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Identity And Regulatory Status — Background and Details

By Editorial Desk · published 2025-06-30 · last reviewed 2025-08-01 · News

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

Reviewed 2025-08-01. Anything still debated is marked as such rather than presented as settled.

Identity and Regulatory Status

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.

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.

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 at a glance

PropertyValueNotes
Common synonymsGW501516; GW-1516; endurobolGW501516 is the research code
Drug classPPARδ agonistNot a selective androgen receptor modulator
Molecular formulaC21H18F3NO3S2Established chemical formula
Molar mass453.5 g/molCalculated from the formula
Regulatory statusProhibited in sport; not approved as medicineStatus varies by country

Mechanism and Safety Research

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.

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.

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Background and Regulatory Status

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.

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.

Notes from published material

=== Biosynthesis === Creatine is not an essential nutrient. It is an amino acid derivative, naturally produced in the body from the amino acids glycine and arginine, with an additional requirement for S-adenosyl methionine (a derivative of methionine) to catalyze the transformation of guanidinoacetate to creatine. In the first step of the biosynthesis, the enzyme arginine:glycine amidinotransferase (AGAT, EC:2.1.4.1) mediates the reaction of glycine and arginine to form guanidinoacetate. This product is then methylated by guanidinoacetate N-methyltransferase (GAMT, EC:2.1.1.2), using S-adenosyl methionine as the methyl donor. Creatine itself can be phosphorylated by creatine kinase to form phosphocreatine, which is used as an energy buffer in skeletal muscles and the brain. A cyclic form of creatine, called creatinine, exists in equilibrium with its tautomer and with creatine.

This enzyme is an oxidoreductase, oxidizing the CH-OH alcohol group to a carbonyl group. NAD+ is the oxidizing agent, yielding reduced NADH. Aryllactates and arylpyruvates are intermediates in tyrosine, phenylalanine and tryptophan metabolism and blood serum levels of these compounds affect intestinal permeability and systemic immunity in mice. Alternative names for these enzymes are: (R)-aromatic lactate dehydrogenase, D-aryllactate D-hydrogenase, (indol-3-yl)lactate:NAD+ oxidoreductase, indolelactate:NAD+ oxidoreductase, (R)-4-hydroxyphenyllactate dehydrogenase, (R)-3-(4-hydroxyphenyl)lactate:NAD(P)+ 2-oxidoreductase

Eosinophilia is a condition in which too many eosinophils (a type of immune cell that attacks parasites and is involved in certain allergic reactions) are present in the blood. Eosinophilia-myalgia syndrome is a form of eosinophilia caused by L-tryptophan supplements. Eosinophilic fasciitis affects the connective tissue surrounding skeletal muscles, bones, blood vessels, and nerves in the arms and legs. Graft-versus-host disease is an autoimmune condition that occurs as a result of bone-marrow transplants in which the immune cells from the transplanted bone marrow attack the host's body. Mycosis fungoides is a type of cutaneous T cell lymphoma, a rare cancer that causes rashes all over the body. Nephrogenic systemic fibrosis is a condition usually caused by kidney failure that results in fibrosis (thickening) of the tissues. Primary biliary cirrhosis is an autoimmune disease of the liver. Primary pulmonary hypertension Complex regional pain syndrome

== See also == Classification of personality disorders Identity disturbance – Deficiency or inability to maintain one or more major components of identity Otto Kernberg – Founder of Transference-Focused Psychotherapy (TFP)Pages displaying short descriptions of redirect targets

=== Small animal imaging === A miniature animal PET has been constructed that is small enough for a fully conscious rat to be scanned. This RatCAP (rat conscious animal PET) allows animals to be scanned without the confounding effects of anesthesia. PET scanners designed specifically for imaging rodents, often referred to as microPET, as well as scanners for small primates, are marketed for academic and pharmaceutical research. The scanners are based on microminiature scintillators and amplified avalanche photodiodes (APDs) through a system that uses single-chip silicon photomultipliers. In 2018 the UC Davis School of Veterinary Medicine became the first veterinary center to employ a small clinical PET scanner as a scanner for clinical (rather than research) animal diagnosis. Because of cost as well as the marginal utility of detecting cancer metastases in companion animals (the primary use of this modality), veterinary PET scanning is expected to be rarely available in the immediate future.

