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Identity And Regulatory Status — Deep Dive

By Editorial Desk · published 2026-01-16 · last reviewed 2026-02-22 · Topic

A practical reference on Nuclear receptor: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

This page was last updated on 2026-02-22 and is reviewed periodically as new material appears.

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.

Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.

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.

PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516; GW-1516; endurobolGW501516 is the research code
Drug classPPARδ agonistNot a selective androgen receptor modulator
Molecular formulaC21H18F3NO3S2Established chemical formula
Molar mass453.5 g/molCalculated from the formula
Regulatory statusProhibited in sport; not approved as medicineStatus varies by country

Cardarine Identity and Mechanism

Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.

Cardarine is the common name for GW501516, a synthetic compound studied as a peroxisome proliferator-activated receptor delta agonist. Researchers developed it to explore treatments for lipid disorders and metabolic conditions. It is not an approved medicine in any country. Early clinical work examined changes in HDL cholesterol and triglycerides, but development was discontinued after animal studies raised concerns about cancer. The compound remains available as a research chemical and appears in discussions of performance enhancement.

At the molecular level, GW501516 binds and activates PPARδ, a nuclear receptor that regulates transcription. Activation shifts expression of genes involved in fatty acid oxidation, energy expenditure, and lipid transport in skeletal muscle and liver. Animal studies report increased endurance and altered lipid profiles after exposure. Human data are limited to small trials and do not establish long-term safety or efficacy. PPARδ also has roles in cell proliferation, so the relationship between activation and cancer risk remains an open question.

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Identity and Pharmacological Classification

Published studies have examined GW501516 in animal models of obesity, insulin resistance, and exercise endurance. Early human trials reportedly ended, and development was discontinued after preclinical findings raised concerns about cancer in some rodent studies. Regulatory agencies have not approved cardarine for any medical use. Its availability through non-pharmaceutical channels raises questions about identity, purity, and legal status that are separate from its laboratory pharmacology. Those questions are often addressed through analytical testing rather than assumptions about product labels.

Cardarine is a common name for GW501516, also GW-1516, a synthetic compound developed as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. It belongs to a class of agents that modulate gene transcription related to lipid and energy metabolism. The compound was studied in preclinical and early clinical research for metabolic and cardiovascular conditions, but it did not progress to approved therapeutic use. Its name appears in fitness and sports contexts despite not being approved as a drug.

PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.

Supporting material

=== Kosovo === → : Kosovar in Serbia Kosovo is still only a partially recognised state and the government of Serbia still claims the territory as its own. Due to Serbian refusal of Kosovo institutions, Serbs in North Kosovo act independently in sport. For example, the Football First League of North Kosovo was primarily formed of Serbian clubs from four of North Kosovo's municipalities. Both governments agreed upon creating a Community of Serb Municipalities. In 2016, Kosovo became the 55th member of UEFA, and therefore Football Federation of Kosovo's Football Superleague of Kosovo became a recognised independent league. From 2010 to 2015, the Football First League of North Kosovo was the top football regional league in North Kosovo, ranked fifth in the Serbian league system. The league was formed primarily of Serbian football clubs that come from four of North Kosovo's municipalities such as Leposavić, Zvečan, Zubin Potok and Northern Kosovska Mitrovica. The league was formed in protest to the establishment of the Kosovo Super League by the Republic of Kosovo; the Serbian clubs from North Kosovo refuse to enter the Republic of Kosovo's institutions as per the Assembly of the Community of Municipalities of the Autonomous Province of Kosovo and Metohija.

