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Cardarine As Investigational Pparδ Agonist — Background and Details

By Editorial Desk · published 2026-02-07 · last reviewed 2026-03-29 · Wiki

A practical reference on GW501516: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

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

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 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.

Notes from published material

The resulting force-displacement curves can be used to calculate elastic modulus. However, it is unclear whether particle size and indentation depth affect the measured elastic modulus of nanoparticles by AFM. Adhesion and friction forces are important considerations in nanofabrication, lubrication, device design, colloidal stabilization, and drug delivery. The capillary force is the main contributor to the adhesive force under ambient conditions. The adhesion and friction force can be obtained from the cantilever deflection if the AFM tip is regarded as a nanoparticle. However, this method is limited by tip material and geometric shape. The colloidal probe technique overcomes these issues by attaching a nanoparticle to the AFM tip, allowing control oversize, shape, and material. While the colloidal probe technique is an effective method for measuring adhesion force, it remains difficult to attach a single nanoparticle smaller than 1 micron onto the AFM force sensor. Another technique is in situ TEM, which provides real-time, high resolution imaging of nanostructure response to a stimulus. For example, an in situ force probe holder in TEM was used to compress twinned nanoparticles and characterize yield strength. In general, the measurement of the mechanical properties of nanoparticles is influenced by many factors including uniform dispersion of nanoparticles, precise application of load, minimum particle deformation, calibration, and calculation model. Like bulk materials, the properties of nanoparticles are materials dependent.

Humans commonly eat the livers of mammals, fowl, and fish as food. Domestic pig, ox, lamb, calf, chicken, and goose livers are widely available from butchers and supermarkets. In the Romance languages, the anatomical word for "liver" (French foie, Spanish hígado, etc.) derives not from the Latin anatomical term, jecur, but from the culinary term ficatum, literally "stuffed with figs", referring to the livers of geese that had been fattened on figs. Animal livers are rich in iron, vitamin A and vitamin B12; and cod liver oil is commonly used as a dietary supplement. Liver can be baked, boiled, broiled, fried, stir-fried, or eaten raw (asbeh nayeh or sawda naye in Lebanese cuisine, or liver sashimi in Japanese cuisine). In many preparations, pieces of liver are combined with pieces of meat or kidneys, as in the various forms of Middle Eastern mixed grill (e.g. meurav Yerushalmi). In the UK, kidney (including caul) was used alongside other organs like the lungs (known as "lights"), abdomen, heart was used as a poverty meal, which used up all of the animal. Other well-known examples include liver pâté, foie gras, chopped liver, and leverpastej. Liver sausages, such as Braunschweiger and liverwurst, are also a valued meal. Liver sausages may also be used as spreads. A traditional South African delicacy, skilpadjies, is made of minced lamb's liver wrapped in netvet (South African for caul fat), and grilled over an open fire. Traditionally, some fish livers were valued as food, especially the stingray liver.

methyl Also carbinyl. The alkyl functional group derived from methane, consisting of one carbon atom bonded to three hydrogen atoms, with the chemical formula CH3. It is the simplest hydrocarbon and occurs as a substituent in numerous organic compounds, though it may also exist independently as an ion or radical. In IUPAC nomenclature, the presence of a methyl substituent is indicated with the prefix methyl in the name of the compound, or with the abbreviation Me in chemical formulae; e.g. methyl alcohol (methanol) is often written with the formula CH3OH or MeOH.

== Structure == OmpT is a 33.5 kDa outer membrane protein consisting of 10 antiparallel strands that are connected by 5 extracellular loops. The antiparallel strands form a beta barrel structure that spans the width of the membrane, creating a pore. E. coli omptins can be coded either from the OmpT gene on a chromosome (part of a DLP12 prophage) or from OmpP on a plasmid (OmpP). The sequences resulting from these two sources differ by 24-25% in the mature protease. Genetic differences between OmpT and other members of the omptin family are found in the extracellular loops, and therefore, this area is thought to be associated with substrate specificity. Also, the barrel is relatively rigid, while the loops have more flexibility to bind to substrates of varying sizes.

Sources: en.wikipedia.org

Further detail

One of the major technical hurdles with immunoprecipitation is the great difficulty in generating an antibody that specifically targets a single known protein. To get around this obstacle, many groups will engineer tags onto either the C- or N- terminal end of the protein of interest. The advantage here is that the same tag can be used time and again on many different proteins and the researcher can use the same antibody each time. The advantages with using tagged proteins are so great that this technique has become commonplace for all types of immunoprecipitation, including all of the types of IP detailed above. Examples of tags in use are the green fluorescent protein (GFP) tag, glutathione-S-transferase (GST) tag and the FLAG-tag tag. While the use of a tag to enable pull-downs is convenient, it raises some concerns regarding biological relevance because the tag itself may either obscure native interactions or introduce new and unnatural interactions.

