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Identity And Regulatory Status — Evidence Review

By Editorial Desk · published 2026-03-02 · last reviewed 2026-04-07 · Wiki

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

This page was last updated on 2026-04-07 and is reviewed periodically as new material appears.

Identity and Regulatory Status

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.

Mechanism and Research Context

Laboratory studies have examined GW501516 in cell cultures and rodents for conditions such as dyslipidemia, insulin resistance, and obesity. Some trials in humans were initiated, but development was discontinued after preclinical findings raised concerns about cancer in certain models. Those findings do not prove that the compound causes cancer in people, but they contributed to regulatory caution. Later reviews often describe the evidence as preliminary and insufficient for assessing long-term safety.

In the fitness and bodybuilding literature, cardarine is frequently discussed as an endurance agent or fat-loss compound, although such claims are not supported by robust clinical evidence. Online descriptions often mix animal data, user anecdotes, and marketing language. Researchers who study PPARδ agonists distinguish between receptor activation in controlled experiments and unsupervised use of unverified products. The latter introduces unknown purity, dose, and interactions, making reported experiences difficult to interpret scientifically.

GW501516 acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in transcription of genes related to lipid handling and energy use. Activation of PPARδ can shift skeletal muscle toward greater fatty acid oxidation in animal models, which is one reason it drew interest for metabolic disease and exercise research. The exact downstream effects depend on tissue, species, dose, and duration. Human data are sparse, so many proposed benefits remain hypotheses rather than established clinical outcomes.

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

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.

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.

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Mechanism and Safety Research

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.

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.

Detection, Regulation, and Quality Context

Because cardarine is not an approved medicine, no pharmacopeial monograph defines its identity, purity, or storage requirements. Laboratories typically rely on in-house methods and reference standards when testing materials labeled as GW501516. Certificates of analysis may report purity and identity for a specific batch, but their scope varies and they do not guarantee safety or legal status. Independent verification can include high-performance liquid chromatography, mass spectrometry, nuclear magnetic resonance, and elemental analysis. The distinction between research chemical labeling and human use is significant because quality standards and oversight differ.

Cardarine can be detected in biological samples and product materials using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The method separates compounds by chromatography and identifies them by mass-to-charge transitions, allowing low-level detection in urine or blood. Sample preparation often involves enzymatic hydrolysis, solid-phase extraction, or protein precipitation. Certified reference materials and isotope-labeled internal standards improve quantification. Detection windows depend on metabolism, matrix, and assay sensitivity, so no single universal window applies.

Regulatory treatment of cardarine differs by context and jurisdiction. In competitive sport, the World Anti-Doping Agency lists PPARδ agonists, including GW501516, as prohibited at all times. Outside sport, it lacks approval as a prescription medicine in major drug markets, and products sold for human consumption may be treated as unapproved drugs. Some countries also restrict importation or sale through general consumer protection and medicines laws. These classifications affect availability, testing, and legal risk without establishing therapeutic value.

Cardarine Identity and Mechanism

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.

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.

Reference notes

== Personal life == D'Abo is the first cousin of Mike d'Abo, a singer and member of 1960s group Manfred Mann. This makes her first cousin once removed of actress Olivia d'Abo. Maryam and Olivia once lived in Los Angeles, buying a house together in 1988, after Olivia turned 19. D'Abo is the granddaughter (on her mother's side) of the anti-communist Georgian general Giorgi Kvinitadze. In November 2003, D'Abo married Hugh Hudson, the Oscar-nominated British director of Chariots of Fire (1981). They remained married until his death on 10 February 2023. In 2007, D'Abo had surgery for a brain haemorrhage from which she recovered.

== Safety and the environment == Indigo has a low oral toxicity, with an LD50 of 5 g/kg (0.5% of total mass) in mammals. In 2009, large spills of blue dye were reported downstream of a blue jeans manufacturer in Lesotho. The compound has been found to act as an agonist of the aryl hydrocarbon receptor.

This formula was developed by Levey et al. The 2009 CKD-EPI formula was suggested to improve cardiovascular risk prediction over the MDRD Study formula in a middle-age population. The 2021 CKD-EPI formula does not include a race coefficient (see discussion below). The 2021 CKD-EPI equation is:

== Finances == For the fiscal year 2017, BASF reported earnings of €6.1 billion, with an annual revenue of €64.5 billion, an increase of 12% over the previous fiscal cycle. BASF's shares traded at over €69 per share, and its market capitalization was valued at €63.7 billion in November 2018. In October 2019, BASF reported a drop of operating income for July to September amounting to 24 percent, along with a drop in EBIT earnings of €1.1 billion ($1.2 billion). The US–China trade war as well as uncertainties related to Brexit were identified as contributing factors. However, overall third quarter profit beat expectations as the acquisition of Bayer AG's agrochemical and seed business help to offset some of the effects of the trade war.

