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Background And Regulatory Status — Research Overview

By Editorial Desk · published 2026-07-23 · last reviewed 2026-08-01 · Wiki

This is a working overview of LC-MS/MS, 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.

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.

Regulation and Detection

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
IUPAC name{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acidSystematic name for GW501516
CAS Registry Number317318-70-0Unique identifier for the parent compound
Molecular formulaC21H18F3NO3S2Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur
Molecular weight453.5 g/molApproximate value for the neutral form
AppearanceWhite to off-white powderTypical description for purified laboratory material

Mechanism and Detection

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.

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

Related pages on this site

Cardarine as Investigational PPARδ Agonist

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.

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.

Background and Research Context

In laboratory settings, cardarine is studied as a tool compound for probing PPARδ biology. Published experiments often use cell cultures, rodent models, or isolated tissues. Some investigations focus on metabolic effects, while others assess potential risks such as carcinogenicity observed in long-term animal studies. Because human trials are sparse, most knowledge comes from preclinical work and adverse event reports. Scientific literature frequently notes the gap between animal findings and human outcomes. The compound is not a dietary supplement and is not intended for human consumption.

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

Background and Regulatory History

GW501516 acts on PPARδ, a nuclear receptor that helps regulate fatty acid oxidation and energy homeostasis. In animal studies, activation of this receptor was associated with increased endurance and changes in lipid metabolism. Human trials examined effects on blood lipids and other metabolic markers, but the compound did not advance to approval. Rodent studies later reported tumors in multiple tissues at doses used in those experiments. Whether those findings translate to human risk remains uncertain, and the clinical relevance of the animal data is still debated.

Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.

Reference notes

== Championships and accomplishments == Konfrontacja Sztuk Walki Knockout of the Night (Two times) vs. Rolles Gracie Jr. and Michał Materla Most wins in Konfrontacja Sztuk Walki heavyweight history (17). Most knockouts in Konfrontacja Sztuk Walki heavyweight history (12). Most knockouts in Konfrontacja Sztuk Walki history (12). Most consecutive knockouts in Konfrontacja Sztuk Walki history (5). Third most wins in Konfrontacja Sztuk Walki history (17). Third most fights in Konfrontacja Sztuk Walki history (24). World MMA Awards 2021 Upset of the Year - Nominee

== Connective tissue membrane == The connective tissue membrane is formed solely from connective tissue. These membranes encapsulate organs, such as the kidneys, and line our movable joints. A synovial membrane is a type of connective tissue membrane that lines the cavity of a freely movable joint. For example, synovial membranes surround the joints of the shoulder, elbow, and knee. Fibroblasts in the inner layer of the synovial membrane release hyaluronan into the joint cavity. The hyaluronan effectively traps available water to form the synovial fluid, a natural lubricant that enables the bones of a joint to move freely against one another without much friction. This synovial fluid readily exchanges water and nutrients with blood, as do all body fluids.

Whey is left over when milk is coagulated during the process of cheese production. Coagulation can happen by adding acid or rennet. It is a 5% solution of lactose in water and contains the water-soluble proteins of milk as well as some lipid content. Processing can be done by simple drying, or the relative protein content can be increased by removing the lactose, lipids and other non-protein materials. The main method to extract protein from whey is membrane filtration. A variety of membrane pore sizes can be used to selectively let different components of whey go through or be retained. Whey can be passed through "microfiltration" which blocks bacteria, casein micelles, and fat, then passed through "ultrafiltration" (UF) which blocks proteins. The part that does not go through UF is spray-dried into a concentrated whey protein. There are also other ways to concentrate protein using filtration membranes. Ion exchange chromatography is another major method for whey protein extraction. Methods in development include aqueous two-phase extraction and magnetic separation.

=== Distinguishing anatomical features === While recent discoveries have made it more difficult to present a universally agreed-upon list of their distinguishing features, nearly all dinosaurs discovered so far share certain modifications to the ancestral archosaurian skeleton, or are clearly descendants of older dinosaurs showing these modifications. Although some later groups of dinosaurs featured further modified versions of these traits, they are considered typical for Dinosauria; the earliest dinosaurs had them and passed them on to their descendants. Such modifications, originating in the most recent common ancestor of a certain taxonomic group, are called the synapomorphies of such a group.

