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Background And Regulatory Status — 2026 Update

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

Cardarine is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.

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

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.

Mechanism and Safety Research

Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.

GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.

Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.

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

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 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.

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Identity and Regulatory Status

Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.

Cardarine is a common name for GW501516, an investigational compound developed in the 1990s for metabolic conditions. It acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in lipid and energy metabolism. The compound is frequently mislabeled as a selective androgen receptor modulator, or SARM, but its molecular target is different. GW501516 reached early clinical testing before development was discontinued. It has no approved therapeutic use in any country. The name cardarine is not a formal international nonproprietary name.

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.

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.

Further detail

==== Ukrainian ==== Providence Association of Ukrainian Catholics in America - Founded in 1912. Headquartered in Philadelphia where the annual convention always meets. Membership is open to "any Ukrainian, either Ukrainian Catholic or of another Christian denomination, who is not hostile to the Ukrainian Catholic Church, is morally stable, mentally and physically sound, honest, practicing his/her Christian faith, of good character, and fully abiding by these Bylaws...[a] Ukrainian, or a person of Ukrainian descent, or of another ethnic affiliation related to a person of Ukrainian origin, in good health, not exceeding 70 years of age, is also eligible for membership." In 1979 had 210 lodges in Pennsylvania and New Jersey. Had the same number of lodges in 2015. Had 11,000 members at the beginning of the 1930s, 8,000 in 1942, 16,994 in 1965, 18,000 in 1979, 17,927 in 1994. Members are admonished to send their children to parochial schools following the law of the church. One of the group's original objectives was to create low-interest loans for religious institutions, particularly parochial schools. Ukrainian Fraternal Association - Founded in 1910 as the Ruthenian National Union, became the Ukrainian Workingmen's Association in 1918, and adopted the present name in 1978. It was open to Ukrainians, Russians and other Slavs without regard to religious or political affiliations; clergy and those who insisted on debating religious questions were encouraged to join another group.

== Selected publications == Viswanathan, V.; Mirshad, R. (2023), "Role of Technology for wound Care in Diabetic Foot", Chronic Wound Management, Cham: Springer International Publishing, pp. 67–76, doi:10.1007/978-3-031-26110-7_4, ISBN 978-3-031-26109-1 Viswanathan, Vijay; Ahmed Khan, Balkhiwala; Nachimuthu, Sukanya; Kumpatla, Satyavani (2023). "Precision of Michigan Neuropathy Screening Instrument (MNSI) Tool for the Diagnosis of Diabetic Peripheral Neuropathy Among People with Type 2 Diabetes—A Study from South India". The International Journal of Lower Extremity Wounds. doi:10.1177/15347346231163209. ISSN 1534-7346. "Current and future perspective in the management of diabetes". {{cite journal}}: Cite journal requires |journal= (help) "Type 2 Diabetes Mellitus – The Epidemic Of The 21st Century: The Indian Scenario A Ramachandran, C Snehalatha*, Int. J. Diab. Dev. Countries (1999), Vol. 19". {{cite journal}}: Cite journal requires |journal= (help) High Prevalence of Obstructive Sleep Apnea among People with Type 2 Diabetes Mellitus in a Tertiary Care Center. J Assoc Physicians India. 2017 Nov;65(11):38-42. PMID 29322708. Need for education on footcare in diabetic patients in India. J Assoc Physicians India. 1999 Nov;47(11):1083-5. PMID 10862318. Diabetic nephropathy in type 2 diabetes: the Indian experience. J Assoc Physicians India. 2001 Dec;49:1185-7. PMID 11996441. Prevalence of pathogens in diabetic foot infection in South Indian type 2 diabetic patients. J Assoc Physicians India. 2002 Aug;50:1013-6. PMID 12421021.

The Calvin cycle, also known as the dark reactions, is a series of biochemical reactions that fixes CO2 into G3P sugar molecules and uses the energy and electrons from the ATP and NADPH made in the light reactions. The Calvin cycle takes place in the stroma of the chloroplast. While named "the dark reactions", in most plants, they take place in the light, since the dark reactions are dependent on the products of the light reactions.

=== Transamination === Urea undergoes transamination. For example, treatment with anilinium gives both N-phenylurea and N,N'-diphenylurea. N-Methylurea can be prepared by a similar acid-catalyzed pathway.

=== Breastfeeding === In 2016, estimates suggested that more widespread breastfeeding could prevent about 823,000 deaths annually of children under age 5. In addition to reducing infant deaths, breast milk provides an important source of micronutrients - which are clinically proven to bolster children's immune systems – and provides long-term defenses against non-communicable and allergic diseases. Breastfeeding may improve cognitive abilities in children, and correlates strongly with individual educational achievements. As previously noted, lack of proper breastfeeding is a major factor in child mortality rates, and is a primary determinant of disease development for children. The medical community recommends exclusively breastfeeding infants for 6 months, with nutritional whole food supplementation and continued breastfeeding up to 2 years or older for overall optimal health outcomes. Exclusive breastfeeding is defined as giving an infant only breast milk for six months as a source of food and nutrition. This means no other liquids, including water or semi-solid foods.

