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Identity And Pharmacological Classification — What the Evidence Shows

By Editorial Desk · published 2026-07-09 · last reviewed 2026-08-01 · Info

Research chemical is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.

Last reviewed on 2026-08-01. Where a claim depends on a specific study, the study is described rather than over-claimed.

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.

Regulation and Analytical Detection

Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.

Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.

Cardarine at a glance

PropertyValueNotes
Chemical classPPARδ agonistNot an anabolic steroid.
Common synonymsGW501516, GW-1516Cardarine is an informal name.
AppearanceWhite to off-white powderTypical for research-grade solid.
Solubility classPoorly soluble in water; soluble in some organic solventsSuch as DMSO or ethanol in laboratory settings.
Typical storage temperatureCool, dry, protected from lightSpecific conditions vary by supplier and form.

Background and Regulatory History

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.

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Cardarine as Investigational PPARδ Agonist

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.

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.

Regulation and Detection

Cardarine has no approved therapeutic indication and is not marketed as a medicine. The World Anti-Doping Agency lists GW501516 as a prohibited substance at all times, covering both in-competition and out-of-competition periods. National laws vary: some countries treat it as an unapproved drug subject to import controls, while others have specific restrictions on sale for human consumption. It is often sold as a research chemical, a label that does not imply safety or legality. Enforcement actions have targeted online vendors and shipments.

Anti-doping laboratories identify GW501516 and related metabolites using liquid chromatography coupled with tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be analyzed. The method targets the parent compound and phase I and phase II metabolites, which extend the detection window. Because the substance is prohibited at all times, athletes can be tested outside competition. Detection limits and windows depend on the assay, sample type, and individual metabolism.

Cardarine is frequently described as a fat-burning or endurance-enhancing supplement, but these claims exceed the available evidence. The compound is not a hormone, steroid, or selective androgen receptor modulator. Research articles discuss it as a tool compound for studying PPARδ biology, while anti-doping literature focuses on its abuse and detection. Quality of unapproved products is uncertain, and independent analyses have found impurities or incorrect labeling. Open questions include whether human cancer risk resembles that seen in rodents and how often non-athletes use the substance.

Further detail

==== Ireland ==== In Ireland, new regulations came into effect on 1 August 2010 concerning codeine, due to worries about the overuse of the drug. Codeine remains a semi non-prescriptive, over-the-counter drug up to a limit of 12.8 mg per pill, but codeine products must be out of the view of the public to facilitate the legislative requirement that these products "are not accessible to the public for self-selection". In practice, this means customers must ask pharmacists for the product containing codeine in name, and the pharmacist makes a judgement whether it is suitable for the patient to be using codeine, and that patients are fully advised of the correct use of these products. Products containing more than 12.8 mg codeine are available on prescription only.

== History == B-cell activating factor is a naturally occurring protein that was discovered by researchers from National Jewish Health (previously the National Jewish Medical and Research Center) and the University of Colorado, who jointly published a paper detailing their findings in May 1999 and named the protein TALL-1. The same protein was named BAFF in another paper published in June 1999, and in a paper published in July of that year, Human Genome Sciences (HGS) referred to it as BLyS (short for B lymphocyte stimulator). Six years later, research showing the key role of BLyS in B cell differentiation, survival, and activation was published. In October 2000, HGS and Cambridge Antibody Technology (CAT) agreed to co-develop monoclonal antibodies targeted at BLyS. Under this agreement, CAT would identify antibodies and HGS would select appropriate ones to take into clinical trials. In 2003, CAT researchers reported that, by using phage display technology, they had elicited an array of more than 1,000 distinct antibodies, half of which inhibited binding of BLyS to its receptor. Later that year, one of these antibodies was isolated and characterized. It was named LymphoStat-B and subsequently called belimumab. In August 2006, HGS and GlaxoSmithKline (GSK) entered into a co-development and commercialization agreement under which HGS would conduct Phase III trials for belimumab with assistance from GSK. The companies would share equally in Phase III/IV development costs, sales and marketing expenses, and profits of any product commercialized under the agreement.

When allowed to react with superacids, sulfuric acid can act as a base and can be protonated, forming the [H3SO4]+ ion. Salts of [H3SO4]+ have been prepared (e.g. trihydroxyoxosulfonium hexafluoroantimonate(V) [H3SO4]+[SbF6]−) using the following reaction in liquid HF:

Sources: en.wikipedia.org

Supporting material

A 100-gram (3+1⁄2-ounce) reference serving of uncooked spelt provides 1,400 kilojoules (340 kilocalories) of food energy and is a rich source (20% or more of the Daily Value) of protein, dietary fiber, several B vitamins, and numerous dietary minerals (table). Highest nutrient contents include manganese (143% DV), phosphorus (57% DV), and niacin (46% DV). Spelt contains about 70% total carbohydrates, including 11% as dietary fibre, and is low in fat (table). Spelt contains gluten, and is therefore suitable for baking, but this component makes it unsuitable for people with gluten-related disorders, such as celiac disease. In comparison to hard red winter wheat, spelt has a more soluble protein matrix characterized by a higher gliadin:glutenin ratio.

