Cardarine 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.
Updated 2026-05-26. Numbers and descriptions here follow the published literature rather than marketing material.
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.
Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.
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.
| Property | Value | Notes |
|---|---|---|
| Regulatory status | Prohibited in sport; not approved as medicine | Listed by WADA at all times. |
| Common synonyms | GW501516, GW-501516, endurobol | Cardarine is a colloquial name. |
| Typical analytical method | LC-MS/MS | Detects parent compound and metabolites. |
| Common test matrix | Urine | Blood and dried blood spots also possible. |
| Legal classification | Varies by country | Often treated as unapproved drug or research chemical. |
Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.
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.
Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.
Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.
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 synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.
5-HT2C receptor agonists reduce appetite by working on serotonin receptors in a region of the brain called the hypothalamus. Lorcaserin (Belviq) was FDA approved for weight loss but was withdrawn from the market because a safety clinical trial shows an increased occurrence of cancer. Cannabinoid receptor antagonists were developed to treat obesity because researchers noticed that cannabinoid agonists (such as THC, the main pharmacologically active component of cannabis), increased appetite. However, some drugs in this class such as rimonabant were withdrawn or ceased development due to concerns about mental health and suicide. More selective drugs—some are in development that act only in peripheral tissues, not the brain—may be able to achieve this result with fewer adverse effects. GLP-1 agonists such as tirzepatide, semaglutide, and liraglutide slow gastric emptying and also have neurologically driven effects on appetite. It is unknown if GLP-1 agonists or dual/triple agonists of GLP-1 and/or the glucagon or GIP receptors act solely by reducing energy intake or if they also increase energy expenditure. Setmelanotide is an agonist of the melanocortin 4 receptor and is used in people with certain rare genetic conditions that cause obesity. It is less effective and not approved for general obesity.
Brenipatide (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code name LY-3537031) is a dual agonist of glucagon-like peptide-1 (GLP-1) receptors and gastric inhibitory polypeptide (GIP) receptors. Brenipatide is under development by Eli Lilly and Company for the treatment of alcoholism, bipolar disorder, asthma, smoking withdrawal, cardiovascular disorders, liver disorders, metabolic disorders, and obesity. It is taken by subcutaneous injection once per month. The drug has a longer elimination half-life than tirzepatide or retatrutide. As of December 2025, it was in phase 3 clinical trials for alcoholism and bipolar disorder, phase 2 trials for asthma and smoking withdrawal, and phase 1 trials for cardiovascular disorders, liver disorders, metabolic disorders, and obesity. List of investigational antipsychotics List of investigational bipolar disorder drugs List of investigational substance-related disorder drugs
Banting House features archival materials, artifacts, and other ephemera associated with Banting as co-discoverer of insulin, doctor, and artist, as well as his involvement in the first and second world wars. One gallery depicts the kind of office Banting might have had, and contains several of his belongings, including his original medicine cabinet, and a graduated cylinder Banting used during his time at the University of Western Ontario. The apothecary in the next room features a sink that Banting installed for his medical practice. Other galleries in the museum hold original belongings of Banting as well, most notably his desk and his bed frame. The bed frame is kept in Banting's bedroom, and visitors are encouraged to take a moment or a picture with it, as it is not roped off like many other areas of the museum. Additionally, an official replica of the Nobel Prize medal co-awarded to Banting and Macleod is on display, as well as many of Banting's other medals. Other displays include the military gallery, which includes a representation of the type of operating room Banting would have worked in on the field during the First World War, some information on the projects he headed during the Second World War, and an entire gallery filled with artwork done by Banting.
