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Identity And Pharmacological Classification — Complete Guide

By Editorial Desk · published 2026-02-20 · last reviewed 2026-03-29 · Wiki

This is a working overview of GW501516, written for readers who want more than a one-paragraph summary but less than a textbook.

Reviewed 2026-03-29. Anything still debated is marked as such rather than presented as settled.

Identity and Pharmacological Classification

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.

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.

Background and Regulatory Status

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.

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 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.

Regulation and Detection

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 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.

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Mechanism and Detection

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 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.

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.

Supporting material

==== Accreditation and regulation ==== Training Institutions: Hospitals and medical centers must be accredited by NPMCN and/or WACP/WACS to offer residency programs. Medical and Dental Council of Nigeria (MDCN): MDCN regulates medical and dental practice in Nigeria, ensuring that residency training aligns with national standards.

=== Co-ingestion === Opioid overdoses are often associated with benzodiazepines, tranquilisers (e.g. xylazine) or alcohol use. Other central nervous system depressants, muscle relaxers, pain relievers, anti-convulsants, anxiolytics, treatment drugs of a psychoactive or epileptic variety or any other such drug with its active function meant to calm or mitigate neuronal signaling (barbiturates, etc.) can additionally cause a worsened condition with less likelihood of recovery cumulative to each added drug. This includes drugs less immediately classed to a slowing of the metabolism such as with GABAergic like GHB or glutamatergic antagonists like PCP or ketamine.

=== Neurodegenerative disorders === As suppression of autophagy has been indicated as a contributing factor in a variety of neurodegenerative disorders, including Alzheimer's disease, rapamycin has been proposed as a potential treatment for these conditions, although results suggest it may not be effective in all cases.

Sources: en.wikipedia.org

Supporting material

metaphase The stage of mitosis and meiosis that occurs after prometaphase and before anaphase, during which the centromeres of the replicated chromosomes align along the equator of the cell, with each kinetochore attached to the mitotic spindle.

== Mechanism of action == Hydroxycarbamide decreases the production of deoxyribonucleotides via inhibition of the enzyme ribonucleotide reductase by scavenging tyrosyl free radicals as they are involved in the reduction of nucleoside diphosphates (NDPs). Additionally, hydroxycarbamide causes production of reactive oxygen species in cells, leading to disassembly of replicative DNA polymerase enzymes and arresting DNA replication. In the treatment of sickle-cell disease, hydroxycarbamide increases the concentration of fetal hemoglobin. The precise mechanism of action is not yet clear, but it appears that hydroxycarbamide increases nitric oxide levels, causing soluble guanylyl cyclase activation with a resultant rise in cyclic GMP, and the activation of gamma globin gene expression and subsequent gamma chain synthesis necessary for fetal hemoglobin (HbF) production (which does not polymerize and deform red blood cells like the mutated HbS, responsible for sickle cell disease). Adult red cells containing more than 1% HbF are termed F cells. These cells are progeny of a small pool of immature committed erythroid precursors (BFU-e) that retain the ability to produce HbF. Hydroxyurea also suppresses the production of granulocytes in the bone marrow which has a mild immunosuppressive effect particularly at vascular sites where sickle cells have occluded blood flow.

=== 17 May === Russia claimed to have destroyed more than 100 air and naval drones over its western regions and in the Black Sea. Explosions were reported at petroleum facilities in Novorossiysk, while two people were reported killed in a drone strike in Belgorod Oblast. The Russian-installed Governor of Sevastopol, Mikhail Razvozhayev, said that the attack caused power outages in the city. Four people were killed and 31 were wounded in a Russian airstrike in Kharkiv. Two people were killed in a separate attack in Vovchansk, while one person was killed in Lyptsi. Police accused Russian soldiers in the town of using up to 40 civilian prisoners as human shields. The regional prosecutor's office also began a criminal proceeding on Russian soldiers allegedly executing a person in a wheelchair. Zelenskyy signed a bill into law permitting individuals convicted of minor offenses to serve in the Ukrainian military, as well as another bill that increases fines for draft dodgers fivefold. Zelenskyy reported the situation in Kharkiv had been "controlled" but not "stabilized". He also reported Ukraine has "about 25 percent" of the air defences needed to counter future Russian attacks, needing 120 to 130 F-16s or other advanced aircraft to achieve air "parity" with Russia.