The term corrosion refers to the electrochemical oxidation of metals in reaction with an oxidant such as oxygen. Rusting, the formation of iron oxides, is a well-known example of electrochemical corrosion: it forms as a result of the oxidation of iron metal. Common rust often refers to iron(III) oxide, formed in the following chemical reaction: 4 Fe + 3 O2 → 2 Fe2O3 The oxidation of iron(II) to iron(III) by hydrogen peroxide in the presence of an acid: Fe2+ → Fe3+ + e− H2O2 + 2 e− → 2 OH− Here the overall equation involves adding the reduction equation to twice the oxidation equation, so that the electrons cancel: 2 Fe2+ + H2O2 + 2 H+ → 2 Fe3+ + 2 H2O

=== Receptor tyrosine kinase === Much like for G protein-coupled receptors, dimerization is essential for receptor tyrosine kinases (RTK) to perform their function in signal transduction, affecting many different cellular processes. RTKs typically exist as monomers, but undergo a conformational change upon ligand binding, allowing them to dimerize with nearby RTKs. The dimerization activates the cytoplasmic kinase domains that are responsible for further signal transduction.

== Expansion == Between 1993 and 1995 five new establishments were opened, and today it has a total of 72 restaurants; 63 in Madrid, 5 in Valencia, 2 in Barcelona, 2 in Sevilla, 1 in Toledo and 1 in Segovia. There is also at least one location in Malaga. In 1995, the company sold approximately 1.5 million sandwiches per month. Already controlled by the brewery Damm since 2012, the Grupo Rodilla was fully bought by Damm in 2015.

A recipe from 1909 adds onions and tomato sauce, and serves it with crisp potato straws, which are considered the traditional side dish for beef Stroganoff in Russia. The version given in the 1938 Larousse Gastronomique includes beef strips, and onions, with either mustard or tomato paste optional. After the fall of the Russian monarchy in 1917, the recipe was popularly served in the hotels and restaurants of China before the start of World War II. The first English cookbook to include a recipe for beef Stroganoff is Ambrose Heath's Good Food (1932). The dish came to Hong Kong in the late 1950s. In 1960s United States, several manufacturers introduced dehydrated beef stroganoff mixes, which were mixed with cooked beef and sour cream. It was also available freeze-dried for campers.

Sources: en.wikipedia.org

Notes from published material

Products that have a minor contribution to revenues include Insulin lispro (Humalog), a modified type of medical insulin; ramucirumab (Cyramza), a fully human monoclonal antibody used for the treatment of cancer; baricitinib (Olumiant), an immunomodulatory medication used for the treatment of rheumatoid arthritis, alopecia areata, and COVID-19; insulin (Humulin) to treat high blood glucose; and galcanezumab (Emgality), a humanized monoclonal antibody used for the prevention of migraines. In 2024, 67% of the company's revenues came from the United States, 18% came from Europe, 3% came from Japan, and 3% came from China. Lilly was the first company to mass-produce both the polio vaccine, developed in 1955 by Jonas Salk, and insulin. It was one of the first pharmaceutical companies to produce human insulin using recombinant DNA, including Humulin (insulin medication), Humalog (insulin lispro), and the first approved biosimilar insulin product in the US, Basaglar (insulin glargine). It achieved commercial success with major depressive disorder drugs Prozac (fluoxetine) (1986), Cymbalta (duloxetine) (2004), and its antipsychotic medication Zyprexa (olanzapine) (1996), all of which are now off patent and are manufactured by others as generic drugs. In 2005, Lilly brought exenatide to market—the first of the GLP-1 receptor agonists—followed by the GIP and GLP-1 receptor agonist drugs Mounjaro and Zepbound (tirzepatide). The Lilly Endowment, a charitable foundation organized in 1937 by the founding family, owns 9.8% of the company.

Iced tea can be purchased, like soda, in canned or bottled form at vending machines and convenience stores; usually, this pre-made tea is sweetened with corn syrup, and sometimes some other flavoring, such as lemon or raspberry, is added. Also, like other soft drinks, it can be purchased as a fountain drink, though in some establishments it is pumped from a bag-in-box, and in others, it is simply poured from a separate container that contains freshly brewed tea. In restaurants, iced tea is usually served unsweetened except in the Southeastern United States where iced tea is much more common and is available both sweet and unsweetened and "iced tea" is often considered to be "sweet tea" unless otherwise specified. The reason for the pre-sweetening is that it may be difficult to dissolve sugar in iced tea, even with constant stirring. The result can be insufficiently sweetened tea or gritty, undissolved sugar crystals in the tea. In the Northern United States and the Western United States, "tea" generally means the hot beverage and iced tea is referred to by name. Iced tea's popularity in the United States has led to an addition to standard cutlery sets; the iced tea spoon is a standard flatware teaspoon, but with a long handle, suitable for stirring sugar into the taller glasses commonly used for iced tea.

