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Regulation And Detection — Quick Reference

By Editorial Desk · published 2026-06-08 · last reviewed 2026-07-16 · Blog

Research chemical raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.

Reviewed 2026-07-16. Anything still debated is marked as such rather than presented as settled.

Regulation and Detection

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.

Background and Regulatory History

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.

Cardarine at a glance

PropertyValueNotes
Regulatory statusProhibited in sport; not approved as medicineListed by WADA at all times.
Common synonymsGW501516, GW-501516, endurobolCardarine is a colloquial name.
Typical analytical methodLC-MS/MSDetects parent compound and metabolites.
Common test matrixUrineBlood and dried blood spots also possible.
Legal classificationVaries by countryOften treated as unapproved drug or research chemical.

Identity and Pharmacological Classification

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.

Cardarine is a common name for GW501516, also GW-1516, a synthetic compound developed as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. It belongs to a class of agents that modulate gene transcription related to lipid and energy metabolism. The compound was studied in preclinical and early clinical research for metabolic and cardiovascular conditions, but it did not progress to approved therapeutic use. Its name appears in fitness and sports contexts despite not being approved as a drug.

Related pages on this site

Cardarine as Investigational PPARδ Agonist

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.

Regulation and Analytical Detection

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 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.

Notes from published material

Hereditary coproporphyria (HCP) is a disorder of heme biosynthesis, classified as an acute hepatic porphyria. HCP is caused by a deficiency of the enzyme coproporphyrinogen oxidase, coded for by the CPOX gene, and is inherited in an autosomal dominant fashion, although homozygous individuals have been identified. Unlike acute intermittent porphyria, individuals with HCP can present with cutaneous findings similar to those found in porphyria cutanea tarda in addition to the acute attacks of abdominal pain, vomiting and neurological dysfunction characteristic of acute porphyrias. Like other porphyrias, attacks of HCP can be induced by certain drugs, environmental stressors or diet changes. Biochemical and molecular testing can be used to narrow down the diagnosis of a porphyria and identify the specific genetic defect. Overall, porphyrias are rare diseases. The combined incidence for all forms of the disease has been estimated at 1:20,000. The exact incidence of HCP is difficult to determine, due to its reduced penetrance.

gene product Any of the biochemical material resulting from the expression of a gene, most commonly interpreted as the functional mRNA transcript produced by transcription of the gene or the fully constructed protein produced by translation of the transcript, though non-coding RNA molecules such as transfer RNAs may also be considered gene products. A measurement of the quantity of a given gene product that is detectable in a cell or tissue is sometimes used to infer how active the corresponding gene is.

Elements of the morphine structure have been used to create completely synthetic drugs such as the morphinan family (levorphanol, dextromethorphan and others) and other groups that have multiple members with morphine-like qualities. The modification of morphine and the aforementioned synthetics has also given rise to non-narcotic drugs with other uses such as emetics, stimulants, antitussives, anticholinergics, muscle relaxants, local anaesthetics, general anaesthetics, and others. Morphine-derived agonist–antagonist drugs have also been developed.

Clinical and Vaccine Immunology (CVI) was a peer-reviewed journal published by the American Society for Microbiology. CVI enhances our understanding of the immune response in health and disease by showcasing important clinically relevant research, including new animal models for human immunologic diseases, viral immunology, immunopathogenesis, and clinical laboratory immunology. In particular, the journal highlights important discoveries in immunization and vaccine research, such as the development and evaluation of vaccines, human and animal immune responses to vaccines, vaccine vectors, adjuvants and immunomodulators, quantitative assays of vaccine efficacy, and clinical trials. The journal publishes primary research articles, editorials, commentaries, minireviews, and case reports. Articles are freely accessible after six months (delayed open access). Through its "Global Outreach Program", free online access is available to qualified microbiologists in eligible developing countries.