The increasing amount of genomic and molecular information is the basis for understanding higher-order biological systems, such as the cell and the organism, and their interactions with the environment, as well as for medical, industrial and other practical applications. The KEGG resource provides a reference knowledge base for linking genomes to biological systems, categorized as building blocks in the genomic space (KEGG GENES), the chemical space (KEGG LIGAND), wiring diagrams of interaction networks and reaction networks (KEGG PATHWAY), and ontologies for pathway reconstruction (BRITE database). The KEGG PATHWAY database is a collection of manually drawn pathway maps for metabolism, genetic information processing, environmental information processing such as signal transduction, ligand–receptor interaction and cell communication, various other cellular processes and human diseases, all based on extensive survey of published literature.
Most class III adenylyl cyclases are transmembrane proteins with 12 transmembrane segments. The protein is organized with 6 transmembrane segments, then the C1 cytoplasmic domain, then another 6 membrane segments, and then a second cytoplasmic domain called C2. The important parts for function are the N-terminus and the C1 and C2 regions. The C1a and C2a subdomains are homologous and form an intramolecular 'dimer' that forms the active site. In Mycobacterium tuberculosis and many other bacterial cases, the AC-III polypeptide is only half as long, comprising one 6-transmembrane domain followed by a cytoplasmic domain, but two of these form a functional homodimer that resembles the mammalian architecture with two active sites. In non-animal class III ACs, the catalytic cytoplasmic domain is seen associated with other (not necessarily transmembrane) domains. Class III adenylyl cyclase domains can be further divided into four subfamilies, termed class IIIa through IIId. Animal membrane-bound ACs belong to class IIIa.
Sources: en.wikipedia.org
As of 2020, normal ALP levels were "not well defined", and there tend to be variations by sex and racial background, and by age, with children and adolescents having markedly higher levels. There are many possible explanations for elevated ALP. When the cause is unclear, isoenzyme studies using electrophoresis can confirm the source of the increase. Skelphosphatase (which is localized in osteoblasts and extracellular layers of newly synthesized matrix) is released into circulation by a yet unclear mechanism. Placental alkaline phosphatase is elevated in seminomas and active forms of rickets, as well as in the following diseases and conditions: Biliary obstruction Bone conditions Osteoblastic bone tumors Osteomalacia Osteoporosis Hepatitis Mononucleosis Cirrhosis Acute cholecystitis Myelofibrosis Leukemoid reaction Congestive heart failure Lymphoma Paget's disease Sarcoidosis Hyperthyroidism Hyperparathyroidism Myocardial infarction Cholangitis Ischemic cholangiopathy Pregnancy High doses of estrogens
The predecessor to the CAD, termed an evaporative electrical detector, was first described by Kaufman in 2002 at TSI Inc in US patent 6,568,245 and was based on the coupling of liquid chromatographic approaches to TSI's electrical aerosol measurement (EAM) technology. At around the same time Dixon and Peterson at California State University were investigating the coupling of liquid chromatography to an earlier version of TSI's EAM technology, which they called an aerosol charge detector. Subsequent collaboration between TSI and ESA Biosciences Inc. (now part of Thermo Fisher Scientific), led to the first commercial instrument, the Corona CAD, which received both the Pittsburgh Conference Silver Pittcon Editor's Award (2005) and R&D 100 award (2005). Continued research and engineering improvements in product design resulted in CADs with ever increasing capabilities. The newest iterations of the CAD are the Thermo Scientific Corona Veo Charged Aerosol Detector, Corona Veo RS Charged Aerosol Detector and Thermo Scientific Vanquish Charged Aerosol Detectors.
