SUV prize of CA$32,000 value when their daughters found a winning "roll up the rim" coffee cup in a garbage bin of an elementary school in Saint-Jérôme, Quebec.
Sources: en.wikipedia.org
On February 13, Charles Ezell, acting director of the U.S. Office of Personnel Management, signed a directive instructing federal agencies to dismiss probationary employees—generally, federal workers who have held their jobs less than a year, or had been promoted into the excepted service during that time. Ezell told agencies to tell the fired employees that their performance was inadequate, and that they needed to cite no evidence. As of May 12, 2025, The New York Times tracked more than 58,000 confirmed cuts, more than 76,000 employee buyouts, and more than 149,000 other planned reductions; cuts total 12% of the 2.4 million civilian federal workers. As of July 14, 2025, CNN has tracked more than 128,000 workers laid off or targeted for layoffs. The administration took back some layoffs such as for bird flu and nuclear safety. In December 2025, the Office of Personnel Management launched the United States Tech Force, a two-year hiring initiative intended to recruit about 1,000 technologists (including AI engineers) for federal technology modernization projects across multiple agencies. Trump oversaw mass firings of federal workers at various agencies, many of them described as breaking with precedent or federal law and with the intent to replace them with workers more aligned with Trump's agenda.
=== Philanthropy and social responsibility === Since 2010, GlaxoSmithKline has several times ranked first among pharmaceutical companies on the Global Access to Medicines Index, which is funded by the Bill and Melinda Gates Foundation. In 2014, the Human Rights Campaign, an LGBT-rights advocacy group gave GSK a score of 100 per cent in its Corporate Equality Index. GSK has been active, with the World Health Organization (WHO), in the Global Alliance to Eliminate Lymphatic Filariasis (GAELF). Around 120 million people globally are believed to be infected with lymphatic filariasis. In 2012, the company endorsed the London Declaration on Neglected Tropical Diseases; it agreed to donate 400 million albendazole tablets to the WHO each year to fight soil-transmitted helminthiasis and to provide 600 million albendazole tablets every year for lymphatic filariasis until the disease is eradicated. As of 2014, over 5 billion treatments had been delivered, and 18 of 73 countries in which the disease is considered endemic had progressed to the surveillance stage. In 2009, the company said it would cut drug prices by 25 per cent in 50 of the poorest nations, release intellectual property rights for substances and processes relevant to neglected disease into a patent pool to encourage new drug development, and invest 20 per cent of profits from the least-developed countries in medical infrastructure for those countries.
==== Raman spectroscopy ==== Raman spectroscopy is one of the easiest methods to integrate into a heterogeneous operando experiment, as these reactions typically occur in the gas phase, so there is very low litter interference and good data can be obtained for the species on the catalytic surface. In order to use Raman, all that is required is to insert a small probe containing two optical fibers for excitation and detection. Pressure and heat complications are essentially negligible, due to the nature of the probe. Operando confocal Raman micro-spectroscopy has been applied to the study of fuel cell catalytic layers with flowing reactant streams and controlled temperature.
Nuclear magnetic resonance (NMR) is one of the most common methods to determine the physical and chemical properties of atoms by detecting the radio frequency absorbed and subsequent relaxation of nuclei in a magnetic field. This is one of the most commonly used characterization techniques and has applications in numerous fields. Primarily, the strong magnetic fields are generated by supercooling electromagnets, although there are spectrometers that do not require cryogens. In traditional superconducting solenoids, liquid helium is used to cool the inner coils because it has a boiling point of around 4 K at ambient pressure. Inexpensive metallic superconductors can be used for the coil wiring. So-called high-temperature superconducting compounds can be made to super conduct with the use of liquid nitrogen, which boils at around 77 K. Magnetic resonance imaging (MRI) is a complex application of NMR where the geometry of the resonances is deconvoluted and used to image objects by detecting the relaxation of protons that have been perturbed by a radio-frequency pulse in the strong magnetic field. This is most commonly used in health applications. Cryogenic electron microscopy (cryoEM) is a popular method in structural biology for elucidating the structures of proteins, cells, and other biological systems. Samples are plunge-frozen into a cryogen such as liquid ethane cooled by liquid nitrogen, and are then kept at liquid nitrogen temperature as they are inserted into an electron microscope for imaging. Electron microscopes are also themselves cooled by liquid nitrogen.