Sources: en.wikipedia.org

Background from the literature

== Chemistry == Diazepam does not possess any chiral centers in its structure, but it does have two conformers: the 'P'-conformer and 'M'-conformer. Diazepam is an equimolar mixture, and it was shown through CD spectra in serum protein solutions that the 'P'-conformer is preferred by α1-acid glycoprotein binding. The drug diazepam occurs as a pale yellow-white crystalline powder without a distinctive smell and has a low molecular weight (MW = 284.74 g/mol). This classic aryl 1,4-benzodiazepine possesses three acceptors and no hydrogen bond donors. Diazepam is moderately lipophilic with LogP (Octanol-Water Partition Coefficient) value of 2,82 and hydrophilic with a TPSA (Topological Polar Surface Area) value of 32.7 Ų. The LogP value indicates that diazepam tends to dissolve more readily in lipid-based environments, such as chloroform, acetone, ethanol and ether, compared to water. The TPSA value implies that a segment of the molecule exhibits a degree of polarity or hydrophilicity and represents the collective surface area of polar atoms, like oxygen or nitrogen, along with their connected hydrogen atoms. A TPSA value of 32,7 Ų signifies a moderate level of polarity within the compound. TPSA is especially useful in medical chemistry as it shows the ability of a molecule to permeate cells. Molecules with a PSA value smaller than 60–70 Ų have a better ability to permeate cells.

Peukert argued that societies that have reached "classical modernity" are characterized by advanced capitalist economic organization and mass production, by the "rationalization" of culture and society, massive bureaucratization of society, the "spirit of science" assuming a dominant role in popular discourses, and the "social disciplining" and "normalization" of the majority of ordinary people. Peukert was greatly influenced by the theories of Max Weber, but unlike many other scholars, who saw Weber attempting to rebut Karl Marx, he viewed Weber's principal intellectual opponent as Friedrich Nietzsche. Peukert wrote that for Weber, the principal problems of modern Germany were: The increasing "rationalization" of everyday life via bureaucratization and secularism had led to a "complete demystification of the world". The popularity of the "spirit of science" had led to a misguided belief that science could solve all problems within the near-future. Contrary to the "Bielefeld School", Peukert argued by the time of the Weimar Republic, Germany had broken decisively with the past, and had become a thoroughly "modern" society in all its aspects. Peukert argued that the very success of German modernization inspired by the "dream of reason" meant the contradictions and problems of "classical modernity" were felt more acutely in Germany than elsewhere. For Peukert, the problems of "classical modernity" were:

== Prevention == Key prevention strategies for cirrhosis are population-wide interventions to reduce alcohol intake (through pricing strategies, public health campaigns, and personal counseling), programs to reduce the transmission of viral hepatitis, and screening of relatives of people with hereditary liver diseases. Little is known about factors affecting cirrhosis risk and progression. However, many studies have provided increasing evidence for the protective effects of coffee consumption against the progression of liver disease. These effects are more noticeable in liver disease that is associated with alcohol use disorder. Coffee has antioxidant and antifibrotic effects. Caffeine may not be the important component; polyphenols may be more important. Drinking two or more cups of coffee a day is associated with improvements in the liver enzymes ALT, AST, and GGT. Even in those with liver disease, coffee consumption can lower fibrosis and cirrhosis.

== Function == Dietary copper enters the bloodstream primarily in its oxidized Cu(II) form. Once absorbed, Cu(II) is taken up by the hCTR1, which mediates its cellular import. At the extracellular face, the flexible N-termini extends outward and captures Cu(II) from the blood carrier protein, after that it reduces Cu(II) to Cu(I) state and preserves the reduced Cu(I) oxidation state. The extracellular domain of hCTR1 holds both Cu(II) and Cu(I) binding sites: 1MDHxHH and 22HHH, serve as two Cu(II) binding sites; 7MxMxxM and 41MMMxM, comprise the first Cu(I) binding sites in the extracellular domain of hCTR1. The extracellular hCTR1 domain is also characterized by two glycosylation sites, N15 and T27. The transmembrane domain of hCTR1 is characterized by 150MxxxM and 167GxxxG motifs. In the second transmembrane helix, M150 and M154 are considered as Cu(I)-binding residues. There are two methionine triads lining the pore, and these methionine rings have soft sulfur ligands and create the "selectivity filter" for Cu(I), that excludes harder ions such as Ca(II). The hCTR1 C-terminal domain controls the distribution of Cu(I), it plays a role in copper trafficking and regulation. It interacts with metallochaperones and with the of the 188HCH motif transfers the Cu(I) ion to Atox1. Althogether hCTR1 operates as a dynamic, adaptable transporter, delicately balancing the flexibility and selectivity of copper ions.

