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Background And Regulatory Status — 2026 Update

By Editorial Desk · published 2026-07-07 · last reviewed 2026-07-24 · Wiki

GW501516 raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.

This page was last updated on 2026-07-24 and is reviewed periodically as new material appears.

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.

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
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

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.

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Regulatory Status and Detection Context

A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.

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.

Reference notes

The lightweight chain of a bicycle with derailleur gears can snap (or rather, come apart at the side-plates, since it is normal for the "riveting" to fail first) because the pins inside are not cylindrical, they are barrel-shaped. Contact between the pin and the bushing is not the regular line, but a point which allows the chain's pins to work its way through the bushing, and finally the roller, ultimately causing the chain to snap. This form of construction is necessary because the gear-changing action of this form of transmission requires the chain to both bend sideways and to twist, but this can occur with the flexibility of such a narrow chain and relatively large free lengths on a bicycle. Chain failure is much less of a problem on hub-geared systems since the chainline does not bend, so the parallel pins have a much bigger wearing surface in contact with the bush. The hub-gear system also allows complete enclosure, a great aid to lubrication and protection from grit.

Pseudomonas fluorescens is a common Gram-negative, rod-shaped bacterium. It belongs to the Pseudomonas genus; 16S rRNA analysis as well as phylogenomic analysis has placed P. fluorescens in the P. fluorescens group within the genus, to which it lends its name.

== Prognosis == The prognosis is quite dire, with early death usual. In fact, most patients die in their first year except in milder forms of the disease, but few are known to have lived longer. The variation is unsurprising given the diversity of mutations causing the disease.

=== Metabolism === The metabolism of progesterone is rapid and extensive, and it occurs mainly in the liver, though enzymes that metabolize progesterone are also expressed widely in the brain, skin, and various other extrahepatic tissues. Progesterone has an elimination half-life of only approximately five minutes in circulation. The metabolism of progesterone is complex, and it may form as many as 35 different unconjugated metabolites when it is ingested orally. Progesterone is highly susceptible to enzymatic reduction via reductases and hydroxysteroid dehydrogenases because of its double bond (between the C4 and C5 positions) and its two ketones (at the C3 and C20 positions). The major metabolic pathway of progesterone is reduction by 5α-reductase and 5β-reductase, into the dihydrogenated 5α-dihydroprogesterone and 5β-dihydroprogesterone, respectively. This is followed by the further reduction of these metabolites via 3α-hydroxysteroid dehydrogenase and 3β-hydroxysteroid dehydrogenase into the tetrahydrogenated allopregnanolone, pregnanolone, isopregnanolone, and epipregnanolone. Subsequently, 20α-hydroxysteroid dehydrogenase and 20β-hydroxysteroid dehydrogenase reduce these metabolites to form the corresponding hexahydrogenated pregnanediols (eight different isomers in total), which are then conjugated via glucuronidation and/or sulfation, released from the liver into circulation, and excreted by the kidneys into the urine.

As the first woman since 1964 to win the Nobel Prize in chemistry, and the first since Dorothy Crowfoot Hodgkin, 45 years previously. She was also the fourth of eight women ever to win the Nobel Prize in chemistry. Although Yonath once remarked, “I am a scientist, not male or female. A scientist,” her 2009 award was noted as a highlight for female scientists. The Australian noted that Yonath's Nobel win was "crushing the lab's glass ceiling". Regarded as an influential Israeli scientist, Yonath helped established the first protein crystallography laboratory in Israel. In 2018, while interviewing Yonath, UNESCO noted that her scientific research has also been "key to understanding how antibiotics work". Following her death, The New York Times noted that Yonath's mapping of the ribosome led to new designs for antibiotics. Her work was noted as "boundary pushing" with it having "immediate and practical consequences" for medicine and in the "fight against infectious disease". President Isaac Herzog noted Yonath as "one of the leading researchers in the history of Israeli science". The Hindu also noted Yonath's academic impact, especially in India through her engagements in academic institutions in the country.

Sources: en.wikipedia.org

Notes from published material

Gas chromatography (GC) is a common type of chromatography used in analytical chemistry for separating and analyzing compounds that can be vaporized without decomposition. Typical uses of GC include testing the purity of a particular substance or separating the different components of a mixture. In preparative chromatography, GC can be used to prepare pure compounds from a mixture. Gas chromatography is also sometimes known as vapor-phase chromatography (VPC), or gas–liquid partition chromatography (GLPC). These alternative names, as well as their respective abbreviations, are frequently used in scientific literature. Gas chromatography is the process of separating compounds in a mixture by injecting a gaseous or liquid sample into a mobile phase, typically called the carrier gas, and passing the gas through a stationary phase. The mobile phase is usually an inert gas or an unreactive gas such as helium, argon, nitrogen or hydrogen. The stationary phase can be solid or liquid, although most GC systems today use a polymeric liquid stationary phase. The stationary phase is contained inside of a separation column. Today, most GC columns are fused silica capillaries with an inner diameter of 100–320 micrometres (0.0039–0.0126 in) and a length of 5–60 metres (16–197 ft). The GC column is located inside an oven where the temperature of the gas can be controlled and the effluent coming off the column is monitored by a suitable detector.

