If you have been reading about regulatory status and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.
Updated 2026-08-01. Numbers and descriptions here follow the published literature rather than marketing material.
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.
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.
GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.
Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.
Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.
| Property | Value | Notes |
|---|---|---|
| CAS Registry Number | 317318-70-0 | Unique identifier for the compound. |
| Chemical class | PPARδ agonist | Synthetic ligand for peroxisome proliferator-activated receptor delta. |
| Appearance | White to off-white solid | Typical form of research-grade material. |
| Solubility | Soluble in DMSO and ethanol | Poorly soluble in water. |
| Typical storage | -20°C | Recommended for long-term storage of stock solutions. |
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.
Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.
Cardarine can be detected in biological samples and product materials using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The method separates compounds by chromatography and identifies them by mass-to-charge transitions, allowing low-level detection in urine or blood. Sample preparation often involves enzymatic hydrolysis, solid-phase extraction, or protein precipitation. Certified reference materials and isotope-labeled internal standards improve quantification. Detection windows depend on metabolism, matrix, and assay sensitivity, so no single universal window applies.
Regulatory treatment of cardarine differs by context and jurisdiction. In competitive sport, the World Anti-Doping Agency lists PPARδ agonists, including GW501516, as prohibited at all times. Outside sport, it lacks approval as a prescription medicine in major drug markets, and products sold for human consumption may be treated as unapproved drugs. Some countries also restrict importation or sale through general consumer protection and medicines laws. These classifications affect availability, testing, and legal risk without establishing therapeutic value.
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.
Christopher Richard Stein (born 4 January 1947) is an English celebrity chef, restaurateur, writer and television presenter. Along with business partner and first wife Jill Stein, he runs the Stein hotel and restaurant business in the UK. The business has a number of renowned restaurants, shops and hotels in Padstow along with other restaurants in Winchester and Barnes. He is the head chef and a co-owner of the Rick Stein at Bannisters restaurants in Mollymook and Port Stephens in Australia, with his second wife, Sarah. He writes cookery books and has presented numerous cookery series for the BBC.
Macleod provided experimental facilities and the assistance of one of his students, Charles Best. Banting and Best, with the assistance of biochemist James Collip, began the production of insulin by this means. As the experiments proceeded, the required quantities could no longer be obtained by performing surgery on living dogs. In November 1921, Banting hit upon the idea of obtaining insulin from the fetal pancreas. He removed the pancreases from fetal calves at a William Davies slaughterhouse and found the extracts to be just as potent as those extracted from the dog pancreases. By December 1921, he had also succeeded in extracting insulin from the adult pancreas. Pork and beef would remain the primary commercial sources of insulin until they were replaced by genetically engineered bacteria in the late 20th century. On January 11, 1922, the first ever injection of insulin was given to 14-year-old Canadian Leonard Thompson at Toronto General Hospital. In spring of 1922, Banting established a private practice in Toronto and began to treat diabetic patients. His first American patient was Elizabeth Hughes Gossett, daughter of U.S. Secretary of State Charles Evans Hughes. Banting and Macleod were jointly awarded the 1923 Nobel Prize in Physiology or Medicine. Banting split his half of the Prize money with Best, and Macleod split the other half of the Prize money with James Collip.
== In nature == Numerous biomolecules exhibit the ability to dissolve certain metal cations. Thus, proteins, polysaccharides, and polynucleic acids are excellent polydentate ligands for many metal ions. Organic compounds such as the amino acids glutamic acid and histidine, organic diacids such as malate, and polypeptides such as phytochelatin are also typical chelators. In addition to these adventitious chelators, several biomolecules are specifically produced to bind certain metals (see next section). Virtually all metalloenzymes feature metals that are chelated, usually to peptides or cofactors and prosthetic groups. Such chelating agents include the porphyrin rings in hemoglobin and chlorophyll. Many microbial species produce water-soluble pigments that serve as chelating agents, termed siderophores. For example, species of Pseudomonas are known to secrete pyochelin and pyoverdine that bind iron. Enterobactin, produced by E. coli, is the strongest chelating agent known. The marine mussels use metal chelation, especially Fe3+ chelation with the Dopa residues in mussel foot protein-1 to improve the strength of the threads that they use to secure themselves to surfaces. In earth science, chemical weathering is attributed to organic chelating agents (e.g., peptides and sugars) that extract metal ions from minerals and rocks. Most metal complexes in the environment and in nature are bound in some form of chelate ring (e.g., with a humic acid or a protein).
Sources: en.wikipedia.org
=== Theobromine and oxalate === Chocolate may be a factor for heartburn in some people because one of its constituents, theobromine, may affect the esophageal sphincter muscle in a way that permits stomach acids to enter the esophagus. Theobromine poisoning is an overdosage reaction to the bitter alkaloid, which happens more frequently in domestic animals than humans. However, daily intake of 50–100 g cocoa (0.8–1.5 g theobromine) by humans has been associated with sweating, trembling, and severe headache. Chocolate and cocoa contain moderate to high amounts of oxalate, which may increase the risk of kidney stones.
The acyl carrier protein (ACP), aryl carrier protein (ArCP), and the peptidyl carrier protein (PCP) are a family of protein cofactors that participate in fatty acid (acyl), polyketide (acyl and aryl), and nonribosomal peptide (peptidyl) biosynthesis. The growing molecule is bound to the A(r)/PCP via a thioester derived from the distal thiol of a 4'-phosphopantetheine (PPant) moiety. A(r)/PCPs are found in bacteria and eukaryotes (including humans) alike. The E. coli version (EcacpP) is the best studied. In E. coli, the ACP is one of the most abundant cytosolic proteins at 0.25% of the total soluble protein (by molecule count). It is small, very acidic, and very soluble. EcacpP works as a cofactor in the synthesis of both long and short chain fatty acids in the bacterium. It interacts with fatty acid synthase proteins that "flips" the growing fatty acid chain out of the ACP's internal cavity and modifies it. This kind of setup where the ACP exists as a free-floating protein is called Type II. An alternative is the Type I system, where a large protein contains several synthase domains as well as its own ACP domain. The ACP domain is pass around by the synthase domains to build a molecule. Polyketide synthases and nonribosomal peptide synthetases interact with their carrier proteins in a similar way. There is a similar distinction in how they are organized into type I and type II. Plant ACPs participate in the biosynthesis of fatty acids, exploited by humans in the form of vegetable oils.
=== Allergy diagnosis === Basophils are easily isolated from venous blood and present good "indicator cells" of an IgE-mediated allergic response based on the upregulation of activation markers such as CD63 and/or CD203c upon suspect allergen stimulation. Therefore, the BAT serves to confirm IgE-mediated allergy following uncertain results from classical testing based on anamnesis, skin testing or specific IgE results. More recently, BAT has also been used for the monitoring of successful allergen immunotherapy (desensitization) to differentiate short-term desensitization versus sustained unresponsiveness to the allergen.
Sources: en.wikipedia.org
Cardarine is a common name for GW501516, a synthetic PPARδ agonist developed for research. It has not been approved as a medication in any country. It is classified as an unapproved drug and a prohibited substance in sport.
No. Cardarine is not an anabolic steroid; it belongs to a different chemical class that targets PPARδ. Steroids act primarily through androgen receptors, while cardarine acts through a nuclear receptor involved in metabolism.
Some rodent studies reported increased endurance and changes in fat metabolism after cardarine exposure. Long-term studies in animals also raised concerns about cancer in certain tissues. Human trial data are limited, so these findings cannot be directly translated to people.
It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.