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Background And Regulatory History — Reference Sheet

By Editorial Desk · published 2026-02-05 · last reviewed 2026-02-26 · Blog

This is a working overview of GW501516, written for readers who want more than a one-paragraph summary but less than a textbook.

This page was last updated on 2026-02-26 and is reviewed periodically as new material appears.

Background and Regulatory History

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.

Cardarine is a common name for the investigational chemical GW501516, also written GW-1516. It was developed as a peroxisome proliferator-activated receptor delta agonist for metabolic conditions such as dyslipidemia. Early research focused on lipid handling and energy use in skeletal muscle and other tissues. The compound was never approved as a medicine. In public discussion, it is often grouped with performance-enhancing substances, although its receptor target differs from that of anabolic steroids or selective androgen receptor modulators. Regulatory and health authorities have issued warnings about its use.

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.

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.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineCommon internet and media name.
Research codeGW501516Also written GW-1516.
Drug classPPARδ agonistNot a selective androgen receptor modulator.
Development statusDiscontinuedClinical development halted after rodent cancer findings.
Regulatory statusProhibited in sportListed by WADA; not approved as medicine.

Background and Regulatory Status

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.

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.

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Regulatory Status and Detection Context

Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.

Analytical laboratories typically identify cardarine and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is a common matrix in anti-doping testing, while blood and tissue may be used in research settings. Detection windows depend on the assay, the sample matrix, and the compound's metabolism. Because cardarine is extensively metabolized, laboratories often target specific metabolites to improve sensitivity and confirmation. Reference standards are required for reliable quantification. Method validation includes checks for selectivity, linearity, and carryover.

Further detail

=== Sultanate and Kingdom of Egypt (1915–1953) === Brigadier Peter Acland (4th class), 1936 Sir Pratap Singh of Idar (Grand Cordon), 1918 Judge Sir Maurice Amos (Grand Cordon) Maharaja Jagatjit Singh Bahadur of Kapurthala (Grand Cordon), 1924 Major Henry Beaumont (4th Class), 1916 Rear Admiral Richard Bevan (4th Class), 1919 Field Marshall Lord Birdwood Lieutenant General Louis Bols Lieutenant Colonel Arthur Borton VC, DSO (3rd Class) Howard Carter, British archaeologist and Egyptologist (3rd Class), 1926 Jovan Dučić Major Aubrey Faulkner Major General Harold Franklyn, Commandant Sudan Defence Force, 1939 Major Harry Gardner (4th Class), 1922 Lieutenant Colonel Alexander Kearsey (3rd Class) Harold Knox-Shaw, British astronomer Lancelot Lowther, 6th Earl of Lonsdale, 1920 Naguib Pasha Mahfouz, obstetrician and gynecologist, 1919 Lieutenant Colonel Cecil L'Estrange Malone David McAllister, Engineer-in-Chief, Egyptian State Railways, (3rd Class), 1916 Earl Mountbatten of Burma, (fourth class), 1922 Charles Paget, 6th Marquess of Anglesey, 1915 General Sir William Peyton (2nd Class), 1916 General Hussein Refki Pasha (Grand Cordon) Admiral of the Fleet The Earl of Cork and Orerry, 3rd class (1916) Admiral Francis Mitchell (Royal Navy officer) Rear Admiral Eric Gascoigne Robinson Captain George Francis Scott Elliot Dr. Hassan Omar Shaheen – Professor of ENT Kasr El-Aini Hospital, Cairo. Circa 1920 Major-General Sir Charlton Watson Spinks, last Sirdar of Egypt (Grand Cordon), 1931 Dr.

C6H5C(O)CH(NOSO2H) + 2 H2O → C6H5C(O)CHO + NH4HSO4 It may also be prepared from methyl benzoate by a reaction with potassium dimsyl to give an intermediate β-ketosulfoxide, which undergoes a Pummerer-type rearrangement, followed by oxidation by with copper(II) acetate. Alternatively, it can also be prepared by oxidation of acetophenone with selenium dioxide.

Leading up to the passing of the laws, there was fierce opposition to them, above all by the FDP, the rising German student movement, a group calling itself Notstand der Demokratie ("Democracy in a State of Emergency") and the labour unions. Demonstrations and protests grew in number, and in 1967 the student Benno Ohnesorg was shot in the head by a policeman. The press, especially the tabloid Bild-Zeitung newspaper, launched a campaign against the protesters. By 1968, a stronger desire to confront the Nazi past had come into being. In the 1970s environmentalism and anti-nationalism became fundamental values among left-wing Germans. As a result, in 1979 the Greens were able to reach the 5% minimum required to obtain parliamentary seats in the Free Hanseatic City of Bremen state election, and with the foundation of the national party in 1980 developed into one of the most politically successful green movements in the world. Another result of the unrest in the 1960s was the founding of the Red Army Faction (RAF). The RAF was active from 1968, carrying out a succession of terrorist attacks in West Germany during the 1970s. Even in the 1990s, attacks were still being committed under the name RAF. The last action took place in 1993, and in 1998 the group announced it was ceasing activities.

