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Identity And Pharmacological Classification — Questions and Answers

By Editorial Desk · published 2026-05-02 · last reviewed 2026-06-04 · Blog

The short version of fatty acid oxidation fits in a sentence. The long version — which is the one that helps — is below.

This page was last updated on 2026-06-04 and is reviewed periodically as new material appears.

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.

PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.

Preclinical Findings and Safety Signals

Safety concerns emerged from long-term animal studies. In rodents given the compound for extended periods, researchers found an increased incidence of certain cancers, including liver and bladder tumors. These findings contributed to the discontinuation of clinical development. Whether similar risks apply to short-term or low-level exposure in humans is not established, and controlled human safety data are limited. The relevance of high-dose rodent carcinogenicity findings to human use remains a subject of debate.

Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.

Laboratory studies indicate that GW501516 activates PPARδ, a nuclear receptor involved in fatty acid oxidation and energy metabolism. In rodent experiments, treated animals often showed increased endurance and reduced fat mass. These effects were observed under controlled conditions and do not establish safe or effective use in humans. The exact dose-response relationship in humans remains poorly characterized. Species differences in metabolism can affect how results translate across animals and people.

Cardarine at a glance

PropertyValueNotes
Chemical classPPARδ agonistNot an anabolic steroid.
Common synonymsGW501516, GW-1516Cardarine is an informal name.
AppearanceWhite to off-white powderTypical for research-grade solid.
Solubility classPoorly soluble in water; soluble in some organic solventsSuch as DMSO or ethanol in laboratory settings.
Typical storage temperatureCool, dry, protected from lightSpecific conditions vary by supplier and form.

Mechanism and Detection

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.

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Detection and Regulatory Landscape

A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.

Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.

Background and Regulatory History

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 is a common name for the investigational chemical GW501516, also written GW-1516. It was developed as a peroxisome proliferator-activated receptor delta agonist for metabolic conditions such as dyslipidemia. Early research focused on lipid handling and energy use in skeletal muscle and other tissues. The compound was never approved as a medicine. In public discussion, it is often grouped with performance-enhancing substances, although its receptor target differs from that of anabolic steroids or selective androgen receptor modulators. Regulatory and health authorities have issued warnings about its use.

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.

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.

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.

Further detail

=== Bibliography === Ashby, Michael; Hugh Shercliff; David Cebon (2007). Materials: engineering, science, processing and design (1st ed.). Butterworth-Heinemann. ISBN 978-0-7506-8391-3. Askeland, Donald R.; Pradeep P. Phulé (2005). The Science & Engineering of Materials (5th ed.). Thomson-Engineering. ISBN 978-0-534-55396-8. Callister, Jr., William D. (2000). Materials Science and Engineering – An Introduction (5th ed.). John Wiley and Sons. ISBN 978-0-471-32013-5. Eberhart, Mark (2003). Why Things Break: Understanding the World by the Way It Comes Apart. Harmony. ISBN 978-1-4000-4760-4. Gaskell, David R. (1995). Introduction to the Thermodynamics of Materials (4th ed.). Taylor and Francis Publishing. ISBN 978-1-56032-992-3. González-Viñas, W. & Mancini, H.L. (2004). An Introduction to Materials Science. Princeton University Press. ISBN 978-0-691-07097-1. Gordon, James Edward (1984). The New Science of Strong Materials or Why You Don't Fall Through the Floor (eissue ed.). Princeton University Press. ISBN 978-0-691-02380-9. Mathews, F.L. & Rawlings, R.D. (1999). Composite Materials: Engineering and Science. Boca Raton: CRC Press. ISBN 978-0-8493-0621-1. Lewis, P.R.; Reynolds, K. & Gagg, C. (2003). Forensic Materials Engineering: Case Studies. Boca Raton: CRC Press. ISBN 978-0-8493-1182-6. Wachtman, John B. (1996). Mechanical Properties of Ceramics. New York: Wiley-Interscience, John Wiley & Son's. ISBN 978-0-471-13316-2. Walker, P., ed. (1993). Chambers Dictionary of Materials Science and Technology. Chambers Publishing. ISBN 978-0-550-13249-9. Mahajan, S. (2015).

Outpatients were not usually a junior house officer's responsibility, but such clinics formed a large part of the workload of more senior trainees, often with little real supervision. Registrar posts lasted one or two years, and sometimes much longer outside an academic setting. It was common to move from one registrar post to another. Fields such as psychiatry and radiology used to be entered at the registrar stage, but the other registrars would usually have passed part one of a higher qualification, such as a Royal College membership or fellowship before entering that grade. Part two (the complete qualification) was necessary before obtaining a senior registrar post, usually linked to a medical school, but many left hospital practice at this stage rather than wait years to progress to a consultant post. Most British clinical diplomas (requiring one or two years' experience) and membership or fellowship exams were not tied to particular training grades, though the length of training and nature of experience might be specified. Participation in an approved training scheme was required by some of the royal colleges. The sub-specialty exams in surgery, now for Fellowship of the Royal College of Surgeons, were originally limited to senior registrars. These rules prevented many of those in non-training grades from qualifying to progress. Once a senior registrar, depending on specialty, it could take anything from one to six years to go onto a permanent consultant or senior lecturer appointment. It might be necessary to obtain an M.D. or Ch. M.

Phil S. Baran (born August 10, 1977) is a synthetic organic chemist and Professor in the Department of Chemistry at the Scripps Research Institute. His work is focused on synthesizing complex natural products, the development of new reaction methodologies within synthetic organic electrochemistry, and the development of new reagents. He holds several patents and has authored over 300 research articles.

