This is a working overview of carcinogenicity, written for readers who want more than a one-paragraph summary but less than a textbook.
Reviewed 2026-08-01. Anything still debated is marked as such rather than presented as settled.
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.
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.
GW501516 binds and activates PPARδ, a nuclear receptor that influences transcription of genes involved in fatty acid oxidation and energy use. Activation shifts some metabolic pathways in preclinical models, which is why the compound has been studied for lipid disorders and exercise-related endpoints. The exact downstream effects in humans are incompletely mapped. PPARδ is expressed in many tissues, including skeletal muscle, liver, and adipose tissue, so broad activation may have varied consequences. Researchers continue to examine how selective or partial activation might alter the balance between benefits and risks.
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.
| Property | Value | Notes |
|---|---|---|
| Common name | Cardarine | Also called GW501516 and endurobol. |
| Chemical formula | C21H18F3NO3S2 | Molecular weight about 453.5 g/mol. |
| Appearance | White to off-white solid | Form depends on synthesis and purity. |
| Solubility | Soluble in DMSO and ethanol | Low solubility in water. |
| Typical storage | -20 °C, desiccated, protected from light | Common for research chemicals. |
Safety concerns emerged from long-term animal studies. In rodents given the compound for extended periods, researchers found an increased incidence of certain cancers, including liver and bladder tumors. These findings contributed to the discontinuation of clinical development. Whether similar risks apply to short-term or low-level exposure in humans is not established, and controlled human safety data are limited. The relevance of high-dose rodent carcinogenicity findings to human use remains a subject of debate.
Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.
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.
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.
=== Effect on metabolism === Horses with PSSM have elevated levels of muscle glycogen at rest. During exercise, glycogen levels are depleted faster than is seen in unaffected horses, and are reduced down to levels considered normal for a resting non-PSSM horse. This demonstrates that glycogen metabolism is actually normal in these animals. However, PSSM horses synthesize muscle glycogen at double the rate of a normal horse once exercise has ceased, which leads to elevated muscle glycogen. The exact mechanism of abnormal glucose metabolism has not yet been established, but it may have similarities to phosphofructokinase deficiency in humans. Quarter Horse-related breeds with PSSM show insulin sensitivity, which improves glucose uptake by cells, and these horses clear the blood of glucose more quickly after eating than unaffected horses. This provides easy access to glucose by the muscles, which can then use the substrate to produce glycogen. The GSY1 defect, which up-regulates the glycogen synthase enzyme, allows the muscles to use this glucose to rapidly produce glycogen for storage in the muscle. Surprisingly, increased insulin sensitivity is not seen in draft horse breeds. Dietary and exercise manipulation may be used to counteract these metabolic changes. Approximately 50% of horses that adhere to the dietary recommendations, and 90% of horses that adhere to both dietary and exercise recommendations, have few to no episodes of exertional rhabdomyolysis.
The argument that Belgians would believe it was butter if it was not cube shaped was disproportionate: it would "considerably exceed the requirements of the object in view" and labelling would protect consumers "just as effectively". In a 2003 case, Commission v Italy Italian law required that cocoa products that included other vegetable fats could not be labelled as "chocolate". It had to be "chocolate substitute". All Italian chocolate was made from cocoa butter alone, but British, Danish and Irish manufacturers used other vegetable fats. They claimed the law infringed article 34. The Court of Justice held that a low content of vegetable fat did not justify a "chocolate substitute" label. This was derogatory in the consumers' eyes. A 'neutral and objective statement' was enough to protect consumers. If member states place considerable obstacles on the use of a product, this can also infringe article 34. So, in a 2009 case, Commission v Italy, the Court of Justice held that an Italian law prohibiting motorcycles or mopeds pulling trailers infringed article 34. Again, the law applied neutrally to everyone, but disproportionately affected importers, because Italian companies did not make trailers. This was not a product requirement, but the Court reasoned that the prohibition would deter people from buying it: it would have "a considerable influence on the behaviour of consumers" that "affects the access of that product to the market". It would require justification under article 36, or as a mandatory requirement.
