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Cardarine Identity And Mechanism — What the Evidence Shows

By Editorial Desk · published 2026-06-17 · last reviewed 2026-07-19 · Wiki

Cardarine raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.

Reviewed 2026-07-19. Anything still debated is marked as such rather than presented as settled.

Cardarine Identity and Mechanism

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.

Identity and Pharmacological Classification

PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.

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.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineAlso called GW501516 and endurobol.
Chemical formulaC21H18F3NO3S2Molecular weight about 453.5 g/mol.
AppearanceWhite to off-white solidForm depends on synthesis and purity.
SolubilitySoluble in DMSO and ethanolLow solubility in water.
Typical storage-20 °C, desiccated, protected from lightCommon for research chemicals.

Identity and Regulatory Status

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.

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Background and Research Context

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.

In laboratory settings, cardarine is studied as a tool compound for probing PPARδ biology. Published experiments often use cell cultures, rodent models, or isolated tissues. Some investigations focus on metabolic effects, while others assess potential risks such as carcinogenicity observed in long-term animal studies. Because human trials are sparse, most knowledge comes from preclinical work and adverse event reports. Scientific literature frequently notes the gap between animal findings and human outcomes. The compound is not a dietary supplement and is not intended for human consumption.

Reference notes

Biochemistry is the study of the chemical substances and vital processes occurring in live organisms. Biochemists focus heavily on the role, function, and structure of bio-molecules. The study of the chemistry behind biological processes and the synthesis of biologically active molecules are applications of biochemistry. Biochemistry studies life at the atomic and molecular level. Genetics is the study of the effect of genetic differences in organisms. This can often be inferred by the absence of a normal component (e.g. one gene). The study of "mutants" – organisms that lack one or more functional components with respect to the so-called "wild type" or normal phenotype. Genetic interactions (epistasis) can often confound simple interpretations of such "knockout" studies. Molecular biology is the study of molecular underpinnings of the biological phenomena, focusing on molecular synthesis, modification, mechanisms and interactions. The central dogma of molecular biology, where genetic material is transcribed into RNA and then translated into protein, despite being oversimplified, still provides a good starting point for understanding the field. This concept has been revised in light of emerging novel roles for RNA. Chemical biology seeks to develop new tools based on small molecules that allow minimal perturbation of biological systems while providing detailed information about their function.

== Production == Natural menthol is obtained by freezing peppermint oil. The resultant crystals of menthol are then separated by filtration. Total world production of menthol in 1998 was 12,000 tonnes of which 2,500 tonnes was synthetic. In 2005, the annual production of synthetic menthol was almost double. Prices are in the $10–20/kg range with peaks in the $40/kg region but have reached as high as $100/kg. In 1985, it was estimated that China produced most of the world's supply of natural menthol, although it appears that India has pushed China into second place. Menthol is manufactured as a single enantiomer (94% e.e.) on the scale of 3,000 tonnes per year by Takasago International Corporation. The process involves an asymmetric synthesis developed by a team led by Ryōji Noyori, who won the 2001 Nobel Prize for Chemistry in recognition of his work on this process:

=== Neurotoxicity === Selegiline has been reported to protect against the damage caused by the potent dopaminergic and/or noradrenergic neurotoxins 6-hydroxydopamine (6-OHDA), N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP-4), and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in animals. Conversely, selegiline is ineffective in protecting against the serotonergic and noradrenergic neurotoxin 5,7-dihydroxytryptamine (5,7-DHT). Selegiline has also been reported to protect against methylenedioxymethamphetamine (MDMA)-induced serotonergic neurotoxicity in rodents. The serotonergic neurotoxicity of MDMA appears to be dependent on release of dopamine and its subsequent metabolism by MAO-B within serotonergic neurons into hydroxyl radicals, which is blocked by MAO-B inhibition. Likewise, selegiline prevented the serotonergic neurotoxicity of a combination of methylenedioxyaminoindane (MDAI) and dextroamphetamine. Conversely, selegiline failed to reduce the serotonergic neurotoxicity caused by fenfluramine and either did not affect or potentiated the serotonergic neurotoxicity caused by para-chloroamphetamine (PCA). In addition, findings are mixed and conflicting on whether selegiline prevents amphetamine- and methamphetamine-induced dopaminergic neurotoxicity in rodents. Although MAO-B-selective doses of selegiline protect against MDMA-induced serotonergic neurotoxicity in rodents, combination of amphetamines like MDMA with MAOIs, including selegiline, can produce serious complications, including serotonin syndrome, hypertensive crisis, and death.

=== August === 1 August – A study in Nature finds that based on current policies, there is a 45% risk of at least one major tipping point by 2300, even if global warming is brought back to below 1.5 °C. The risk is "strongly accelerated" for peak warming above 2.0 °C. The Atlantic Meridional Overturning Current (AMOC) is identified as being at the most urgent risk of collapse – possibly occurring as early as 2040 – followed by the Amazon rainforest in the 2070s. 5 August A study indicates vegetarian and vegan dog diets are healthier than both conventional meat and raw meat diets according to indicators like numbers of veterinary visits and reported veterinary assessment of being unwell, consistent with all related studies published to date. An analysis suggests hydraulic lifts may have been used to build ancient large Egyptian pyramids. 7 August – Scientists in Australia publish a new 400-year temperature reconstruction for the Coral Sea, showing that recent ocean heat has led to mass bleaching on the Great Barrier Reef. 8 August – A study on the terraforming of Mars suggests that releasing metal nanorods into the planet's atmosphere could warm it by 30 K, and would be far more efficient than trying to do so with greenhouse gases. 12 August Liquid water is confirmed to be present at depths of 10 to 20 km (6.2 to 12.4 mi) below the surface of Mars, based on a new analysis of data from NASA's InSight lander. An Earth-sized, ultra-short period exoplanet called TOI-6255b is found to be undergoing extreme tidal distortion, caused by the close proximity of its parent star.

