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Cardarine As Investigational Pparδ Agonist — Background and Details

By Editorial Desk · published 2026-07-07 · last reviewed 2026-08-01 · Blog

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

This page was last updated on 2026-08-01 and is reviewed periodically as new material appears.

Cardarine as Investigational PPARδ Agonist

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.

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.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516, GW-501516, GW 501516, endurobolNames vary in research and anti-doping documents.
Chemical classSynthetic PPARδ agonistSmall-molecule nuclear receptor ligand.
CAS Registry Number317318-70-0Identifier commonly associated with GW501516.
AppearanceWhite to off-white powderTypical for purified research material.
SolubilityLow in water; soluble in DMSO and ethanolOrganic solvents are common for laboratory stock solutions.

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.

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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.

Regulation and Analytical Detection

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.

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.

Preclinical Findings and Safety Signals

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.

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.

Supporting material

Maternal behavior: Female rats given oxytocin antagonists after giving birth do not exhibit typical maternal behavior. By contrast, virgin female sheep show maternal behavior toward foreign lambs upon cerebrospinal fluid infusion of oxytocin, which they would not do otherwise. Oxytocin is involved in the initiation of human maternal behavior, not its maintenance; for example, it is higher in mothers after they interact with unfamiliar children rather than their own. Human ingroup bonding: Oxytocin can increase positive attitudes, such as bonding, toward individuals classified as "in-group" members, whereas other individuals become classified as "out-group" members. Oxytocin has also been implicated in lying when lying would prove beneficial to other in-group members. In a study where such a relationship was examined, it was found that when individuals were administered oxytocin, rates of dishonesty in the participants' responses increased for their in-group members when a beneficial outcome for their group was expected. Both of these examples show the tendency of individuals to act in ways that benefit those considered to be members of their social group, or in-group. Decreased oxytocin and receptor expression has been associated with aggressive behavior in aggressive-impulsive disorders. Oxytocin is not only correlated with individuals' preferences to associate with members of their own group, but it is also evident during conflicts between members of different groups.

== Risk factors == Although it is difficult to predict which individuals will be affected from drug-induced long QT syndrome, there are general risk factors that can be associated with the use of certain medications. Generally, as the dose of a drug increases, the risk of QT prolongation increases as well. In addition, factors such as rapid infusion, concurrent use of more than one drug known to prolong QT interval, diuretic treatment, electrolyte derangements (hypokalemia, hypomagnesemia, or hypocalcemia), advanced age, bradyarrhythmias, and female sex have all been shown to be risk factors for developing drug-induced QT prolongation. TdP has been shown to occur up to three times more often in female patients compared with males, likely as a result of post-pubertal hormonal influence on cardiac ion channels. The QTc interval is longer in females, as well as having a stronger response to IKr-blocking agents. In males, the presence of testosterone upregulates IKr channels and therefore decreases QT interval. Stated otherwise, estrogens prolong the QT interval, while androgens shorten it and decrease the response to IKr-blocking agents. Structural heart disease, such as heart failure, myocardial infarction, and left ventricular hypertrophy, are also risk factors. Diuretic-induced hypokalemia and/or hypomagnesemia taken for heart failure can induce proarrthymia. The ischemia that results from myocardial infarctions also induce QT prolongation.

== Analysis techniques == Age and compositional zonation as well as the texture of monazite provide evidence on the successive growth of the crystal during discrete geological events. The scope of information that can be obtained largely depends on the analysis techniques employed in geochronology.

=== Generic names === Methylestradiol has not been assigned an INNTooltip International Nonproprietary Name or other formal name designations. Its generic name in English and German is methylestradiol, in French is méthylestradiol, and in Spanish is metilestadiol. It is also known as 17α-methylestradiol.

Sources: en.wikipedia.org

Supporting material

Chains shoots and kills Nancy, then straps a bomb to Joe's chest and has him tied up in a helicopter on its way to the Capitol. Joe escapes and seizes control of the helicopter. Inside of the courtroom, Chains retrieves a hidden submachine gun and uses it to kill government agent Martinez, two security officers, all of the justices and Whipperton. Joe overpowers Chains and hands him over to the authorities. Chains frees himself and steals a revolver from an officer, aiming for Joe. Lance intervenes and shoots Chains twice, sending him tumbling over a railing to his death. Joe exits the courthouse as SWAT officers storm the building.