Sources: en.wikipedia.org

Background from the literature

Opportunistic bands of Normans successfully established a foothold in southern Italy. Probably as the result of returning pilgrims' stories, the Normans entered southern Italy as warriors in 1017 at the latest. In 999, according to Amatus of Montecassino, Norman pilgrims returning from Jerusalem called in at the port of Salerno when a Muslim attack occurred. The Normans fought so valiantly that Prince Guaimar III begged them to stay, but they refused and instead offered to tell others back home of the Prince's request. William of Apulia tells that, in 1016, Norman pilgrims to the shrine of the Archangel Michael at Monte Gargano were met by Melus of Bari, a Lombard nobleman and rebel, who persuaded them to return with more warriors to help throw off the Byzantine rule, which they did. The two most prominent Norman families to arrive in the Mediterranean were descendants of Tancred of Hauteville and the Drengot family. A group of Normans with at least five brothers from the Drengot family fought the Byzantines in Apulia under the command of Melus of Bari. Between 1016 and 1024, in a fragmented political context, the County of Ariano was founded by another group of Norman knights headed by Gilbert Buatère and hired by Melus of Bari. Defeated at Cannae, Melus of Bari escaped to Bamberg, Germany, where he died in 1022. The county, which replaced the pre-existing chamberlainship, is considered to be the first political body established by the Normans in the south of Italy.

Not all selenoproteins were retained, however: the selenoprotein U contains selenocystine in fishes and chicken, but mammals (including humans) have a selenium-free version of this protein, replacing the selenocystine with cysteine (human genes PRXL2A, PRXL2B, PRXL2C). Another example is the human GPX5 and rodent GPX6, both of which have a vestigial SECIS element pointing clearly to a selenocystine past.

A β-helix is formed from repeating structural units consisting of two or three short β-strands linked by short loops. These units "stack" atop one another in a helical fashion so that successive repetitions of the same strand hydrogen-bond with each other in a parallel orientation. See the β-helix article for further information. In lefthanded β-helices, the strands themselves are quite straight and untwisted; the resulting helical surfaces are nearly flat, forming a regular triangular prism shape, as shown for the 1QRE archaeal carbonic anhydrase at right. Other examples are the lipid A synthesis enzyme LpxA and insect antifreeze proteins with a regular array of Thr sidechains on one face that mimic the structure of ice.

=== Distribution === In June 2013, U.S. State Department released a report on slavery. It placed Russia, China, and Uzbekistan in the worst offenders category. Cuba, Iran, North Korea, Sudan, Syria, and Zimbabwe were at the lowest level. The list also included Algeria, Libya, Saudi Arabia and Kuwait among a total of 21 countries. In Kuwait, there are more than 600,000 migrant domestic workers who are vulnerable to forced labor and legally tied to their employers, who often illegally take their passports. In 2019, online slave markets on apps such as Instagram were uncovered. In the preparations for the 2022 World Cup in Qatar, thousands of Nepalese, the largest group of labourers, faced slavery in the form of denial of wages, confiscation of documents, and inability to leave the workplace. In 2016, the United Nations gave Qatar 12 months to end migrant worker slavery or face investigation. The Walk Free Foundation reported in 2018 that slavery in wealthy Western societies is much more prevalent than previously known, in particular the United States and Great Britain, which have 403,000 (one in 800) and 136,000 slaves respectively. Andrew Forrest, founder of the organization, said that "The United States is one of the most advanced countries in the world yet has more than 400,000 modern slaves working under forced labour conditions." An estimated 40.3 million are enslaved globally, with North Korea having the most slaves at 2.6 million (one in 10). Of the estimated 40.3 million people in contemporary slavery, 71% are women and 29% are men.

Sources: en.wikipedia.org

Further detail

In addition, sexual wellbeing is often lower in women with PMOS. Women with PMOS are about three times more likely to develop endometrial cancer. This is linked to lack of periods and lower levels of sex hormone-binding globulin (SHBG) and progesterone. Women with PMOS more often have sleep apnea, particularly if obesity is present.

== Notes == a "Points" refers to carry-over points accrued following the sanction. For example, 154.69 points draw a one-match suspension, with 54.69 carry-over points (for every 100 points, a one-match suspension is given). s Denotes amount of seasons on the Essendon list only.

=== Activity profile === Flibanserin acts as a full agonist in the frontal cortex and the dorsal raphe nucleus, but only as a partial agonist in the CA3 region of the hippocampus of the 5-HT1A receptor (serotonin receptor) (Ki = 1 nM in CHO cells, but only 15–50 nM in cortex, hippocampus and dorsal raphe) and, with lower affinity, as an antagonist of the 5-HT2A receptor (Ki = 49 nM) and antagonist or very weak partial agonist of the D4 receptor (Ki = 4–24 nM, Ki = 8–650 nM). Flibanserin demonstrates selectivity for postsynaptic 5-HT1A receptors. Despite the much greater affinity of flibanserin for the 5-HT1A receptor, and for reasons that are unknown (although it might be caused by the competition with endogenous serotonin), flibanserin occupies the 5-HT1A and 5-HT2A receptors in vivo with similar percentages. Flibanserin also has low affinity for the 5-HT2B receptor (Ki = 89.3 nM) and the 5-HT2C receptor (Ki = 88.3 nM), both of which it behaves as an antagonist of. Flibanserin preferentially activates 5-HT1A receptors in the prefrontal cortex, demonstrating regional selectivity, and has been found to increase dopamine and norepinephrine levels and decrease serotonin levels in the rat prefrontal cortex, actions that were determined to be mediated by activation of the 5-HT1A receptor. As such, flibanserin has been described as a norepinephrine–dopamine disinhibitor (NDDI). The proposed mechanism of action refers to the Kinsey dual control model of sexual response.

Cold Cave is the solo electronic music project for musician Wesley Eisold, described as a "collage of darkwave, noise, and synthpop." A number of reviewers note the affinity with early 1980s post-punk and early synthpop, in particular Joy Division and New Order.

=== Food === Before being introduced into the aquarium trade, the dwarf, along with the snakeskin gourami was and still is a popular food fish in its native range. In Bangladesh it is known as "Kholisha" and "Khosti" in India and "Kungee" in Punjab as well as different linguistic variants within its range.

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 the main molecular target of cardarine?

It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.

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