==== MeSH D12.776.624.776.355 – cyclin-dependent kinase inhibitor proteins ==== MeSH D12.776.624.776.355.100 – cyclin-dependent kinase inhibitor p15 MeSH D12.776.624.776.355.200 – cyclin-dependent kinase inhibitor p16 MeSH D12.776.624.776.355.300 – cyclin-dependent kinase inhibitor p18 MeSH D12.776.624.776.355.400 – cyclin-dependent kinase inhibitor p19 MeSH D12.776.624.776.355.500 – cyclin-dependent kinase inhibitor p21 MeSH D12.776.624.776.355.600 – cyclin-dependent kinase inhibitor p27 MeSH D12.776.624.776.355.700 – cyclin-dependent kinase inhibitor p57

Specifically, flutamide and particularly its major metabolite hydroxyflutamide inhibit enzymes in the mitochondrial electron transport chain in hepatocytes, including respiratory complexes I (NADH ubiquinone oxidoreductase), II (succinate dehydrogenase), and V (ATP synthase), and thereby reduce cellular respiration via ATP depletion and hence decrease cell survival. Inhibition of taurocholate (a bile acid) efflux has also been implicated in flutamide-induced hepatotoxicity. In contrast to flutamide and hydroxyflutamide, which severely compromise hepatocyte cellular respiration in vitro, bicalutamide does not significantly do so at the same concentrations and is regarded as non-mitotoxic. It is thought that the nitroaromatic group of flutamide and hydroxyflutamide enhance their mitochondrial toxicity; bicalutamide, in contrast, possesses a cyano group in place of the nitro moiety, greatly reducing the potential for such toxicity. The hepatotoxicity of flutamide appears to depend on hydrolysis of flutamide catalyzed by an arylacetamide deacetalyse enzyme. This is analogous to the hepatotoxicity that occurs with the withdrawn paracetamol (acetominophen)-related medication phenacetin. In accordance, the combination of paracetamol (acetaminophen) and flutamide appears to result in additive to synergistic hepatotoxicity, indicating a potential drug interaction. Hepatotoxicity with flutamide may be cross-reactive with that of cyproterone acetate.

Sources: en.wikipedia.org

Background from the literature

=== Music === As Chocolate Droppa, his alias, he signed to Motown Records and released Kevin Hart: What Now? (The Mixtape Presents Chocolate Droppa), the soundtrack to his stand-up film of the same name. He released the singles "Push It On Me" featuring Trey Songz and "Baller Alert" with Migos & T.I.

Eggshells, snail shells and most seashells are predominantly calcium carbonate and can be used as industrial sources of that chemical. Oyster shells have experienced recognition as a source of dietary calcium since the early 2010s, but also remain a practical industrial source. Dark green vegetables such as broccoli and kale contain dietarily significant amounts of calcium carbonate, but they not practical as an industrial source. Annelids in the family Lumbricidae, earthworms, possess a regionalization of the digestive track called calciferous glands, Kalkdrüsen, or glandes de Morren, that processes calcium and CO2 into calcium carbonate, which is later excreted into the dirt. The function of these glands is unknown but is believed to serve as a CO2 regulation mechanism within the animals' tissues. This process is ecologically significant, stabilizing the pH of acid soils.

== History == The first report of angiogenesis can be traced back to the book A treatise on the blood, inflammation, and gun-shot wounds published in 1794, where Scottish anatomist John Hunter's research findings were compiled. In his study, Hunter observed the growth process of new blood vessels in rabbits. However, he did not coin the term "Angiogenesis," which is now widely used by scholars. Hunter also erroneously attributed the growth process of new blood vessels to the effect of an innate vital principle within the blood. The term "angiogenesis" is believed to have emerged not until the 1900s. The inception of modern angiogenesis research is marked by Judah Folkman's report on the pivotal role of angiogenesis in tumor growth.

=== NAD+ pptimization === 1-MNA is an inhibitor of nicotinamide N-methyltransferase (NNMT). By inhibiting NNMT activity, it regulates NAD+ biosynthesis via the nicotinamide salvage pathway, the primary route for NAD+ synthesis in mammals. By participating in this pathway, 1-MNA optimizes NAD+ levels.

Sources: en.wikipedia.org

Reference notes

Species of Capsicum that produce chili peppers are shown on the simplified phylogenetic tree, with examples of cultivars: The World Vegetable Center has one of the largest collection of chili peppers in the world. It has researched climate change resistant cultivars.

These neurosteroid metabolites of progesterone have relatively short biological half-lives in circulation. Because of this, there are dramatic and highly supraphysiological spikes in allopregnanolone and pregnanolone concentrations followed by steep declines with each oral intake of progesterone. As such, neurosteroid levels fluctuate substantially (e.g., 15-fold in the case of allopregnanolone) and in an unphysiological manner with oral progesterone therapy. In addition, consumption of food with oral progesterone increases its absorption by 2-fold, and this may also further amplify fluctuations in neurosteroid levels, particularly if food intake with progesterone is not consistent from dose to dose. In contrast to oral administration, parenteral progesterone, such as with vaginal administration, avoids the first-pass effect, and is not associated with supraphysiological levels of neurosteroid metabolites, nor with spikes or marked fluctuations in neurosteroid levels. Parenteral routes can be used instead of oral administration to avoid adverse effects related to neurosteroid fluctuations if they prove to be problematic. Lower doses of oral progesterone (e.g., 100 mg/day) are also associated with relatively reduced formation of neurosteroid metabolites, and may similarly help to alleviate such side effects. In addition, the 5α-reductase inhibitor dutasteride, which blocks the production of allopregnanolone (though not of pregnanolone) from progesterone, has been found to diminish symptoms of premenstrual syndrome.

=== 18 July === General al-Burhan ordered the SAF's withdrawal from Khartoum as part of efforts to end looting. The European Union imposed sanctions on SAF commander Abuqala Mohamed Kaikal, RSF commander Hussein Barsham and the firms Al-Khaleej Bank and Red Rock Mining.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a selective androgen receptor modulator?

No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.

Why did clinical development stop?

Preclinical rodent studies reported cancers, including liver and bladder tumors, at tested doses. The human relevance of those findings is uncertain, but development was discontinued. No approved human product resulted.

Is cardarine approved for medical use?

No. It remains an investigational compound without approved therapeutic labeling. Sports regulators prohibit its use, and health agencies have warned against consuming it.

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.

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