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Cardarine Identity And Mechanism — Reference Sheet

By Editorial Desk · published 2026-07-29 · last reviewed 2026-08-01 · Guide

Cardarine comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.

Updated 2026-08-01. Numbers and descriptions here follow the published literature rather than marketing material.

Cardarine Identity and Mechanism

At the molecular level, GW501516 binds and activates PPARδ, a nuclear receptor that regulates transcription. Activation shifts expression of genes involved in fatty acid oxidation, energy expenditure, and lipid transport in skeletal muscle and liver. Animal studies report increased endurance and altered lipid profiles after exposure. Human data are limited to small trials and do not establish long-term safety or efficacy. PPARδ also has roles in cell proliferation, so the relationship between activation and cancer risk remains an open question.

Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.

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.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineAlso called GW501516 and endurobol.
Chemical formulaC21H18F3NO3S2Molecular weight about 453.5 g/mol.
AppearanceWhite to off-white solidForm depends on synthesis and purity.
SolubilitySoluble in DMSO and ethanolLow solubility in water.
Typical storage-20 °C, desiccated, protected from lightCommon for research chemicals.

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.

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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.

Further detail

== Previous studies == Phaeobacter sp. JL2886, a deep sea strain that was sequestered in 2012 from a sediment that was 2000 m deep in the South China sea, "was analyzed for its entire genome sequence". In another study, from 56 sediments collected from the deep sea (depth range 800–1500 m), "28 ᴅ-amino acid utilizers" were isolated, in Sagami Bay, Japan. Independent attempts to sequester micro-organisms that grow healthier, due to D-amino acids, has also been done. Most conducted studies and experiments usually also utilize mainly D-alanine, D-aspartate, and D-glutamate, as they signify the most common D-amino acids found in living organisms. Moreover, they also aid as nitrogen sources for many of the fundamental processes involved in the ocean.

=== Chromatography === Internal standards are used in GC/MS and LC/MS to control for variability introduced by injection, sample preparation and other matrix effects. The ratio of peak areas between the internal standard and analyte is calculated to determine analyte concentration. A common type of internal standard is an isotopically labeled analogue of the analyte, which incorporates one or more atoms of 2H, 13C, 15N and 18O into its structure.

In the 13th century, the category of reptile was recognized in Europe as consisting of a miscellany of egg-laying creatures, including "snakes, various fantastic monsters, lizards, assorted amphibians, and worms", as recorded by Beauvais in his Mirror of Nature. In the 18th century, the reptiles were, from the outset of classification, grouped with the amphibians. Linnaeus, working from species-poor Sweden, where the common adder and grass snake are often found hunting in water, included all reptiles and amphibians in class "III – Amphibia" in his Systema Naturæ. The terms reptile and amphibian were largely interchangeable, reptile (from Latin repere, 'to creep') being preferred by the French. J.N. Laurenti was the first to formally use the term Reptilia for an expanded selection of reptiles and amphibians basically similar to that of Linnaeus. Today, the two groups are still commonly treated under the single heading herpetology.

Sources: en.wikipedia.org

Supporting material

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== Mistaken portrait == For two centuries, until the discovery of the error in 2005, books, paintings and articles had incorrectly shown a profile portrait of the obscure French politician Louis Legendre (1752–1797) as a portrait of the mathematician. The error arose from the fact that the sketch was labelled simply "Legendre" and appeared in a book along with contemporary mathematicians such as Lagrange. One of only two known portraits of Legendre, rediscovered in 2008, is found in the 1820 book Album de 73 portraits-charge aquarellés des membres de I'Institut, a book of caricatures of seventy-three members of the Institut de France in Paris by the French artist Julien-Léopold Boilly as shown below. The other portrait is from the book Le Panthéon scientifique de la tour Eiffel.

Domino's sponsored CART's Doug Shierson Racing, which was driven by Arie Luyendyk and won the 1990 Indianapolis 500. In 2003, Domino's teamed up with NASCAR for a multi-year partnership to become the "Official Pizza of NASCAR". Domino's also sponsored Michael Waltrip Racing and driver David Reutimann during the 2007 season in the NASCAR Sprint Cup Series. In June 2018, Domino's announced that it had started a project to pave over cracks and potholes on roads in the United States called "Paving for Pizza" to prevent their pizzas from being ruined, giving cities and towns grants for road repairs. The company had reached an agreement with four cities and towns, including Burbank, California; Bartonville, Texas; Athens, Georgia; and Milford, Delaware, to pave their roads. The paved sections feature the Domino's logo along with the slogan "OH YES, WE DID".

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is a common name for the investigational compound GW501516. It acts as a PPARδ agonist and is not approved for human use. It is prohibited in sport.

How does cardarine work?

It activates PPARδ, a nuclear receptor that influences gene expression related to lipid and energy metabolism. Animal studies show changes in endurance and lipid levels. Human effects and risks are not well established.

Is cardarine a steroid?

No, cardarine is not a steroid. It belongs to a different chemical class, the PPARδ agonists. It is also not a selective androgen receptor modulator.

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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