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Identity And Pharmacological Mechanism — Research Overview

By Editorial Desk · published 2026-06-06 · last reviewed 2026-06-21 · Guide

The short version of WADA Prohibited List fits in a sentence. The long version — which is the one that helps — is below.

This page was last updated on 2026-06-21 and is reviewed periodically as new material appears.

Identity and Pharmacological Mechanism

The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.

Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.

Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.

Detection, Regulation, and Quality Context

Regulatory treatment of cardarine differs by context and jurisdiction. In competitive sport, the World Anti-Doping Agency lists PPARδ agonists, including GW501516, as prohibited at all times. Outside sport, it lacks approval as a prescription medicine in major drug markets, and products sold for human consumption may be treated as unapproved drugs. Some countries also restrict importation or sale through general consumer protection and medicines laws. These classifications affect availability, testing, and legal risk without establishing therapeutic value.

Because cardarine is not an approved medicine, no pharmacopeial monograph defines its identity, purity, or storage requirements. Laboratories typically rely on in-house methods and reference standards when testing materials labeled as GW501516. Certificates of analysis may report purity and identity for a specific batch, but their scope varies and they do not guarantee safety or legal status. Independent verification can include high-performance liquid chromatography, mass spectrometry, nuclear magnetic resonance, and elemental analysis. The distinction between research chemical labeling and human use is significant because quality standards and oversight differ.

Cardarine at a glance

PropertyValueNotes
Chemical classSynthetic PPARδ agonistNot a steroid or a selective androgen receptor modulator.
Common synonymsCardarine, GW501516, GW-501516, endurobolNames vary by supplier and literature source.
AppearanceWhite to off-white powderConsistent with many small-molecule research chemicals.
SolubilityLow in water; soluble in DMSO and ethanolOften prepared in organic solvent for laboratory work.
Primary targetPPARδ (NR1C2)Nuclear receptor involved in lipid and energy metabolism.

Mechanism and Research Context

GW501516 acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in transcription of genes related to lipid handling and energy use. Activation of PPARδ can shift skeletal muscle toward greater fatty acid oxidation in animal models, which is one reason it drew interest for metabolic disease and exercise research. The exact downstream effects depend on tissue, species, dose, and duration. Human data are sparse, so many proposed benefits remain hypotheses rather than established clinical outcomes.

Laboratory studies have examined GW501516 in cell cultures and rodents for conditions such as dyslipidemia, insulin resistance, and obesity. Some trials in humans were initiated, but development was discontinued after preclinical findings raised concerns about cancer in certain models. Those findings do not prove that the compound causes cancer in people, but they contributed to regulatory caution. Later reviews often describe the evidence as preliminary and insufficient for assessing long-term safety.

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Preclinical Findings and Safety Signals

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.

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.

Further detail

=== Interchangeability of centipede species in clinical practices === Comparative studies on S. mutilans and S. mojiangica, a common substitute for the former, has found that in pharmacodynamics and toxicology, the two centipede species have similar effects, and is theoretically proved that S. mutilans can be replaced by S. mojiangica. The same study found that two species showed similar results in various fields, including effects on animal haemoglobin and weight, chromosomal aberration tests, anticonvulsive tests, effects on in vitro fungal and bacterial growth, and acute toxicity tests. The study also suggested both centipede species can be used in relatively large doses, as they were both low in acute and genetic toxicities. Although the two centipede species were shown to be interchangeable in clinical practices, their interchangeability in clinical application was again questioned by some researchers, as more recent studies suggested that centipede proteins have a major role in their clinical effects. Through proteomics, researchers had found that the venoms of S. monjiangica and S. mutilans are different in the number of overlapping sequences and precursors for proteins and peptides. In addition, unique precursors were also found in both species for proteins and peptide levels. As the species differ in protein and peptide level, researchers of this study concluded that the interchangeability of centipede species requires further evaluation.