Sources: en.wikipedia.org
== Specific varieties == Tripolite is the variety found in Tripoli, Libya. Bann clay is the variety found in the Lower Bann valley in Northern Ireland. Moler (mo-clay) is the variety found in northwestern Denmark, especially on the islands of Fur and Mors. Freshwater-derived food grade diatomaceous earth is the type used in United States agriculture for grain storage, as feed supplement, and as an insecticide. It is produced uncalcinated, has a very fine particle size, and is very low in crystal silica (<2%). Salt-water-derived pool / beer / wine filter grade is not suitable for human consumption or effective as an insecticide. Usually calcinated before being sold to remove impurities and undesirable volatile contents, it is composed of larger particles than the freshwater version and has a high crystalline silica content (>60%).
The Nobel Assembly at the Karolinska Institute did consider awarding half to Fleming and one-quarter each to Florey and Chain, but in the end decided to divide it equally three ways. On 25 October 1945, it announced that Fleming, Florey and Chain equally shared the 1945 Nobel Prize in Physiology or Medicine "for the discovery of penicillin and its curative effect in various infectious diseases." When The New York Times announced that "Fleming and Two Co-Workers" had won the prize, Fulton demanded – and received – a correction in an editorial the next day. Dorothy Hodgkin received the 1964 Nobel Prize in Chemistry "for her determinations by X-ray techniques of the structures of important biochemical substances", most notably penicillin and vitamin B12. She became only the third woman to receive the Nobel Prize in Chemistry, after Marie Curie in 1911 and Irène Joliot-Curie in 1935.
This water insecurity has a direct impact on political stability. Outsiders hear most about the proxy war between factions supported by other countries, but according to the Yemeni newspaper Al-Thawra, 70% to 80% of conflicts in the country's rural regions are water-related. The country's Interior Ministry has estimated that across the country, water and land related disputes kill 4,000 people a year - more than terrorism. In Al-Jawf Governorate, a dispute over a well's placement has led to a blood feud that has continued for more than 30 years In 2007, Yemen's minister of Water and Natural Resources suggested that Sanaa, the capital city, might have to be evacuated if it runs out of water. Although the government was unable to move the capital in an orderly and peaceful way, the war and political crisis have rendered Sanaa and most of Yemen into a battleground that people have been forced to flee. Additional environmental catastrophes have battered Yemen as the war has progressed. In late 2015, two historic cyclones struck the country. The first of these, Cyclone Chapala, struck the island of Socotra before hitting the port of Mukalla on Yemen's south coast, where it caused catastrophic flash flooding. This storm, combined with the following Cyclone Megh, left enough moisture in the soil for locusts to breed. These locusts can fly 100 miles in a day and destroy any crop they encounter.
== Function == This gene is a member of the glycoprotein hormone beta chain family and encodes the beta subunit of luteinizing hormone (LH). Glycoprotein hormones are heterodimers consisting of a common alpha subunit and a unique beta subunit (this protein) which confers biological specificity. LH is expressed in the pituitary gland and promotes spermatogenesis and ovulation by stimulating the testes and ovaries to synthesize steroids.
== History == The 5-HT2c receptor agonist Fenfluramine (market names Pondimin, Ponderax and Adifax) was discovered in 1972 as a result of research performed to identify anorectic compounds lacking the effects of psycho-stimulants and sympathomimetic agents (such as amphetamines). Prior to the discovery of fenfluramine, amphetamines were the primary form of anorectic drugs available, however the side effects made them difficult to use. Fenfluramine's anorectic effect is achieved through an increase in serotonin levels, imparting a sensation of fullness, which leads to a lower intake of food. Fenfluramine was sold as a racemic mixture of two enantiomers, dexfenfluramine and levofenfluramine. In 1994, sales of the combination drug Fen-phen (fenfluramine and phentermine) increased dramatically, as this combination produced substantial and apparent synergistic effect in promoting weight loss. Subsequently, reports of severe side effects associated with heart valve abnormalities and an increased risk of pulmonary hypertension resulted in a decision to remove products containing fenfluramine from the U.S. market, and then from other markets around the world. Dexfenfluramine inhibits serotonin reuptake, stimulating the release of serotonin. In 1996, dexfenfluramine became the first long-term treatment anti-obesity medication approved in the US; adverse effects observed during clinical trials included dry mouth, diarrhea and drowsiness. In the mid-1990s the US FDA approved dexfenfluramine as a weight loss drug.
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 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.