In November 2021, CleanTechnica reported that Tesla would be opening Superchargers at 26 Buc-ee's locations in seven states. As of February 2023, there were operational Superchargers at more than half of the planned locations including in Alabama (Leeds and Robertsdale); Florida (St. Augustine); South Carolina (Florence); Tennessee (Crossville); and Texas (Bastrop, Baytown, Ennis, Giddings, Katy, Madisonville, Melissa, New Braunfels, and Wharton). Since then, more Superchargers have been added into more locations, such as in Colorado (Berthoud); Florida (Daytona Beach); Georgia (Adalrsville and Fort Valley); Kentucky (Richmond); Tennessee (Kodak); and Texas (Denton, Fort Worth, Luling, Pearland, Royse City, Temple, Terrell, and Waller).

== SY == SY – (s) Syria (ISO 3166 and FIPS 10-4 country code digram) SYC – (s) Seychelles (ISO 3166 trigram) SYLK – Microsoft 'Symbolic Link' data file format SYP – (s) Syrian pound (ISO 4217 currency code) SYR – (s) Syria (ISO 3166 trigram) Syriza – (p) Synaspismós Rizospastikís Aristerás (Greek Συνασπισμός Ριζοσπαστικής Αριστεράς, "Coalition of the Radical Left") SysML – (p) System Modeling Language Sysop – (p) System Operator

== Clinical significance == Mutations in this gene have been associated with tardive dyskinesia (TD), an increased risk of hematotoxicity after exposure to benzene, and susceptibility to various forms of cancer. Altered expression of this protein has been seen in many tumors and is also associated with Alzheimer's disease (AD).

Sources: en.wikipedia.org

Background from the literature

On 2 March, Hezbollah fired several rockets at northern Israel, setting off sirens in Haifa and the Upper Galilee. The group said its actions were in response to the assassination of Iranian supreme leader Ali Khamenei. One of the rockets was intercepted, while several others hit open areas. Hezbollah later claimed that the attack was a "defensive act" after over a year of Israeli attacks despite a truce. It added that it restarted fighting to force Israel to stop its aggression and evacuate from seized Lebanese territories, emphasising that the move was unrelated to the Iran war. The IAF and Israeli Navy conducted extensive retaliatory strikes across Lebanon, mainly targeting Dahieh and southern Lebanon. The IDF said it struck over 70 targets, while issuing evacuation orders for over 50 villages in the south and east. It added that Hussein Meklad, Hezbollah's intelligence chief, was killed. At least 52 people were killed, 154 were injured, and 29,000 others were displaced, according to the Lebanese Health Ministry. In response to Hezbollah's actions, prime minister Nawaf Salam banned the group from conducting military activities. On 3 March, Israel resumed ground operations in Lebanon and continued conducting strikes. Attacks hit weapons facilities, command centers, and communication equipment, along with the studios of Hezbollah-linked outlets Al-Nour and Al-Manar. The IDF said it struck 160 targets since the escalation and announced that it killed a senior liaison to the IRGC in Beirut the day prior.

Authorities in Italy have investigated a 'Ndrangheta mafia clan accused of trafficking and illegally dumping nuclear waste. According to a whistleblower, a manager of the Italy state energy research agency Enea paid the clan to get rid of 600 drums of toxic and radioactive waste from Italy, Switzerland, France, Germany, and the United States, with Somalia as the destination, where the waste was buried after buying off local politicians. Former employees of Enea are suspected of paying the criminals to take waste off their hands in the 1980s and 1990s. Shipments to Somalia continued into the 1990s, while the 'Ndrangheta clan also blew up shiploads of waste, including radioactive hospital waste, sending them to the sea bed off the Calabrian coast. According to the environmental group Legambiente, former members of the 'Ndrangheta have said that they were paid to sink ships with radioactive material for the last 20 years. In 2008, Afghan authorities accused Pakistan of illegally dumping nuclear waste in the southern parts of Afghanistan when the Taliban were in power between 1996 and 2001. The Pakistani government denied the allegation.