DNA nanoball sequencing is a type of high throughput sequencing technology used to determine the entire genomic sequence of an organism. The company Complete Genomics uses this technology to sequence samples submitted by independent researchers. The method uses rolling circle replication to amplify small fragments of genomic DNA into DNA nanoballs. Unchained sequencing by ligation is then used to determine the nucleotide sequence. This method of DNA sequencing allows large numbers of DNA nanoballs to be sequenced per run and at low reagent costs compared to other high-throughput sequencing platforms. However, only short sequences of DNA are determined from each DNA nanoball which makes mapping the short reads to a reference genome difficult.

== Powers and abilities == Neo has carried, since his conception, the Matrix's source code known as the Prime Program. This gives him the ability to freely manipulate the simulated reality of the Matrix, similar to the authority a system administrator has over a given system. He manifests these abilities as various superhuman powers. The power Neo exhibits most often is akin to telekinesis in the Matrix. In that, he seems capable of manipulating any object in the Matrix through will alone. By focusing this ability upon himself, he can fly at amazing speeds and jump great distances. Whilst his speed is never specified, he flies from the Merovingian's mountain manor to the highway "500 miles due south" in a very short time. It can thus be extrapolated that if it took him roughly 10 minutes to fly from the château in the mountains to the freeway in the Mega City, he would have to have been flying at around 3,000 mph, or just shy of Mach 4. However, his speed of flight is further exemplified by his ability to escape explosions, and the sonic boom left in his wake has the power to overturn rows of heavy vehicles and reap massive destruction, indicating he can probably fly much faster than Mach 4 when pressed. He has used this ability multiple times to stop several bullets in mid flight, first against the Agents and again against the Merovingian. In addition to his abilities, Neo possesses superhuman strength and agility, and is near-invulnerable to most attacks.

== History == EFLM was created from the merger of two precursor organisations, The Federation of European Societies of Clinical Chemistry (FESCC), (a European representative of the International Federation of Clinical Chemistry and Laboratory Medicine, IFCC) and the European Community Confederation of Clinical Chemistry (EC4) at the EuroMedlab meeting in Amsterdam in 2007. Both precursor organizations arose in the 1970s. The increasing overlap between the European Union, represented by EC4 and FESCC, representing geographical Europe, meant that merger was appropriate.

Sources: en.wikipedia.org

Background from the literature

CEEs are naturally occurring estrane steroids. They are in conjugate form, as the sodium salts of the C17β sulfate esters. The estrogens in CEEs, in their unconjugated active forms, include bioidentical human estrogens like estradiol and estrone as well as equine-specific estrogens such as equilin and 17β-dihydroequilin. The equine estrogens differ from human estrogens in that they have additional double bonds in the B ring of the steroid nucleus. CEEs contain both 17β-estrogens like estradiol and 17β-dihydroequilin and the C17α epimers like 17α-estradiol and 17α-dihydroequilin.

== Preparation and use == Fruits can be dried whole (e.g., grapes, berries, apricot, plum), in halves, or as slices (e.g., mango, papaya, kiwi). Alternatively, they can be chopped after drying (e.g., dates), made into pastes, or concentrated juices. The residual moisture content can vary from small (3–8%) to substantial (16–18%), depending on the type of fruit. Fruits can also be spread out, dried and cut into strips in its puree form without the addition of sugar or fats with at least 50% moisture content as fruit leather, (see patent listed under the references section) or as a powder by spray or drum drying. They can be freeze dried. Fresh fruit is frozen and placed in a drying chamber under a vacuum. Heat is applied, and water evaporates from the fruit while it is still frozen. The fruit becomes very light and crispy and retains much of its original flavor. Dried fruit is widely used by the confectionery, baking, and sweets industries. Food manufacturing plants use dried fruits in various sauces, soups, marinades, garnishes, puddings, and food for infants and children. As ingredients in prepared food, dried fruit juices, purées, and pastes impart sensory and functional characteristics to recipes:

"Novel Liquid Crystalline Compounds and Polymers,"J.S. Bradshaw, M.L. Lee, K.E. Markides, and B.A. Jones. US Patent Number 4,864,033. Filed: November 27, 1985. Issued: February 1989. "Multi-Element Selective Radio Frequency Plasma Detector for Capillary Gas Chromatography, F. Yang, P. Farnsworth, R. Skelton, K.E. Markides, and M.L. Lee. U.S. Patent Application Serial No. 24,095. Filed: March 12, 1987. Issued: January 25, 1989. "Oligoethylene Oxide Substituted Siloxane Compounds and Polymers," J.S. Bradshaw, M.L. Lee, K.E. Markides, Filed: December, 1987. "Chiral Polysiloxane Compounds and Polymers," J.S. Bradshaw, M.L. Lee, K.E. Markides, Filed: January, 1988. Issued: June 1990. "Chromatographic Arylcarboxamide Polysiloxanes," J.S. Bradshaw, M.L. Lee, K.E. Markides, Filed: June, 1988. Issued: March 1990. "Novel Chiral Copolymers with Oligosiloxane Spacers," J.S. Bradshaw, B.E. Rossiter, B.J. Tarbet, D.F. Johnson, M.L. Lee, K.E. Markides, File No. 9393 CIP. Filed: March 1992. “Encapsulated Nanoparticles for Drug Delivery”, G. Jacobson, R.N. Zare, K.E. Markides, R.R. Shinde and C.H. Contag, File No. 11/748,408, Filed: May 14, 2007.

Sources: en.wikipedia.org

Reference notes

Angelicin synthase is a cytochrome P450 protein containing heme, isolated from parsnip. It uses molecular oxygen for the oxidation and requires a partner cytochrome P450 reductase for functional expression. This uses nicotinamide adenine dinucleotide phosphate.

=== DVD documentary === A DVD documentary is a documentary film of indeterminate length that has been produced with the sole intent of releasing it for direct sale to the public on DVD, which is different from a documentary being made and released first on television or on a cinema screen (a.k.a. theatrical release) and subsequently on DVD for public consumption. This form of documentary release is becoming more popular and accepted as costs and difficulty with finding TV or theatrical release slots increases. It is also commonly used for more "specialist" documentaries, which might not interest a wider TV audience. Examples are military, cultural arts, transport, sports, animals, etc.

== Environmental effects == Considering the volume of polyacrylamide produced, these materials have been heavily scrutinized with regards to environmental and health impacts. Polyacrylamide is of low toxicity but its precursor acrylamide is a neurotoxin and carcinogen. Thus, concerns naturally center on the possibility that polyacrylamide is contaminated with acrylamide. Considerable effort is made to scavenge traces of acrylamide from the polymer intended for use near food. Additionally, there are concerns that polyacrylamide may de-polymerise to form acrylamide. Under conditions typical for cooking, polyacrylamide does not de-polymerise significantly. The single claim that polyacrylamide reverts to acrylamide has been widely challenged. Polyacrylamide is most commonly partially biodegraded by the action of amidases, producing ammonia and polyacrylates. Polyacrylates are hard to biodegrade, but some soil microbe cultures have been shown to do so in aerobic conditions.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.

How does cardarine interact with the body?

It binds to and activates PPARδ, a nuclear receptor that regulates genes related to fatty acid oxidation and energy use. This activation alters transcription in tissues such as skeletal muscle and liver. The full range of downstream effects in humans is not fully established.

Is cardarine found naturally?

No, cardarine is not known to occur naturally in plants, animals, or humans. It is a synthetic molecule produced for laboratory research. Products labeled as cardarine should therefore be treated as manufactured chemicals with variable purity.

How is cardarine detected in anti-doping tests?

Anti-doping laboratories typically use LC-MS/MS to detect GW501516 and its metabolites in urine. The method is sensitive and can identify the compound at low concentrations. Detection depends on sample timing, metabolism, and the specific assay.

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