== Clinical trials == As of September 2024, traneurocin is in phase 3 clinical trials for COVID-19, phase 2 clinical trials for Alzheimer's disease, fragile X syndrome, and Rett syndrome, and phase 1 clinical trials for major depressive disorder. No development has been reported for treatment of other neurological disorders. Traneurocin was first developed, under the name cycloprolylglycine (CPG), in Russia in 1991 as a drug related structurally and pharmacologically to piracetam. Cycloprolylglycine is also related to and known to be the major metabolite of omberacetam (Noopept). Another drug, vineurocin (NA-704), is also being developed for treatment of Alzheimer's disease. This drug is described as a recombinant growth hormone with neuroprotective and neurogenic effects.

Calcitonin gene-related peptide 2 (CGRP2), also called calcitonin related polypeptide beta, is a hormone that in humans is encoded by the CALCB gene (previously CALC2). Like the related hormone, calcitonin gene-related peptide 1 (CGRP1), this hormone induces vasodilation (relaxation of blood vessels) through the activation of the CGRP receptor. This form of calcitonin gene-related peptide is traditionally considered to be the primary form used in the enteric nervous system (nervous system in the gut). The gene that encodes CGRP1, CALCA, also encodes the blood-calcium-reducing hormone calcitonin, but despite its name, this protein is encoded by a distinct gene (CALCB).

As a result of the Partition of India in 1947, the formations, units, assets, and indigenous personnel of the Indian Army were divided between the Dominion of India and the Dominion of Pakistan. As Brian Lapping wrote, "By comparison with the two great provinces [Bengal & Punjab], partition of the army and the civil service was easy, though by any other standard, it was difficult, wasteful, and destructive. ... The men were transferred in their units. Regiments of Sikh and Hindu soldiers from the north-west frontier had to make their way through Muslim territory to get out of what was to be Pakistan." Also in 1947 a final agreement was signed regarding the Gurkha regiments in the British Indian Army. Four Gurkha regiments, recruited from both eastern and western Nepal, would join the British Army. The remaining six Gurkha regiments of the British Indian Army joined the Dominion of India. During the transition period after partition, those Gurkha regiments that were in Pakistan, did their service, but were eventually moved back to India. The partition reduced the ethnic imbalance of the British Indian Army, which became the present-day Indian Army. But, the partition resulted in more ethnic imbalance in the Pakistani military, mainly because the new nation state of Pakistan was formed by joining West Punjab, NWFP, East Bengal, Baluchistan, and Sind. The new Pakistan Army was mainly made up of soldiers from two of these provinces. The Bangladesh Army, which was created from the Pakistan Army on the independence of Bangladesh, retain many British Indian Army traditions.

An independent 2024 assembly of the same strain using a new technique (PacBio HiFi) produced an extra 4.17 million base pairs total and 8.0 million base pairs on chromosome arms. In 2024, a near-complete "telomere-to-telomere" genome assembly was produced for D. melanogaster strain Canton S, closing 93.28% of gaps in the release 6 genome. This was enabled by a combination of PacBio HiFi, Oxford Nanopore ultra-long reads, and Hi-C data. It measured 161.63 million base pairs, though a lot of the increase relative to reference appear to reflect actual strain-to-strain variation (and not an error in the R6 genome). D. melanogaster originated in sub-Saharan Africa and populations diverged as the species expanded across the globe. As of 2024, there are more than 1439 genome sequences representing the global diversity of this species, allowing for a detailed estimate of its global evolutionary history.

Sources: en.wikipedia.org

Supporting material

== Research == Cocaine haptens are chemically modified derivatives of cocaine that retain key immunogenic features, allowing them to be attached to carrier proteins such as keyhole limpet hemocyanin or bovine serum albumin. This enables the immune system to recognize cocaine and produce anti-cocaine antibodies, which can bind cocaine in the bloodstream and prevent it from reaching the brain, thereby blocking its psychoactive effects. The cocaine esterase enzyme and redesigned versions of it have been studied as a potential treatment for cocaine addiction in humans. Coca tea has been explored as a supportive treatment for cocaine dependence. A study in Lima, Peru, found that using coca leaf infusion along with counseling reduced relapse rates and significantly increased the duration of abstinence among addicted individuals, suggesting that this approach may help prevent relapse during treatment. Recent research has also examined the use of prescription psychostimulants for cocaine dependence, following the Self-Medication Hypothesis. This hypothesis suggests that some individuals use cocaine to address underlying neurochemical or psychological issues. While some studies indicate that psychostimulant therapy may reduce cocaine use and cravings, the evidence is mixed and further research is needed. In animal studies, nicotine exposure in mice increases the likelihood of later cocaine use, with clear molecular changes in the brain.