Dulaglutide, sold under the brand name Trulicity, is a medication used for the treatment of type 2 diabetes in combination with diet and exercise. This medication is often prescribed for adults and children age 10 and older with type 2 diabetes (citation). It is utilized alongside diet and exercise in order to improve blood sugar. It is also approved in the United States for the reduction of major adverse cardiovascular events such as death, heart attack, or stroke in adults with type 2 diabetes who have established cardiovascular disease or multiple cardiovascular risk factors. It is not yet known if it is beneficial, safe, or effective in lowering blood sugar in children under 10 years of age. Trulicity is taken by giving an injection once a week under the skin of your stomach, thigh, or upper arm. The medication is a prescription that comes in the form of a pre-filled single-dose pen in 0.75mg, 1.5mg, 3mg, or 4.5mg per 5mg injection. You are able to take the dosage at any time during the day of administration with/without food eaten. The most common side effects upon administration are nausea, diarrhea, vomiting, abdominal pain, and decreased appetite. Dulaglutide injection is in a class of medications called incretin mimetics, as it is a glucagon-like peptide-1 receptor agonist (GLP-1 agonist) consisting of GLP-1(7-37) covalently linked to an Fc fragment of human IgG4. GLP-1 is a hormone that is involved in normalizing the level of glucose in blood (glycemia). It works by aiding the pancreas to release the correct amount of insulin when blood sugar levels are high.

=== Activity === This enzyme participates in 8 metabolic pathways: alanine and aspartate metabolism, methionine metabolism, valine, leucine and isoleucine degradation, tyrosine metabolism, phenylalanine metabolism, tryptophan metabolism, phenylalanine, tyrosine and tryptophan biosynthesis, and alkaloid biosynthesis. It employs one cofactor, flavin adenine dinucleotide (FAD). The enzyme binds to FAD in the first step of the catalytic process, thereby reducing FAD to FADH2. The FAD is regenerated from FADH2 by oxidation as a result of O2 being reduced to H2O2. The mechanism proceeds via oxidative deamination of the L-amino acid, which affords an imino acid intermediate. Following hydrolysis of the intermediate, the enzyme successfully affords the 2-oxo acid, as shown in Scheme 1.

The vagrant population of the Bowery declined after the 1970s, in part because of the city's effort to disperse it. Since the 1990s the entire Lower East Side has been reviving, and gentrification has contributed to ongoing change along the Bowery. In particular, the number of high-rise condominiums is growing. In 2007, the SANAA-designed facility for the New Museum of Contemporary Art opened between Stanton and Prince Street. In 2008, AvalonBay Communities opened Avalon Bowery Place, its first luxury apartment complex on the Bowery; the structure includes a Whole Foods Market. Avalon Bowery Place was quickly followed with the development of Avalon Bowery Place II. The new development has not come without social costs. Michael Dominic's 2001 documentary Sunshine Hotel followed the lives of residents of one of the few remaining flophouses. Construction on the Wyndham Garden Hotel at 93 Bowery in the late Aughts destabilized neighboring building 128 Hester Street (owned by the same man, William Su), and 60 tenants were thrown out of the building with the help of the Department of Buildings. At least 75 tenants were displaced from 83 to 85 Bowery in January 2018 in frigid temperatures due to long-overdue repairs that needed to be made. Tenants accused the landlord of using this displacement to start renovating the buildings into a hotel, and they went on a hunger strike. The Bowery from Houston to Delancey Street still serves as New York's principal market for restaurant equipment and from Delancey to Grand for lamps.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a SARM?

No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.

Is cardarine approved for human use?

No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.

Why was its development discontinued?

Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist developed for research. It has not been approved as a medication in any country. It is classified as an unapproved drug and a prohibited substance in sport.

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