The short version of Laboratory compound fits in a sentence. The long version — which is the one that helps — is below.
This page was last updated on 2025-10-13 and is reviewed periodically as new material appears.
Because cardarine is not an approved medicine, no pharmacopeial monograph defines its identity, purity, or storage requirements. Laboratories typically rely on in-house methods and reference standards when testing materials labeled as GW501516. Certificates of analysis may report purity and identity for a specific batch, but their scope varies and they do not guarantee safety or legal status. Independent verification can include high-performance liquid chromatography, mass spectrometry, nuclear magnetic resonance, and elemental analysis. The distinction between research chemical labeling and human use is significant because quality standards and oversight differ.
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.
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.
| Property | Value | Notes |
|---|---|---|
| WADA classification | S4 Hormone and Metabolic Modulators | Prohibited at all times in sport. |
| Drug approval status | Not approved in major jurisdictions | No accepted therapeutic indication. |
| Common detection method | LC-MS/MS | Detects parent compound and metabolites. |
| Typical test matrix | Urine or blood | Urine is common in anti-doping testing. |
| Product labeling | Research chemical or supplement | Often not independently verified. |
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.
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.
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.
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.
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.
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.
== Geschichte == Vicin wurde erstmals im Jahr 1870 aus den Samen von Futterwicken isoliert, indem mit Schwefelsäure extrahiert und mit Quecksilbersulfat ausgefällt wurde. Später wurde Vicin auch in anderen Vicia-Arten wie Ackerbohnen und Erbsen-Wicken nachgewiesen, aber auch in anderen Arten wie Saat-Platterbsen. Die chemische Struktur der Verbindung wurde schrittweise ermittelt. Zunächst wurde 1896 die glykosidische Natur der Verbindung erkannt. Im selben Jahr wurde das Aglykon des Vicins, Divicin, isoliert. Zu Beginn des 20. Jahrhunderts wurde die Pyrimidinstruktur nachgewiesen. Trotz dieser anfänglichen Erfolge wurde die korrekte Formel von Vicin erst 1953 bestimmt.
== Metabolismus == Vicin selbst ist im Körper inaktiv. Wird Vicin über die Nahrung aufgenommen, hydrolisiert die Darmmikroflora die β-glykosidische Bindung zwischen dem Glukoseteil und der Hydroxylgruppe am C5 des Pyrimidinrings. Dabei entsteht das hochreaktive, freie Radikale erzeugende Aglykon Divicin (2,6-Diamino-4,5-dihydroxypyrimidin). Divicin weist ein hohes Oxidationspotential für Glutathion auf und wird über das Darmepithel ins Blut und die Erythrozyten aufgenommen. Divicin bzw. von diesem gebildete reaktive Sauerstoffspezies werden in den Erythrozyten von Glutathion reduziert. Glutathion wird durch das vom Enzym Glucose-6-Phosphat-Dehydrogenase bereitgestellte NADPH regeneriert.
== Physiologische Wirkung beim Menschen == Toxische Nebenwirkungen treten fast ausschließlich bei Menschen auf, die an einem Glucose-6-phosphat-Dehydrogenase-Mangel (G6PD-Mangel, Favismus) leiden. Dieser verursacht einen Mangel an Glutathion in den Erythrozyten, da Glutathion für die Neutralisierung der reaktiven Sauerstoffspezies benötigt wird, welche durch das stark reduzierende Divicin gebildet werden. Personen mit G6PD-Mangel sind sehr häufig asymptomatisch. Allerdings können sehr plötzlich lebensbedrohliche Anfälle von akuter hämolytischer Anämie auftreten. Anzeichen für solch einen plötzlichen Anfall von Favismus sind dunkler Urin, Blässe, Gelbsucht, Bauchschmerzen und in den meisten Fällen Fieber.
== Physiologische Wirkung bei Tieren == Eine Diät mit 10 g Vicin/kg Körpergewicht bei Legehennen führte zu einer verringerten Futteraufnahme, einem geringeren Eigewicht, einem geringeren Hämoglobingehalt und einer geringeren Fruchtbarkeit sowie zu einer Erhöhung des Lebergewichts, des Leberglutathionspiegels und der Plasmalipidspiegel. Eine Ernährung mit vergleichbaren Vicinmengen pro kg Körpergewicht bei Schweinen zeigte nur geringe Auswirkungen auf die Verdauung von Proteinen und Kohlenhydraten. In einer anderen Studie wurden Lege- und Masthühner mit Körnern gefüttert, die unterschiedlich lange eingeweicht waren, wodurch das Vicin teilweise oder vollständig entfernt wurde. Hennen, die Körner erhalten hatten, in denen sich noch Vicin befand, wiesen einen signifikanten Rückgang des korpuskularen Hämoglobins auf, während dies bei der Vergleichsgruppe nicht der Fall war. Eine In-vivo-Studie an Ratten zeigte, dass die orale Verabreichung von Vicin nur zu einer geringen Verringerung der Glutathionkonzentration und zu keiner erhöhten Sterblichkeit führte. Die intraperitoneale-Verabreichung hingegen führte zu einem raschen Abfall des Glutathions, gefolgt vom Tod aufgrund von Anoxie.
Sources: de.wikipedia.org
Anti-doping laboratories typically use LC-MS/MS to detect GW501516 and its metabolites in urine. The method is sensitive and can identify the compound at low concentrations. Detection depends on sample timing, metabolism, and the specific assay.
Legality varies by country and context. It lacks marketing approval as a medicine in major countries. Sports organizations prohibit its use at all times.
A certificate of analysis may report identity, purity, and testing methods for a specific batch. It does not guarantee safety or legal status. Independent verification can confirm whether the material matches the label.
Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.