3-Glucuronidation to oxymorphone-3-glucuronide predominantly via UGT2B7 6-Ketoreduction to 6α-oxymorphol and 6β-oxymorphol N-Demethylation to noroxymorphone The first pathway of the above three accounts for 40% of the metabolism of oxymorphone, making oxymorphone-3-glucuronide the main metabolite of oxymorphone, while the latter two pathways account for less than 10% of the metabolism of oxymorphone. After N-demethylation of oxymorphone, noroxymorphone is further glucuronidated to noroxymorphone-3-glucuronide. Because oxycodone is metabolized by the cytochrome P450 system in the liver, its pharmacokinetics can be influenced by genetic polymorphisms and drug interactions concerning this system, as well as by liver function. Some people are fast metabolizers of oxycodone, while others are slow metabolizers, resulting in polymorphism-dependent alterations in relative analgesia and toxicity. While higher CYP2D6 activity increases the effects of oxycodone (owing to increased conversion into oxymorphone), higher CYP3A4 activity has the opposite effect and decreases the effects of oxycodone (owing to increased metabolism into noroxycodone and noroxymorphone). The dose of oxycodone must be reduced in patients with reduced liver function.

Sources: en.wikipedia.org

Background from the literature

Applications of antipsychotic drugs in the treatment of schizophrenia include prophylaxis for those showing symptoms that suggest that they are at high risk of developing psychosis; treatment of first-episode psychosis; maintenance therapy (a form of prophylaxis, maintenance therapy aims to maintain therapeutic benefit and prevent symptom relapse); and treatment of recurrent episodes of acute psychosis. A recent 2024 study found that using high doses of antipsychotics for schizophrenia was linked to a higher risk of mortality. Researchers analyzed data from 32,240 individuals aged 17 to 64 diagnosed with schizophrenia between 2002 and 2012 to arrive at this conclusion.

=== Introductory === Nelson DL, Cox MM (2004). Lehninger Principles of Biochemistry (4th ed.). W. H. Freeman. ISBN 0-7167-4339-6. Schneider ED, Sagan D (2006). Into the Cool: Energy Flow, Thermodynamics and Life (1st ed.). University of Chicago Press. ISBN 0-226-73937-6. Lane N (2006). Power, Sex, Suicide: Mitochondria and the Meaning of Life (1st ed.). Oxford University Press, USA. ISBN 0-19-920564-7.

Argentine President Cristina Fernández de Kirchner posthumously promoted her to the rank of general. Javiera Carrera was also a significant figure in the Chilean War of Independence, who used her family influence and status to form social groups of women to advocate for independence. Carrera sewed the first Chilean flag as a sign of their independence and endured imprisonment multiple times in her life as a result of her great contributions. She is seen as one of the main female figures in Chilean Independence. Another significant figure in documenting the experiences of women during the Independence Wars was Marquita Sanchez, also known as Madame Mendeville. Sanchez recorded many of her experiences during the Argentine Independence War while also recording accounts of her daily life as a female activist during this period in history. She also helped record several events and battles central to the Argentine military and their continued fighting against the Spanish. According to gender stereotypes, women were not meant to be soldiers; only men were supposed to engage in fighting and conflict. There were still plenty of women present on the battlefields to help rescue and nurse soldiers. Some women fought alongside their husbands and sons on the battlefield. The majority of women assumed supportive and non-competitive roles such as fundraising and caring for the sick. Revolution for women meant something different from for men. Women saw revolution as a way to earn equal rights, such as voting, and to overcome the suppression and subordination of women to men.

=== Biofilms formation and cyclic di-GMP === As in most Gram negative bacteria, P. aeruginosa biofilm formation is regulated by one single molecule: cyclic di-GMP. At low cyclic di-GMP concentration, P. aeruginosa has a free-swimming mode of life. But when cyclic di-GMP levels increase, P. aeruginosa start to establish sessile communities on surfaces. The intracellular concentration of cyclic di-GMP increases within seconds when P. aeruginosa touches a surface (e.g.: a rock, plastic, host tissues...). This activates the production of adhesive pili, that serve as "anchors" to stabilize the attachment of P. aeruginosa on the surface. At later stages, bacteria will start attaching irreversibly by producing a strongly adhesive matrix. At the same time, cyclic di-GMP represses the synthesis of the flagellar machinery, preventing P. aeruginosa from swimming. When suppressed, the biofilms are less adherent and easier to treat. The biofilm matrix of P. aeruginosa is composed of nucleic acids, amino acids, carbohydrates, and various ions. It mechanically and chemically protects P. aeruginosa from aggression by the immune system and some toxic compounds. P. aeruginosa biofilm's matrix is composed of up to three types of sugar polymers (or "exopolysaccharides") named PSL, PEL, and alginate. Which exopolysaccharides are produced varies by strain.

Adhesion is the tendency of dissimilar particles or surfaces to cling to one another. (Cohesion refers to the tendency of similar or identical particles and surfaces to cling to one another.) The forces that cause adhesion and cohesion can be divided into several types. The intermolecular forces responsible for the function of various kinds of stickers and sticky tape fall into the categories of chemical adhesion, dispersive adhesion, and diffusive adhesion. In addition to the cumulative magnitudes of these intermolecular forces, there are also certain emergent mechanical effects.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine also known as?

Cardarine is commonly known as GW501516 or GW-1516. These names refer to the same synthetic compound. It is not a brand-name approved medicine.

Is cardarine a steroid?

No, cardarine is not a steroid. It is classified as a PPARδ agonist. Its structure and receptor target differ from anabolic steroids.

Has cardarine been approved for human use?

No regulatory agency has approved cardarine as a medicine. It was investigated in early research but development was discontinued. It is not available as a prescription drug.

What did animal studies show?

Rodent studies reported increased endurance and fat oxidation after GW501516 exposure. Long-term studies also found higher rates of some tumors, which led to halted development.

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