Sources: en.wikipedia.org

Reference notes

The 3C-like protease (3CLpro) or main protease (Mpro), formally known as C30 endopeptidase, is the main protease found in coronaviruses. It cleaves the coronavirus polyprotein at eleven conserved sites. It is a cysteine protease and a member of the PA clan of proteases. It has a cysteine-histidine catalytic dyad at its active site and cleaves a Gln–(Ser/Ala/Gly) peptide bond. The Enzyme Commission refers to this family as SARS coronavirus main proteinase (Mpro; EC 3.4.22.69). The 3CL protease corresponds to coronavirus nonstructural protein 5 (nsp5). The "3C" in the common name refers to the 3C protease (3Cpro) which is a homologous protease found in picornaviruses.

== Clinical significance == The epithelium of the glans penis consists of mucosal tissue. Birley et al. report that excessive washing with soap may dry the mucous membrane which covers the glans penis and cause non-specific dermatitis. The condition is described as an inflammation of the skin, often caused by an irritating substance or a contact allergy. Sensitivity to chemicals in certain products can cause an allergic reaction, including irritation, itching and rash. Inflammation of the glans penis is known as balanitis. It is a treatable condition that occurs in about 3–11% of males (up to 35% of diabetic males). Edwards reported that it is generally more common in males who have poor hygiene habits or have not been circumcised. It has many causes, including irritation or infection with a wide variety of pathogens. Symptoms of balanitis may appear suddenly or develop gradually. They might include pain, irritation, redness or red patches on the glans penis. Careful identification of the cause with the aid of patient history, physical examination, swabs and cultures, and biopsy are essential in order to determine the proper treatment. The meatus (opening) of the urethra located at the tip of the glans might become subject to meatal stenosis, a condition mostly seen as a late complication of circumcision. It occurs in about 2–20% of circumcised boys and it is rarely seen in uncircumcised men. It is characterized by a narrowing of the meatus, which might cause sudden or often urges to urinate and burning during the process.

== Geographic distribution == TEV appears to be a virus that evolved in the New World. It has been reported in Canada, the United States (including Hawaii), Mexico and Puerto Rico in North America and in Venezuela in South America.

Sources: en.wikipedia.org

Reference notes

== Veterinary use == Based on a 2010 review of injectable-agent use for short-duration anesthesia, the American Association of Equine Practitioners recommends the use of xylazine as a sedative for induction of anesthesia for durations of around 20 minutes or less. In addition, diazepam and ketamine are recommended after the xylazine. For longer duration anesthesia, those over 30 minutes, the most common anesthetics is the combination of guaifenesin, ketamine, and xylazine or isoflurane.

In cell biology, ion trapping is the build-up of a higher concentration of a chemical across a cell membrane due to the pKa value of the chemical and difference of pH across the cell membrane. This results in basic chemicals accumulating in acidic bodily fluids such as the cytosol, and acidic chemicals accumulating in basic fluids.

A 2017 literature review indicated there are numerous potential carcinogens of colorectal tissue in red meat, particularly those in processed red meat products, such as N-nitroso compounds, polycyclic aromatic hydrocarbons (PAHs), and heterocyclic amines (HCAs). Cooking meat with "high-temperature methods, such as pan frying or grilling directly over an open flame", also causes formation of PAHs and HCAs.

Mephedrone acts as a potent substrate for monoamine transporters, including the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET). It inhibits the reuptake of these neurotransmitters and promotes their release. The drug induces a rapid and significant increase in extracellular levels of dopamine, serotonin, and norepinephrine. This effect is more pronounced for serotonin compared to dopamine, which distinguishes mephedrone from much of the other psychostimulants. The pharmacodynamic profile of mephedrone is often compared to MDMA and methamphetamine. Like MDMA, it has a greater effect on serotonin than dopamine release. Similar to methamphetamine, it causes rapid dopamine release. Mephedrone has been found to be a full releaser of serotonin but a partial releaser of dopamine. In addition to induction of monoamine release via the monoamine transporters, mephedrone shows significant affinity for various receptors, including the serotonin 5-HT2A, 5-HT2B, 5-HT2C, and α2-adrenergic receptors, as well as the trace amine-associated receptor 1 (TAAR1). Mephedrone is a potent and near-full agonist of the serotonin 5-HT2A receptor, whereas it was inactive as an agonist of the serotonin 5-HT2B receptor. Mephedrone binds to and activates the rat and mouse TAAR1 with micromolar potencies, but is not an agonist of the human TAAR1 (EC50Tooltip half-maximal effective concentration > 30 μM).

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.

How does cardarine work in the body?

It binds and activates PPARδ, a nuclear receptor that influences gene expression related to fatty acid metabolism and energy balance. This mechanism has been studied mainly in animals and cell models, not established as a safe human therapy.

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