== Research == Her achievements include the discovery of adaptins, which are specific proteins that manage cell-trafficking to ensure the correct cell cargo is transported to the right location. She also discovered different combinations of adapting, when together with clathrin, form a coat around vesicles that bud from intracellular membranes and act as transporters for protein packages to be distributed in the cell. She also developed the technique "knock sideways," which inactivates proteins in seconds. After finishing her postdoc, she was able to start her own lab. Her main focus was to learn more about the AP protein in depth. She had to also work with DNA because in order to characterize the complexes thoroughly, she needed to clone the subunits. Robinson and her lab managed to find another AP complex, AP-3, which interacts with lysosomal membrane proteins such as LAMP1. AP-3 also interacts with tyrosinase, which is a key enzyme in melanin biosynthesis, so AP-3 is important for tyrosinase trafficking to premelanosomes. As of 2016 Robinson has a lab at Cambridge Institute for Medical Research. She specifically works with coated vesicles. The best-characterized coated vesicles are the clathrin-coated vesicles (CCVs). The coats on CCVs are primarily of clathrin, adaptor protein (AP) complexes, and alternative adaptors. Her working hypothesis is that for each trafficking pathway, there are a number of different adaptors, each of which is recruited independently onto the appropriate membrane.

== Early life == Dorothy Mary Crowfoot was born in Cairo, Egypt, the oldest of the four daughters whose parents worked in North Africa and the middle East in the colonial administration and later as archaeologists. Dorothy came from a distinguished family of archaeologists. Her parents were John Winter Crowfoot (1873–1959), working for the country's Ministry of Education, and his wife Grace Mary (née Hood) (1877–1957), known to friends and family as Molly. The family lived in Cairo during the winter months, returning to England each year to avoid the hotter part of the season in Egypt. In 1914, Hodgkin's mother left her (age 4) and her two younger sisters Joan (age 2) and Elisabeth (age 7 months) with their Crowfoot grandparents near Worthing, and returned to her husband in Egypt. They spent much of their childhood apart from their parents, yet they were supportive from afar. Her mother would encourage Dorothy to pursue the interest in crystals first displayed at the age of 10. In 1923, Dorothy and her sister would study pebbles that they had found in nearby streams using portable mineral analysis kit. Their parents then moved south to Sudan where, until 1926, her father was in charge of education and archaeology. Her mother's four brothers were killed in World War I and as a result she became an ardent supporter of the new League of Nations. In 1921 Hodgkin's father entered her in the Sir John Leman Grammar School in Beccles, England, where she was one of two girls allowed to study chemistry.

Sources: en.wikipedia.org

Notes from published material

Female cannabis plants contain at least 113 cannabinoids, including cannabidiol (CBD), thought to be the major anticonvulsant that helps people with multiple sclerosis, and cannabichromene (CBC), an anti-inflammatory which may contribute to the pain-killing effect of cannabis.

Sales of the top 20 blockbuster drugs are reported in Table 6. The APIs of 12 of them are "small" (LMW) molecules. Averaging a MW of 477, they have quite complex structures. They typically show three cyclic moieties. 10 of them exhibit at least one N-heterocyclic moiety. Five of the top 10, up from none in 2005, are biopharmaceuticals. The largest-selling non-proprietary drugs are paracetamol, omeprazole, ethinylestradiol, amoxicillin, pyridoxine, and ascorbic acid. The innovator pharma companies mainly require custom manufacturing services for their proprietary drug substances. The demand is driven primarily by the number of new drug launches, the volume requirements and the industry's "make or buy" strategy. A summary of the pro's and con's for outsourcing from the pharma industry's perspective is given in Table 7. As extended studies at the Stern Business School of the New York City University have shown, financial considerations clearly favor the "buy" option.

== Regenerated skin: discovery and clinical use == A process for inducing regeneration in skin was invented by Ioannis V. Yannas (then an assistant professor in the Fibers and Polymers Division, Department of Mechanical Engineering, at Massachusetts Institute of Technology) and John F. Burke (then chief of staff at Shriners Burns Institute in Boston, Massachusetts). Their initial objective was to discover a wound cover that would protect severe skin wounds from infection by accelerating wound closure. Several kinds of grafts made of synthetic and natural polymers were prepared and tested in a guinea pig animal model. By the late 1970s it was evident that the original objective was not reached. Instead, these experimental grafts typically did not affect the speed of wound closure. In one case, however, a particular type of collagen graft led to significant delay of wound closure. Careful study of histology samples revealed that grafts that delayed wound closure induced the synthesis of new dermis de novo at the injury site, instead of forming scar, which is the normal outcome of the spontaneous wound healing response. This was the first demonstration of regeneration of a tissue (dermis) that does not regenerate by itself in the adult mammal. After the initial discovery, further research led to the composition and fabrication of grafts that were evaluated in clinical trials.

Nevertheless, benzodiazepines are still prescribed for long-term treatment of anxiety disorders, although specific antidepressants and psychological therapies are recommended as the first-line treatment options with the anticonvulsant drug pregabalin indicated as a second- or third-line treatment and suitable for long-term use. NICE stated that long-term use of benzodiazepines for panic disorder with or without agoraphobia is an unlicensed indication, does not have long-term efficacy, and is, therefore, not recommended by clinical guidelines. Psychological therapies such as cognitive behavioural therapy are recommended as a first-line therapy for panic disorder; benzodiazepine use has been found to interfere with therapeutic gains from these therapies.

Sources: en.wikipedia.org

Frequently asked questions

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.

Is cardarine a steroid?

No, cardarine is not a steroid. It is classified as a PPARδ agonist. Its structure and receptor target differ from anabolic steroids.

Has cardarine been approved for human use?

No regulatory agency has approved cardarine as a medicine. It was investigated in early research but development was discontinued. It is not available as a prescription drug.

Is cardarine legal to buy?

Legal status varies by country, but cardarine is not approved as a medicine in major jurisdictions. It is often sold as a research chemical, a category that may not be lawful for human use. Buyers should check local laws and product labels carefully.

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