A summary of the atomic-scale molecular dynamics simulations is then provided which contains important information as follows: 1) a system number that corresponds to a particular phospholipid simulation 2) the concentration of ethanol mol% used in a particular simulation 3) the concentration of ethanol (v/v%) used for the simulation 3) the ethanol/lipid ratio that is derived from the simulation 4) the area (nm2) of the phospholipid membrane which details the expansion of the membranes as the concentration of ethanol is increased 5) the thickness of the membrane which is based on the distance between the average positions of the phosphorus atoms on opposite sides of the phospholipid membrane and 6) the tilt of the head group of the POPC lipid based on changes in the angle towards the interior region of the phospholipid membrane which was surprisingly not very significant.

== Recent extraditions == On 29 April 2024, prominent El Mencho associate Juan Manuel Abouzaid El Bayeh, also known as "El Escorpion," was arrested in Mexico and then immediately extradited to the United States. On 27 February 2025, Antonio Oseguera was among 29 suspected Mexican drug trafficking figures who were extradited to the United States. In August 2025, Mexico extradited 26 individuals accused of involvement in major drug-trafficking organizations, including the CJNG and the Sinaloa Cartel, to the United States. The extraditions were conducted under U.S. pressure, with assurances that the death penalty would not be pursued. This marked the second large-scale extradition of alleged cartel members in 2025, following a similar transfer in February. These actions reflect ongoing cooperation between Mexico and U.S. authorities in combating transnational organized crime. Among those extradited included the imprisoned head of CJNG's Los Cuinis fraction, Abigael González Valencia.

A. Ajayaghosh, born on 30 July 1962 in Kollam in the south Indian state of Kerala, graduated in science from the University of Kerala and completed his master's degree from Calicut university in 1984. Subsequently, working under the guidance of Prof. V. N. Rajasekharan Pillai, he secured a Ph.D. from University of Calicut in 1989; his thesis was on Solid-Phase Peptide Synthesis. His career started in 1988 at the Regional Research Laboratory, presently the National Institute for Interdisciplinary Science and Technology (NIIST), of the Council of Scientific and Industrial Research, as a Scientist and held various positions before promoting to an Outstanding Scientist (Scientist-H) and the head of the Photosciences and Photonics Group of NIIST. Subsequently he became the head of the Chemical Sciences and Technology group He was the director of the Institute from 2015 and held the additional responsibility as the Dean of Chemical Sciences, Academy of Scientific and Innovative Research (AcSIR) New Delhi. In between, he was as an Alexander von Humboldt Fellow at the Max Planck Institute for Strahlen Chemie, Germany during 1994–96. He served as an adjunct professor of Material Science Programme at the Indian Institute of Technology, Kanpur. Presently, he is a J. C. Bose National Fellow at CSIR-NIIST and an adjunct professor at IISER Thiruvananthapuram. Ajayaghosh is married to Ambili, and together they have two children, one of whom is Anantharaman Ajay, known for his roles in the 2023 movie "Romancham", Gaganachari, and the YouTube channel "Appooppan and the Boys","Nissaram".

Addition of antipsychotics, which are potent dopamine receptor antagonists, to SSRIs, has been found to significantly augment their effectiveness in the treatment of OCD. As such, besides strong serotonin reuptake inhibition, clomipramine at high doses might also block dopamine receptors to treat OCD symptoms, and this could additionally or alternatively be involved in its possible effectiveness advantage over SSRIs. For this reason, it may also be that augmentation with neuroleptics (a common procedure in the occurrence of inadequate response to monotherapy with an SRI) is needed with less frequency with clomipramine relative to SSRIs, the latter of-which apparently lack significant activity as dopamine-receptor antagonists. Although clomipramine is probably more effective in the treatment of OCD compared to SSRIs, it is greatly inferior to them in terms of tolerability and safety due to its lack of selectivity for the SERT and promiscuous pharmacological activity. In addition, clomipramine has high toxicity in overdose and can potentially result in death, whereas death rarely, if ever, occurs with overdose of SSRIs. It is for these reasons that clomipramine, in spite of potentially superior effectiveness to SSRIs, is now rarely used as a first-line agent in the treatment of OCD, with SSRIs being used as first-line therapies instead and clomipramine generally being reserved for more severe cases and as a second-line agent.

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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