Sources: en.wikipedia.org

Notes from published material

However, up to 10% of cases are due to a new mutation. Expansion of CAG repeats (known as a trinucleotide repeat expansion) in the gene coding for the huntingtin protein results in an abnormal mutant protein (mHTT), which gradually damages brain cells through a number of possible mechanisms. The mutant protein is dominant, so having one parent who is a carrier of the trait is sufficient to trigger the disease in their children. Diagnosis is by genetic testing, which can be carried out at any time, regardless of whether or not symptoms are present. This fact raises several ethical debates: the age at which an individual is considered mature enough to choose testing; whether parents have the right to have their children tested; and managing confidentiality and disclosure of test results. No cure for HD is known, and full-time care is required in the later stages. Treatments can relieve some symptoms and possibly improve quality of life. The best evidence for treatment of the movement problems is with tetrabenazine. HD affects about 4 to 15 in 100,000 people of European descent. It is rare among the Finnish and the Japanese, while the incidence in Africa is unknown. The disease affects males and females equally. Complications such as pneumonia, heart disease, and physical injury from falls reduce life expectancy; fatal aspiration pneumonia is commonly cited as the ultimate cause of death for those with the condition. Suicide is the cause of death in about 9% of cases. Death typically occurs 15–20 years from when the disease was first detected.

Tanabe Young Investigator Award from the American College of Clinical Pharmacology (2014) Division for Drug Metabolism Early Career Achievement Award by the American Society for Pharmacology and Experimental Therapeutics (ASPET) (2015) The International Society for the Study of Xenobiotics (ISSX) North American New Investigator Award in Honor of James R. Gillette (2017) The Daily Record Leading Women Award (2017) Leon I. Goldberg Young Investigator Award from the American Society for Clinical Pharmacology and Therapeutics (2017) John J. Abel Award in Pharmacology from ASPET (2019)

== List of main islands == While in Russian sources the islands are mentioned for the first time in 1646, the earliest detailed information about them was provided by the explorer Vladimir Atlasov in 1697. In the 18th and early 19th centuries, the Kuril Islands were explored by: Danila Antsiferov, I. Kozyrevsky, Ivan Yevreinov, Fyodor Luzhin, Martin Spanberg, Adam Johann von Krusenstern, Vasily Golovnin, and Henry James Snow.

Sources: en.wikipedia.org

Further detail

A meta-analysis conducted in 2007 and updated in 2020 by the international Cochrane Collaboration, which reviewed numerous randomized controlled trials, found that treatment with glargine and detemir insulins resulted in fewer cases of hypoglycemia compared to NPH insulin. Additionally, treatment with detemir was associated with a reduction in the frequency of severe hypoglycemia. However, the review acknowledged limitations, such as the use of low glucose and Hemoglobin A1c targets, which could affect the generalizability of these findings to routine clinical practice. In 2007, a report from Germany's Institute for Quality and Cost Effectiveness in the Health Care Sector (IQWiG) concluded that there was insufficient evidence to support the superiority of short-acting insulin analogues over synthetic human insulin for the treatment of adult patients with type 1 diabetes. Many of the studies reviewed were criticized for being too small to provide statistically reliable results, and notably, none were blinded.

Fatty acid metabolism consists of various metabolic processes involving or closely related to fatty acids, a family of molecules classified within the lipid macronutrient category. These processes can mainly be divided into (1) catabolic processes that generate energy and (2) anabolic processes where they serve as building blocks for other compounds. In catabolism, fatty acids are metabolized to produce energy, mainly in the form of adenosine triphosphate (ATP). When compared to other macronutrient classes (carbohydrates and protein), fatty acids yield the most ATP on an energy per gram basis, when they are completely oxidized to CO2 and water by beta oxidation and the citric acid cycle. Fatty acids (mainly in the form of triglycerides) are therefore the foremost storage form of fuel in most animals, and to a lesser extent in plants. In anabolism, intact fatty acids are important precursors to triglycerides, phospholipids, second messengers, hormones and ketone bodies. For example, phospholipids form the phospholipid bilayers out of which all the membranes of the cell are constructed from fatty acids. Phospholipids comprise the plasma membrane and other membranes that enclose all the organelles within the cells, such as the nucleus, the mitochondria, endoplasmic reticulum, and the Golgi apparatus. In another type of anabolism, fatty acids are modified to form other compounds such as second messengers and local hormones. The prostaglandins made from arachidonic acid stored in the cell membrane are probably the best-known of these local hormones.

Bernoulli's principle predicts that the decrease in pressure is associated with an increase in speed; in other words, as the air passes over the paper, it speeds up and moves faster than it was moving when it left the demonstrator's mouth. But this is not apparent from the demonstration.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

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.

How does cardarine work?

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.

Is cardarine a steroid?

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.

What is cardarine also known as?

Cardarine is commonly known as GW501516 or GW-1516. These names refer to the same synthetic compound. It is not a brand-name approved medicine.

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