If you have been reading about nuclear receptor 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.
Last reviewed on 2025-09-11. Where a claim depends on a specific study, the study is described rather than over-claimed.
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.
Cardarine is a common name for GW501516, a synthetic compound first described in the 1990s as a selective agonist of the peroxisome proliferator-activated receptor delta. It was studied in preclinical models for metabolic and cardiovascular conditions, but it has not been approved as a medicine in the United States, Europe, or other major jurisdictions. Retail products labeled as cardarine are generally research chemicals or supplements, not pharmaceutical formulations. Because human safety and efficacy data remain limited, regulatory agencies treat it as an unapproved substance rather than a therapeutic product.
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.
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.
| 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 |
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.
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.
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.
== Chemistry == LAAM, or levomethadyl acetate, is the levo isomer of acetylmethadol, or α-methadyl acetate. The dextro isomer, d-alphacetylmethadol (d-α-acetylmethadol), is more potent but shorter acting. The levo isomer is also less toxic with an LD50 in mice of 110 mg/kg s.c. and 172.8 mg/kg orally as opposed to LD50s of 61 mg/kg s.c. and 118.3 mg/kg orally for dl-α-methadyl acetate. It has a melting point of 215 °C and a molecular weight of 353.50. β-methadyl acetate also exists, but is more toxic and less active than α-methadyl acetate and has no current medical use.
== Use == The vaccine vial monitor consists of a temperature sensitive square within a circle. If the monitor is exposed to heat it changes color with time and with increasing speed in hotter conditions. If the square becomes the same color as the circle or becomes darker than the circle, then the vaccine contained in the vial is heat-damaged and the vial should be discarded. A vaccine should only be used if the VVM has the right color and the expiration date has not passed. Studies have shown that health workers without proper training sometimes do not understand what a VVM is or how it works. A 2007 study in urban areas of Valsad in India showed that vaccine administrators were unaware of the purpose of the monitors.
Bring ye unto him milk and fat with meat; this is the right food for the dog. By Medieval times, dogs were more seen as pets rather than just companions and workers which affected their quality of the diet to include "Besides being fed bran bread, the dogs would also get some of the meat from the hunt. If a dog was sick, he would get better food, such as goat's milk, bean broth, chopped meat, or buttered eggs." In France, the word pâtée began to appear in the 18th century and referred to a paste originally given to poultry. In 1756, a dictionary indicates it was made of a mixture of bread crumbs and little pieces of meat given to pets. In 1781, an encyclopedia mentioned an earlier practice of removing the liver, heart, and blood of a downed stag and mixing it with milk, cheese, and bread, and then giving it to dogs. In 1844, the French writer, Nicolas Boyard, warned against even giving tallow graves (the dregs of the tallow pot) to dogs, though the English favored them (see below), and suggested a meat-flavored soup:
== Provitamin A activity == Plant carotenoids are the primary dietary source of provitamin A worldwide, with β-carotene as the best-known provitamin A carotenoid. Others include α-carotene and β-cryptoxanthin. Carotenoid absorption is restricted to the duodenum of the small intestine. One molecule of β-carotene can be cleaved by the intestinal enzyme β,β-carotene 15,15'-monooxygenase into two molecules of vitamin A.
Sources: en.wikipedia.org
== Early business career == Bello entered the Amos Tuck School at Dartmouth College, graduating with an MBA in 1974. While at Tuck he was named an Edward Tuck Scholar. After Tuck, his first business position was in brand management at General Foods, where he worked on Sanka and Maxwell House coffee brands. After an interim experience in athletic footwear as product director for Keds Brand footwear, he moved on to a strategic planning and marketing functions in the Pepsi Cola Division of PepsiCo where he worked on Mountain Dew and the Pepsi Challenge.
Carbohydrates are the main source of energy in organisms for metabolism. They are an important source of fuel in exercise. A study conducted by the Institute of Food, Nutrition, and Human Health at Massey University investigated the effect of consuming a carbohydrate and electrolyte solution on muscle glycogen use and running capacity on subjects that were on a high carbohydrate diet. The group that consumed the carbohydrate and electrolyte solution before and during exercise experienced greater endurance capacity. This could not be explained by the varying levels of muscle glycogen; however, higher plasma glucose concentration may have led to this result. Dr. Stephen Bailey posits that the central nervous system can sense the influx of carbohydrates and reduces the perceived effort of the exercise, allowing for greater endurance capacity.
== History == Patellamide A was first isolated in 1981 from the tunicate L. patella collected from the reefs of Korror Island, Palau Islands. L. patella has been a rich source of peptide natural products. Aside from the patellamides, the lissoclinamides, ulicyclamide, ulithiacyclamide and ascidiacyclamide were all isolated from L. patella. The absolute stereochemistry was later determined by X-ray crystallography.