Withdraw from the Geneva Consensus Declaration Rejoin the Union of South American Nations and the Community of Latin American and Caribbean States Restore recognition of Nicolás Maduro as president of Venezuela and reopen the Brazilian embassy in Caracas Restore goals of reduction of greenhouse gas emissions according to the Paris Agreement Restore monitoring against deforestation of the Amazon rainforest and illegal mining Relaunch the Growth Acceleration Programme Relaunch the Minha Casa, Minha Vida programme
Sources: en.wikipedia.org
== Discovery == In 1839, the German anatomist Hermann Friedrich Stannius discovered a pair of novel structures inside the kidneys of sturgeon and bony fishes. He believed that they were a kind of adrenal gland (found in mammals) in these fishes. In 1896, the French physiologist A. Petit demonstrated that removal of one of the structures led to degeneration of the other. He suggested that these structures were endocrine organs. In 1908, the Italian zoologist Ercole Giacomini was the first to describe that these structures were present only in fishes which lack a parathyroid gland. He distinguished and named them "posterior interrenal" from the anterior portion of the kidney, which he named "anterior interrenal". A French Physiologist M. Fontaine reported that the corpuscles were responsible for controlling calcium level in the blood. In 1971 Peter K.T. Pang of Yale University showed in the male killifish, Fundulus heteroclitus, that the corpuscles control calcium metabolism. He found that removal of the corpuscle led to development of kidney stone and increase in serum calcium level. By the mid 1970s, it was confirmed that the corpuscles secrete a factor that can reduce calcium level, similar to calcitonin but completely different. and Pang gave the prospective name "hypocalcin". The chemical compound was isolated in 1986 from sockeye salmon (Oncorhynchus nerka), and since it was from a teleost, it was called "teleocalcin". A better isolation was reported in 1988 from different species, including European eel, tilapia, goldfish, and carp.
The share of the world's lead production by the Eastern Bloc increased from 10% to 30%, from 1950 to 1990, with the Soviet Union being the world's largest producer during the mid-1970s and the 1980s, and China starting major lead production in the late 20th century. Unlike the European communist countries, China was largely unindustrialized by the mid-20th century; in 2004, China surpassed Australia as the largest producer of lead. As was the case during European industrialization, lead has had a negative effect on health in China.
== Potential uses == Lobeline has been sold, in tablet form, for use as a smoking cessation aid, but scientific research has not provided supporting evidence for this use. Lobeline has also been studied for the treatment of other drug addictions such as addiction to amphetamines, cocaine, or alcohol; however, there is limited clinical evidence of any efficacy.
== Research == As of August 2025, KNX-100 is in phase 2 clinical trials for treatment of agitation and aggression in dementia, phase 1 trials for opioid-related disorders and substance-related disorders, and the preclinical research stage of development for behavioral disorders. Phase 1 trials were first planned for 2019. Several clinical trials of KNX-100 have been registered with details provided. In addition to the preceding indications, there is also interest in KNX-100 for other potential applications like treatment of social anxiety, other types of addiction besides substance addiction like gambling, and pain, among others. Besides KNX-100, Kinoxis Therapeutics also has selective oxytocin receptor partial agonists like its KNX-200 series and oxytocin receptor positive allosteric modulators like its KNX-300/400 series in its developmental pipeline.
Sources: en.wikipedia.org
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.
It activates PPARδ, a nuclear receptor that influences gene expression related to lipid and energy metabolism. Animal studies show changes in endurance and lipid levels. Human effects and risks are not well established.
No, cardarine is not a steroid. It belongs to a different chemical class, the PPARδ agonists. It is also not a selective androgen receptor modulator.
Anti-doping and clinical laboratories commonly use liquid chromatography-tandem mass spectrometry. The method can identify GW501516 and its metabolites in urine or blood. Detection depends on sample timing and the amount present.