Powdered milk is a common item in UN food aid supplies, fallout shelters, warehouses, and wherever fresh milk is not a viable option. It is frequently used in the manufacture of infant formula. Like other dry foods, it is considered nonperishable and is favored by survivalists, hikers, and others requiring nonperishable, easy-to-prepare food. It is widely used in many developing countries because of reduced transport and storage costs (reduced bulk and weight, no refrigerated vehicles). Because of its resemblance to cocaine and other drugs, powdered milk is sometimes used in filmmaking as a non-toxic prop that may be insufflated.

Sources: en.wikipedia.org

Reference notes

== Function == Cytosolic and membrane-bound forms of glutathione S-transferase are encoded by two distinct supergene families. At present, eight distinct classes of the soluble cytoplasmic mammalian glutathione S-transferases have been identified: alpha, kappa, mu, omega, pi, sigma, theta and zeta. This gene encodes a cytoplasmic glutathione S-transferase that belongs to the mu class. The mu class of enzymes functions in the detoxification of electrophilic compounds, including carcinogens, therapeutic drugs, environmental toxins, and products of oxidative stress, by conjugation with glutathione. The genes encoding the mu class of enzymes are organized in a gene cluster on chromosome 1p13.3, and are known to be highly polymorphic. These genetic variations can change an individual's susceptibility to carcinogens and toxins, as well as affect the toxicity and efficacy of certain drugs. Null mutations of this class mu gene have been linked with an increase in a number of cancers, likely due to an increased susceptibility to environmental toxins and carcinogens. Multiple protein isoforms are encoded by transcript variants of this gene.

The investigators found that SAGE systems were nontoxic in vivo, and were capable of eliciting CD4 T cell and B cell responses in the case of the tetanus toxoid and ovalbumin systems while eliciting a CD8 T cell response with the hemagglutinin system. Some advantages to using SAGE systems for antigen presentation include the ability to remain stable and functional after functionalization with cargo, the ability to modify and tune cellular uptake properties, and the modularity of the platform which could potentially be used to present multiple antigens at the same time, resulting in increased antigen immunogenicity. Another type of coiled-coil nanoparticle system is the self-assembling protein nanoparticles (SAPN). SAPN differs from SAGE in that SAPN utilizes trimeric and pentameric coiled-coil motifs. This change results in the self-assembly of a symmetrical polyhedral 16 nm nanoparticle composed of 60 monomer building blocks. The small size of SAPN allows the nanoparticle system to resemble viruses in shape and size, which is beneficial to antigen presentation. Specifically, SAPN has been utilized by Dr. David Lanar and colleagues to develop a P. falciparum malaria vaccine whereby B and CD8-T cell epitopes of the disease were modified into the SAPN coiled-coil motifs. In vivo results showed that a long-lasting immune response was generated in the mice for up to 13 months, capable of preventing malaria infection in vaccine-treated mice.

These cytosolic formyltransferase produce fMet-tRNAi, which can be used by cytosolic ribosomes to produce proteins with a N-terminal fMet. These proteins are targeted for degradation by specific processes in the cell.

== Diagnosis == Epidemiologically, the disorder usually develops slowly and is mainly observed in people over the age of 50. Diagnosis is made on the basis of bone marrow biopsy. Fibrosis grade 2 or 3 defines overt PMF whereas grade 0 or 1 defines prefibrotic primary myelofibrosis. A physical exam of the abdomen may reveal enlargement of the spleen, the liver, or both. Bone marrow biopsy shows fibrosis of the bone marrow. In early stages, this fibrosis is characterised by scattered linear reticulin fibres.

=== Orientational anisotropy === SHG polarization anisotropy can be used to determine the orientation and degree of organization of proteins in tissues since SHG signals have well-defined polarizations. By using the anisotropy equation:

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine legal?

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.

How is cardarine detected in athletes?

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.

Is cardarine a SARM?

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.

Is cardarine a selective androgen receptor modulator?

No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.

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