Sources: en.wikipedia.org

Notes from published material

=== Television === Coatsworth is Nine Network's Medical Expert appearing regularly as a guest on Nine Network programmes. He is presenter of a Nine Network television show he created, Do You Want To Live Forever? which he hosts with Tracey Grimshaw. He has been a guest on multiple television programs including:

Conduction velocity The speed at which an action potential travels along a nerve fiber. It is influenced by factors such as axon diameter and myelination. Consciousness A state of awareness of self and the environment. In neuroscience, it involves the coordinated activity of multiple brain regions, particularly the thalamocortical system. Corpus callosum The largest white matter structure in the brain, consisting of a thick band of axons that connects the left and right cerebral hemispheres. Cortical column A vertically organized group of neurons in the cerebral cortex that processes the same type of information, such as orientation or location in space. It is a basic functional unit of the cortex. Cortical plasticity The ability of the cerebral cortex to adapt and reorganize in response to experience, learning, or injury. Corticospinal tract A major descending pathway from the motor cortex to the spinal cord that mediates voluntary motor control, especially fine movements of the limbs. Creutzfeldt–Jakob disease (CJD) A rare and fatal neurodegenerative disorder caused by misfolded prion proteins. It leads to rapid cognitive decline, motor dysfunction, and ultimately death. Critical period A developmental window during which the nervous system is particularly sensitive to certain environmental stimuli, crucial for proper development of functions such as vision and language. Cross modal plasticity The ability of one sensory modality to reorganize and compensate in another’s absence (e.g., visual cortex being recruited for touch in individuals who are blind).

==== Other consequences ==== In contrast to adults, excessive daytime sleepiness (EDS) is not the most commonly reported symptoms in children with OSA. However, using objective questionnaires, it is possible to notice that the frequency of EDS in children is higher than what is reported by the parents or caretakers (40–50%). And the risk for EDS is even increased when OSA is associated with obesity. Due to the consequences and symptoms it generates, OSA in children leads to a significant decrease in quality of life, the decrease being even higher when obesity is present. The quality of life can however be improved with the treatment of OSA. SDB have also been linked to a higher rate of internalizing disorders such as anxiety and depression. Indeed, depressive symptoms have shown to be higher in children with OSA, especially in males. Once again, the severity of depressive symptoms is positively correlated with the severity of the SDB. It also interacts with obesity as obese children have higher risk to show depressive symptoms and obesity can cause OSA. The link can also go the other way around with the depression inducing obesity (due to overeating) which worsens the OSA. Adenotonsillectomy can decrease the intensity of the depressive symptoms. Other consequences of a disturbed sleep in children with OSA comprise anhedonia increased fatigue and decreased interest in daily activities, which in turn can affect the child's social relationships.

The outermost wall of the organ is known as the parietal layer The skin of the organ is known as the visceral layer. The organs have specialized names for their visceral fasciae. In the brain, they are known as meninges; in the heart they are known as pericardia; in the lungs, they are known as pleurae; and in the abdomen, they are known as peritonea. Visceral fascia is less extensible than superficial fascia. Due to its suspensory role for the organs, it needs to maintain its tone rather consistently. If it is too lax, it contributes to organ prolapse, yet if it is hypertonic, it restricts proper organ motility.

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.

Is cardarine approved for human use?

No. Major drug regulators have not approved GW501516 for treating any medical condition. Products sold as cardarine are typically unapproved research chemicals or supplements, so their contents and safety are not assured.

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