Physical organic chemists use the mathematical foundation of chemical kinetics to study the rates of reactions and reaction mechanisms. Unlike thermodynamics, which is concerned with the relative stabilities of the products and reactants (ΔG°) and their equilibrium concentrations, the study of kinetics focuses on the free energy of activation (ΔG‡) -- the difference in free energy between the reactant structure and the transition state structure—of a reaction, and therefore allows a chemist to study the process of equilibration. Mathematically derived formalisms such as the Hammond Postulate, the Curtin-Hammett principle, and the theory of microscopic reversibility are often applied to organic chemistry. Chemists have also used the principle of thermodynamic versus kinetic control to influence reaction products.

=== Legal status === Risperidone was approved by the United States Food and Drug Administration (FDA) in 1993 for the treatment of schizophrenia. In 2003, the FDA approved risperidone for the short-term treatment of the mixed and manic states associated with bipolar disorder. In 2006, the FDA approved risperidone for the treatment of irritability in autistic children and adolescents. The FDA's decision was based in part on a study of autistic people with severe and enduring problems of violent meltdowns, aggression, and self-injury; risperidone is not recommended for autistic people with mild aggression and explosive behavior without an enduring pattern. On 22 August 2007, risperidone was approved as the only drug agent available for the treatment of schizophrenia in youths, ages 13–17; it was also approved that same day for the treatment of bipolar disorder in youths, ages 10–17, joining lithium. In December 2021, the Committee for Medicinal Products for Human Use of the European Medicines Agency recommended market authorization for Okedi, a long-acting depot injection of risperidone. Okedi was approved for the treatment of schizophrenia in adults for whom the tolerability and effectiveness of risperidone had already been established using an oral formulation. Long-acting depot injectable risperidone was approved for medical use in the European Union in February 2022.

The Scottish Government had wanted it delayed until after a separate hearing into determining the definition of a woman. 6 August – Five people are arrested when protestors interrupt the Men's Elite Road Race at Falkirk. The environmental protest group This Is Rigged claims responsibility. 7 August – Police Scotland confirms that the bodies of three hillwalkers have been found after they failed to return from a trip to Aonach Eagach Ridge in Glen Coe two days earlier. Education staff at ten local authorities who belong to the Unite union vote to take rolling industrial action after rejecting a pay offer from the Scottish Government. 8 August – Jamie Starrs is sentenced to ten and a half years in prison for the rape of Amber Gibson in June 2021, five months before she was murdered by her brother. 9 August – The names of several thousand people adopted as children going back 100 years are removed from the ScotlandsPeople website amid concerns over privacy and safety. 10 August – Social Security Scotland issues an apology over a staff quiz that included pictures of child killers. The Friday Fun Quiz asked staff to identify people called Ian from images, and includes pictures of Ian Brady and Ian Huntley. 11 August – At the High Court in Stirling, James White, the leader of one of Scotland's largest organised crime gangs who was extradited from Brazil to face trial, is sentenced to ten years in prison for series organised crime and firearms offences. 12 August – Police Scotland announces plans to cut civilian staff and freeze recruitment in order to maintain officer numbers.

Endogenous Originating from within an organism, tissue, or cell. In neuroscience, it typically refers to naturally occurring neurotransmitters or signaling molecules. Endorphins Endogenous opioid peptides that bind to opioid receptors and act as natural painkillers and mood enhancers. Engram A theoretical physical trace or biological substrate of memory in the brain. The term is used in memory research to describe the neural changes underlying a specific memory. Enteric nervous system A subdivision of the autonomic nervous system that governs the function of the gastrointestinal system. Sometimes called the "second brain." Epinephrine A hormone and neurotransmitter (also known as adrenaline) involved in the body’s fight-or-flight response. Produced in the adrenal medulla. EPSP (Excitatory Postsynaptic Potential) A depolarizing event in a postsynaptic neuron caused by the influx of positive ions, making the neuron more likely to fire an action potential. Equilibrium potential The membrane potential at which there is no net flow of a particular ion across the cell membrane. It can be calculated using the Nernst equation. Estrogen A steroid hormone that, in addition to reproductive functions, affects brain structure, cognition, and neuroprotection, particularly in areas such as the hippocampus. Evoked potential A measured electrical response of the nervous system to a specific sensory, motor, or cognitive stimulus, commonly recorded with EEG. Excitability The ability of a neuron or muscle cell to respond to a stimulus and generate an action potential.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

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.

Is cardarine a steroid?

No. Cardarine is not a steroid hormone; it targets the nuclear receptor PPARδ. Its classification in anti-doping rules differs from anabolic steroids, though it remains prohibited in sport.

Why was cardarine not developed further?

Early rodent studies reported tumor formation at multiple sites, which raised safety concerns. Sponsors stopped clinical development, and no approved human product exists.

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.

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