Sources: en.wikipedia.org

Reference notes

Both religions revere John the Baptist, Saint George, and Elijah. Druze, believe that Elijah came back as John the Baptist, or as Saint George, since they belief in reincarnation and the transmigration of the soul, Druze believe that El Khidr and John the Baptist and Saint George are one and the same. Elijah is a central figure of Druzism, and he considered patron of the Druze people. Due to the Christian influence on the Druze faith, two Christian saints become the Druze's favorite venerated figures: Saint George and the Prophet Elijah. Thus, in all the villages inhabited by the Druze and Christians in central Mount Lebanon, a Christian church or Druze maqam is dedicated to either the Prophet Elijah or Saint George. The reverence for Saint George, who is often identified with Al-Khidr, is deeply integrated into various aspects of Druze culture and religious practices. According to scholar Ray Jabre Mouawad, the Druze appreciated the two saints for their bravery, Saint George because he confronted the dragon and the Prophet Elijah because he competed with the pagan priests of Baal and won over them. In both cases the explanations provided by Christians are that Druzes were attracted to warrior saints that resemble their own militarized society. The Druze environment influenced in turn the Christians, and Christians living among Druze started to adopt the same word for some of their churches, using maqām instead of kanīsah (church). Saint George is seen as a guardian of the Druze community and a symbol of their enduring faith and resilience.

Dextranomer (trade name Debrisan, Exudex) is a cicatrizant used in dressings for wound healing, and in pharmaceutical products to treat fecal incontinence. It consists of dextran polymer chains cross-linked into a three-dimensional network.

=== Active site === The cleft between GALE's N- and C-terminal domains constitutes the enzyme's active site. A conserved Tyr-X-X-X Lys motif is necessary for GALE catalytic activity; in humans, this motif is represented by Tyr 157-Gly-Lys-Ser-Lys 161, while E. coli GALE contains Tyr 149-Gly-Lys-Ser-Lys 153. The size and shape of GALE's active site varies across species, allowing for variable GALE substrate specificity. Additionally, the conformation of the active site within a species-specific GALE is malleable; for instance, a bulky UDP-GlcNAc 2' N-acetyl group is accommodated within the human GALE active site by the rotation of the Asn 207 carboxamide side chain.

Under the partitioning powers, economic diversification and progress, including large-scale industrialisation, were introduced in the traditionally agrarian Polish lands, but this development turned out to be very uneven. Advanced agriculture was practiced in the Prussian Partition, except for Upper Silesia, where the coal-mining industry created a large labor force. The densest network of railroads was built in German-ruled western Poland. In Russian Congress Poland, a striking growth of industry, railways and towns took place, all against the background of an extensive, but less productive agriculture. The industrial initiative, capital and know-how were provided largely by entrepreneurs who were not ethnic Poles. Warsaw (a metallurgical center) and Łódź (a textiles center) grew rapidly, as did the total proportion of urban population, making the region the most economically advanced in the Russian Empire (industrial production exceeded agricultural production there by 1909). The coming of the railways spurred some industrial growth even in the vast Russian Partition territories outside of Congress Poland. The Austrian Partition was rural and poor, except for the industrialized Cieszyn Silesia area. Galician economic expansion after 1890 included oil extraction and resulted in the growth of Lemberg (Lwów, Lviv) and Kraków. Economic and social changes involving land reform and industrialization, combined with the effects of foreign domination, altered the centuries-old social structure of Polish society.

Mexico's tequila protection interests were prominent during the Chinese accession negotiations to the World Trade Organization. In accordance with WTO accession regulations, in order to gain considerations for WTO membership, China had to sign bilateral agreements with all existing members, including Mexico. Since China has a climatic condition suitable for blue agave plants, Mexico was worried about rival pseudo tequilas from China. The Mexican authorities took the opportunity of the bilateral negotiations with China to ensure that the latter accepted tequila as a geographically indicated product.

Sources: en.wikipedia.org

Frequently asked questions

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.

Why is cardarine banned in sport?

It is prohibited by the World Anti-Doping Agency as a hormone and metabolic modulator. Athletes who test positive for GW501516 can face sanctions, including suspensions and loss of results.

What is the difference between cardarine and GW501516?

Cardarine is a common or trade-style name, while GW501516 is the research code for the same chemical entity. Some sources also use Endurobol or GSK-516. The names refer to the same compound, not distinct drugs.

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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