Stalin had the support of the majority of the religious people in the USSR even through the late 1980s. The general tendency of this period was an increase in religious activity among believers of all faiths. Under Nikita Khrushchev, the state leadership clashed with the churches in 1958–1964, a period when atheism was emphasized in the educational curriculum, and numerous state publications promoted atheistic views. During this period, the number of churches fell from 20,000 to 10,000 from 1959 to 1965, and the number of synagogues dropped from 500 to 97. The number of working mosques also declined, falling from 1,500 to 500 within a decade. Religious institutions remained monitored by the Soviet government, but churches, synagogues, temples, and mosques were all given more leeway in the Brezhnev era. Official relations between the Orthodox Church and the government again warmed to the point that the Brezhnev government twice honoured Orthodox Patriarch Alexy I with the Order of the Red Banner of Labour. A poll conducted by Soviet authorities in 1982 recorded 20% of the Soviet population as 'active religious believers.'

Removal of pathogens includes encapsulated bacteria, which reduces sepsis risk (see § Complications below). Removal of damaged erythrocytes reduces iron burden from heme via hepatosplenic recycling, which reduces sepsis risk (see Complications below). Removal of damaged erythrocytes continues healthy signaling to bone marrow, where erythropoiesis replaces red blood cells lost to wear and tear. In relation to the three facts above, the spleen misguidedly filters spherocytes – regardless of the age or functional status of the cell. The spleen is not dysfunctional itself when selecting spherocytes for destruction, as this is the regular function of the spleen both at an anatomic structure level, and at the molecular cellular level. At the anatomic level, the passage from the cords of Billroth into the sinusoids may be seen as a "bottleneck", where red blood cells need to be flexible in order to pass through. In HS, the erythrocytes fail to pass through fenestrations, and this is where resident splenic macrophages sample, or "bite", part of the stuck spherocytes' plasma membranes. The macrophages recognize that the spherocyte is not normal, and the macrophage is "programmed" to destroy irregularities filtered at the spleen from the blood. The resident splenic macrophages therefore phagocytose the spherocytes, causing extravascular hemolysis. This leads to both splenomegaly and anemia. Should this process continue unchecked chronically, inappropriate regulation of erythropoiesis leads to extramedullary hematopoiesis.

=== Maximum depositional age === Some of the most important information we can get from detrital zircon ages is the maximum depositional age of the referring sedimentary unit. The sedimentary unit cannot be older than the youngest age of the analyzed detrital zircons because the zircon should have existed before the rock formation. This provides useful age information to rock strata where fossils are unavailable, such as the terrestrial successions during Precambrian or pre-Devonian times. Practically, maximum depositional age is averaged from a cluster of youngest age data or the peak in age probability because the youngest U-Pb age within a sample is almost always younger with uncertainty.

Sources: en.wikipedia.org

Background from the literature

=== Side reactions === The three main side reactions that produce impurities have in common that they decompose urea. Urea hydrolyzes back to ammonium carbamate in the hottest stages of the synthesis plant, especially in the stripper, so residence times in these stages are designed to be short. Biuret is formed when two molecules of urea combine with the loss of a molecule of ammonia.

== Adverse effects == Most of the comparatively few fatal incidents associated with psychedelic mushroom usage involve the simultaneous use of other drugs, especially alcohol. A common adverse effect resulting from psilocybin mushroom use involves "bad trips" or panic reactions, in which people become anxious, confused, agitated, or disoriented. Accidents, self-injury, or suicide attempts can result from serious cases of acute psychotic episodes. No studies have linked psilocybin with birth defects, but it is recommended that pregnant women avoid its usage.

=== Serotonin precursor === Tryptophan affects brain serotonin synthesis when given orally in a purified form and is used to modify serotonin levels for research. Low brain serotonin level is induced by administration of tryptophan-poor protein in a technique called acute tryptophan depletion. Studies using this method have evaluated the effect of serotonin on mood and social behavior, finding that serotonin reduces aggression and increases agreeableness.

The Wallerian degeneration pathway has been further illuminated by the discovery that sterile alpha and TIR motif containing 1 (SARM1) protein plays a central role in the Wallerian degeneration pathway. The gene was first identified in a Drosophila melanogaster mutagenesis screen, and subsequently knockouts of its homologue in mice showed robust protection of transected axons comparable to that of WldS. SARM1 catalyzes the synthesis and hydrolysis of cyclic ADP-ribose (cADPR) from NAD+ to ADP-ribose. SARM1 activation locally triggers a rapid collapse of NAD+ levels in the distal section of the injured axon, which then undergoes degeneration. This collapse in NAD+ levels was later shown to be due to SARM1's TIR domain having intrinsic NAD+ cleavage activity. The SARM1 protein has four domains, a mitochondrial localization signal, an auto-inhibitory N-terminus region consisting of armadillo/HEAT motifs, two sterile alpha motifs responsible for multimerization, and a C-terminus Toll/Interleukin-1 receptor that possesses enzymatic activity. Activation of SARM1 is sufficient to collapse NAD+ levels and initiate the Wallerian degeneration pathway. The activity of SARM1 helps to explain the protective nature of the survival factor NMNAT2, as NMNAT enzymes have been shown to prevent SARM1-mediated depletion of NAD+. This relationship is further supported by the fact that mice lacking NMNAT2, which are normally not viable, are completely rescued by SARM1 deletion, placing NMNAT2 activity upstream of SARM1.

Combination of small size, ease of engineering, high affinity and specificity makes Affibody molecules suitable alternative as monoclonal antibodies for both molecular imaging and therapeutical applications, especially for the receptor-overexpressing tumors. These proteins are characterized by a high rate of extravasation and rapid clearance of non-bound tracer from the circulation, as well as other nonspecific compartments, when compared to antibodies and their fragments

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.

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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