Sampling provides one rational means of verification that a production lot conforms to the requirements of technical specifications. 100% inspection does not guarantee 100% compliance and is too time-consuming and costly. Rather than evaluating all items, a specified sample is taken, inspected or tested, and a decision is made about accepting or rejecting the entire production lot. Sampling plans have known risks: an acceptable quality limit (AQL) and a rejectable quality level, such as lot tolerance percent defective (LTDP), are part of the operating characteristic curve of the sampling plan. These are primarily statistical risks and do not necessarily imply that a defective product is intentionally being made or accepted. Plans can have a known average outgoing quality limit (AOQL). A single sampling plan for attributes is a statistical method by which the lot is accepted or rejected on the basis of one sample. Suppose that we have a lot of sizes M {\displaystyle M} ; a random sample of size N < M {\displaystyle N<M} is selected from the lot; and an acceptance number B
the carboxylation of glutamate allows for better binding of calcium cations, Hydroxyproline, generated by hydroxylation of proline, is a major component of the connective tissue collagen. Hypusine in the translation initiation factor EIF5A, contains a modification of lysine. Some non-proteinogenic amino acids are not found in proteins. Examples include 2-aminoisobutyric acid and the neurotransmitter gamma-aminobutyric acid. Non-proteinogenic amino acids often occur as intermediates in the metabolic pathways for standard amino acids – for example, ornithine and citrulline occur in the urea cycle, part of amino acid catabolism (see below). A rare exception to the dominance of α-amino acids in biology is the β-amino acid beta alanine (3-aminopropanoic acid), which is used in plants and microorganisms in the synthesis of pantothenic acid (vitamin B5), a component of coenzyme A.
Sources: en.wikipedia.org
G-protein-coupled receptor oligomerisation is a widespread phenomenon. One of the best-studied examples is the metabotropic GABAB receptor. This so-called constitutive receptor is formed by heterodimerization of GABABR1 and GABABR2 subunits. Expression of the GABABR1 without the GABABR2 in heterologous systems leads to retention of the subunit in the endoplasmic reticulum. Expression of the GABABR2 subunit alone, meanwhile, leads to surface expression of the subunit, although with no functional activity (i.e., the receptor does not bind agonist and cannot initiate a response following exposure to agonist). Expression of the two subunits together leads to plasma membrane expression of functional receptor. It has been shown that GABABR2 binding to GABABR1 causes masking of a retention signal of functional receptors.
Many of the payloads for oncology ADCs (oADC) are natural product based with some making covalent interactions with their target. Payloads include the microtubulin inhibitors monomethyl auristatin E (MMAE), monomethyl auristatin F (MMAF) and mertansine, DNA binder calicheamicin and topoisomerase 1 inhibitors SN-38 and exatecan resulting in a renaissance for natural product total synthesis. Glucocorticoid receptor modulators (GRMs) represent to most active payload class for iADCs. Approaches releasing marketed GRM molecules such as dexamethasone and budesonide have been developed. Modified GRM molecules have also been developed that enable the attachment of the linker with the term ADCidified describing the medicinal chemistry process of payload optimization to facilitate linker attachment. Alternatives to small molecule payloads have also been investigated, for example, siRNA. More recently, targeted protein degraders have been explored as payloads for antibody conjugates. A 2025 study described a KIF11-directed degrader–antibody conjugate (DAC), in which a cereblon-recruiting degrader was used as the payload to induce antigen-dependent protein degradation and cytotoxicity in preclinical models.
In molecular biology, ATP10 protein (mitochondrial ATPase complex subunit ATP10) is an ATP synthase assembly factor. It is essential for the assembly of the mitochondrial F1-F0 complex. A yeast nuclear gene (ATP10) encodes a product that is essential for the assembly of a functional mitochondrial ATPase complex. Mutations in ATP10 induce a loss of rutamycin sensitivity in the mitochondrial ATPase, but do not affect the respiratory enzymes. ATP10 has a molecular weight of 30,293 Da and its primary structure is not related to any known subunit of the yeast or mammalian mitochondrial ATPase complexes. ATP10 is associated with the mitochondrial membrane. It is suggested that the ATP10 product is not a subunit of the ATPase complex but rather a protein required for the assembly of the F0 sector of the complex.
Sources: en.wikipedia.org
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.
Laboratories use liquid chromatography-tandem mass spectrometry to detect GW501516 and its metabolites. Urine is commonly tested, and testing can occur in and out of competition.
No, cardarine is not a SARM. It is a PPARδ agonist, which acts on a different receptor. The two classes are often confused in online discussions.
No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.