Sources: en.wikipedia.org

Background from the literature

In this role, she serves as an advocate and liaison for basic science researchers working in clinical departments to help facilitate the combination of “basic research” which seeks to answer fundamental scientific questions and “translational research” that seeks to put those findings to use, for example in a clinical setting. In 2020, she was named director of the department of pharmacology and molecular sciences at Johns Hopkins University School of Medicine, becoming the first African-American director of a basic science department, and the first Black woman to chair any department, at Johns Hopkins University School of Medicine. Outside of Johns Hopkins, Bumpus chaired the National Institute of Health (NIH)'s Xenobiotic and Nutrient Disposition and Action study section and served as a science commissioner and member of Washington, D.C.’s Science Advisory Board. She was an associate editor of the journal Drug Metabolism and Disposition. She has been strongly involved with the American Society for Pharmacology and Experimental Therapeutics (ASPET), where she served as secretary and treasurer and president.

The king of Thogar, called Mendre, or "the Persian" (Po-lo-si), or Anandavarma, had images painted in these caves for the followers of Buddha, by the artist and painter Mitradatta, also by Naravahanadatta, who came from a place of worship (Kultort) of the Niganthas, finally by Priyaratna who came from Syria also with their apprentices (Werkschüler). Mendre, the king, received an image of Amitabha from the emperor of China, and went into the land of blessedness (Sukhavati). A son of the emperor of China came to the castle of Mir-li, killed, according to an oath that he had made, all Jaina-Niganthas and all followers of Kalachakra and restored all the caves for the worship of Buddha (Buddha-Kultus). The Japanese Buddhist scholar Teramoto Enga gave a rather different translation:

Adiponectin (also referred to as GBP-28, apM1, AdipoQ and Acrp30) is a protein hormone and adipokine, which is involved in regulating glucose levels and fatty acid breakdown. In humans, it is encoded by the ADIPOQ gene and is produced primarily in adipose tissue, but also in muscle and even in the brain. Adiponectin is a 244-amino-acid-long polypeptide (protein). It has four distinct regions: The first is a short signal sequence that targets the hormone for secretion outside the cell; next is a short region that varies between species; the third is a 65-amino acid region with similarity to collagenous proteins; the last is a globular domain. Overall, this protein shows similarity to the complement 1Q factors (C1Q), but when the three-dimensional structure of the globular region was determined, a striking similarity to TNFα was observed, despite unrelated protein sequences.

Plants and animals alike both use small polypeptides for signaling in cell-to-cell communication. CLAVATA3/Embryo Surrounding Region-Related, also known as a plant peptide hormone, signaling is important for cell to cell signaling but also long distance communication. These two actions are especially important for plant cells because they are stationary and must perform cell expansion. In multicellular organisms, cell-to-cell communication has been found to be very crucial for many growth processes that occur inside the organism. The 12 or 13 amino acid polypeptides are the mature forms of the CLE proteins that are derived from the conserved CLE domains. More and more CLE genes are being identified with more research being conducted in this area. CLE genes have not only been found in seed plants but also in lycophytes, bryophytes, and green algae.

Control patterns describe how a perturbation to a given parameter affects the steady-state level of a given variable. For example, a concentration control coefficient can describe how the overexpression of a specific enzyme can influence steady-state metabolite concentrations. Flux control coefficients are similar in that they describe how a perturbation in a given enzyme affects steady-state flux through a pathway. Such coefficients can be written in terms of elasticity coefficients. Elasticity coefficients are local properties that describe how a single reaction is influenced by changes in the substrates and products that might influence the rate. For example, given a reaction such as: S ⟶ v P {\displaystyle S{\stackrel {v}{\longrightarrow }}P} we will assume it has a rate of reaction of v {\displaystyle v} . This reaction rate can be influenced by changes in the concentrations of substrate S {\displaystyle S} or product P {\displaystyle P} . This influence is measured by an elasticity which is defined as: ε s v = ∂ v ∂ s s v

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a SARM?

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.

Is cardarine approved for human use?

No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.

Why was its development discontinued?

Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.

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.

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