Astatine was first produced by bombarding bismuth-209 with energetic alpha particles, and this is still the major route used to create the relatively long-lived isotopes astatine-209 through astatine-211. Astatine is only produced in minuscule quantities, with modern techniques allowing production runs of up to 6.6 gigabecquerels (about 86 nanograms or 2.47×1014 atoms). Synthesis of greater quantities of astatine using this method is constrained by the limited availability of suitable cyclotrons and the prospect of melting the target. Solvent radiolysis due to the cumulative effect of astatine decay is a related problem. With cryogenic technology, microgram quantities of astatine might be able to be generated via proton irradiation of thorium or uranium to yield radon-211, in turn decaying to astatine-211. Contamination with astatine-210 is expected to be a drawback of this method. The most important isotope is astatine-211, the only one in commercial use. To produce the bismuth target, the metal is sputtered onto a gold, copper, or aluminium surface at 50 to 100 milligrams per square centimeter. Bismuth oxide can be used instead; this is forcibly fused with a copper plate. The target is kept under a chemically neutral nitrogen atmosphere, and is cooled with water to prevent premature astatine vaporization. In a particle accelerator, such as a cyclotron, alpha particles are collided with the bismuth. Even though only one bismuth isotope is used (bismuth-209), the reaction may occur in three possible ways, producing astatine-209, astatine-210, or astatine-211.
=== Modeling === Models inform the design of engineered biological systems by better predicting system behavior prior to fabrication. Synthetic biology benefits from better models of how biological molecules bind substrates and catalyze reactions, how DNA encodes the information needed to specify the cell and how multi-component integrated systems behave. Multiscale models of gene regulatory networks focus on synthetic biology applications. Simulations can model all biomolecular interactions in transcription, translation, regulation and induction of gene regulatory networks.
Sources: en.wikipedia.org
== Non-classical examples of PLP == PLP is also found on glycogen phosphorylase in the liver, where it is used to break down glycogen in glycogenolysis when glucagon or epinephrine signals it to do so. However, this enzyme does not exploit the reactive aldehyde group, but instead utilizes the phosphate group on PLP to perform its reaction. Although the vast majority of PLP-dependent enzymes form an internal aldimine with PLP via an active site lysine residue, some PLP-dependent enzymes do not have this lysine residue, but instead have a histidine in the active site. In such a case, the histidine cannot form the internal aldimine, and, therefore, the co-factor does not become covalently tethered to the enzyme. GDP-4-keto-6-deoxymannose-3-dehydratase (ColD) is an example of such an enzyme. Human Serine hydroxymethyltransferase 2 regulates one-carbon transfer reactions required for amino acid and nucleotide metabolism, and exists in dimeric and tetrameric forms. The dimeric SHMT2 variant is a potent inhibitor of the BRISC deubiquitylase enzyme complex, which regulates immune-based cell signaling. Recent studies show that SJMT2 tetramerization is induced by PLP. This prevents interaction with the BRISC deubiqutylase complex, potentially linking vitamin B6 levels and metabolism to inflammation.
B'Tselem also argues that the restrictions on ill, wounded and pregnant Palestinians seeking acute medical care is in contravention of international law that states that medical professionals and the sick must be granted open passage. While Israeli Supreme Court has deemed the measures acceptable for security reasons, Haaretz's Amira Hass argues this policy defies one of the principles of the Oslo Accords, which states that Gaza and the West Bank constitute a single geographic unit. Strained intercommunal relations in Northern Ireland between Irish Catholics and the descendants of Protestant settlers from England and Scotland have resulted in de facto internal checkpoints. The peace lines are an internal border security measure to separate predominantly republican and nationalist Catholic neighbourhoods from predominantly loyalist and unionist Protestant neighbourhoods. They have been in place in some form or another since the end of The Troubles in 1998, with the Good Friday Agreement. The majority of peace walls are located in Belfast, but they also exist in Derry, Portadown, and Lurgan, with more than 32 kilometres (20 miles) of walls in Northern Ireland. The peace lines range in length from a few hundred metres to over 5 kilometres. They may be made of iron, brick, steel, or a combination of the three and are up to 8 metres (26 feet) high. Some have gates in them (sometimes staffed by police) that allow passage during daylight but are closed at night.
polymerization The formation of a polymer from its constituent monomers; the chemical reaction or series of reactions by which monomeric subunits are covalently linked together into a polymeric chain or branching aggregate; e.g. the polymerization of a nucleic acid chain by linking consecutive nucleotides, a reaction catalyzed by a polymerase enzyme.
=== Non-human models === Azvudine is found to be mutagenic in in vitro in the Ames test, CHL test, and in vitro in the mice micronucleus test. Azvudine is toxic to the reproductive system of rats and rabbit. The minimum reproductive NOAEL found for males is 5.0 mg/kg/d and for females 0.5 mg/kg/d. It is excreted in rat breast milk; the NOAEL for rat pups is 1.5 mg/kg/d. Azvudine is mainly toxic to the immune system, bone marrow, and digestive system of model animals. The chronic NOAELs are 0.5 mg/kg/d (rat, 3 months), 0.3 mg/kg/d (rat, 26 weeks), and 0.1 mg/kg/d (beagle dog, 1 month and 39 weeks). For comparison, the chronic human dose for HIV treatment is 0.05 mg/kg/d, using the reference 3 mg dose and an average Chinese body mass of 59.5 kg (2014).
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.
Legal status varies by country. It is not approved as a medicine, and it is prohibited in sport. Some jurisdictions restrict import, sale, or possession.