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Identity And Regulatory Status — Beginner to Advanced

By Editorial Desk · published 2025-10-01 · last reviewed 2025-11-05 · Blog

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

Reviewed 2025-11-05. Anything still debated is marked as such rather than presented as settled.

Identity and Regulatory Status

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.

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.

Identity and Pharmacological Mechanism

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 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

Detection, Regulation, and Quality Context

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.

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.

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Mechanism and Research Context

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.

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.

Preclinical Findings and Safety Signals

Safety concerns emerged from long-term animal studies. In rodents given the compound for extended periods, researchers found an increased incidence of certain cancers, including liver and bladder tumors. These findings contributed to the discontinuation of clinical development. Whether similar risks apply to short-term or low-level exposure in humans is not established, and controlled human safety data are limited. The relevance of high-dose rodent carcinogenicity findings to human use remains a subject of debate.

Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.

Laboratory studies indicate that GW501516 activates PPARδ, a nuclear receptor involved in fatty acid oxidation and energy metabolism. In rodent experiments, treated animals often showed increased endurance and reduced fat mass. These effects were observed under controlled conditions and do not establish safe or effective use in humans. The exact dose-response relationship in humans remains poorly characterized. Species differences in metabolism can affect how results translate across animals and people.

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.

Further detail

== Health == Domestic kittens in developed societies are usually vaccinated against common illnesses from two to three months of age. The usual combination vaccination protects against feline viral rhinotracheitis (FVR), feline calicivirus (C), and feline panleukopenia (P). This FVRCP inoculation is usually given at eight, twelve, and sixteen weeks, and an inoculation against rabies may be given at sixteen weeks. Kittens are usually spayed or neutered at seven months of age, but kittens may be neutered as young as seven weeks (if large enough), especially in animal shelters. Such early neutering does not appear to have any long-term health risks for cats, and it may even be beneficial in male cats. Kittens are commonly given deworming treatments for roundworms from about four weeks.

Any floating object displaces its own weight of fluid. In other words, for an object floating on a liquid surface (like a boat) or floating submerged in a fluid (like a submarine in water or dirigible in air) the weight of the displaced fluid equals the weight of the object. Thus, only in the special case of floating does the buoyant force acting on an object equal the objects weight. Consider a 1-ton block of solid iron. As iron is nearly eight times as dense as water, it displaces only 1/8 ton of water when submerged, which is not enough to keep it afloat. Suppose the same iron block is reshaped into a bowl. It still weighs 1 ton, but when it is put in water, it displaces a greater volume of water than when it was a block. The deeper the iron bowl is immersed, the more water it displaces, and the greater the buoyant force acting on it. When the buoyant force equals 1 ton, it will sink no farther. When any boat displaces a weight of water equal to its own weight, it floats. This is often called the "principle of flotation": A floating object displaces a weight of fluid equal to its own weight. Every ship, submarine, and dirigible must be designed to displace a weight of fluid at least equal to its own weight. A 10,000-ton ship's hull must be built wide enough, long enough and deep enough to displace 10,000 tons of water and still have some hull above the water to prevent it from sinking. It needs extra hull to fight waves that would otherwise fill it and, by increasing its mass, cause it to submerge.

When cells on one side of a stem grow longer and faster than cells on the other side, the stem will bend to the side of the slower growing cells as a result. This directional growth can occur via a plant's response to a particular stimulus, such as light (phototropism), gravity (gravitropism), water, (hydrotropism), and physical contact (thigmotropism). Plant growth and development are mediated by specific plant hormones and plant growth regulators (PGRs) (Ross et al. 1983). Endogenous hormone levels are influenced by plant age, cold hardiness, dormancy, and other metabolic conditions; photoperiod, drought, temperature, and other external environmental conditions; and exogenous sources of PGRs, e.g., externally applied and of rhizospheric origin.

Sources: en.wikipedia.org

Supporting material

Salad and Go blamed its bankruptcy filing on an ongoing Cyclosporiasis outbreak and stressful cash flow from rent from closed locations, as well as a continued decline in sales. On August 5, all locations were permanently closed. That same day, Dutch Bros. Coffee had reached an agreement to purchase 51 locations in Nevada and Arizona, as well as 14 locations in Texas and Oklahoma for a total of 65 locations to be bought out. These locations were expected to be refurbished and reopened under Dutch Bros. Coffee until 7 Brew outbid Dutch Bros. on September 1. The competitor acquired 73 locations- 35 in Arizona, 19 in Texas, 5 in Nevada and 7 in Oklahoma.

== External links == Institute of General, Inorganic and Theoretical Chemistry, University of Innsbruck: CV Prof. Bernd Michael Rode Curriculum Vita - Prof. Bernd Michael Rode, on the Website of the Theoretical Chemistry Genealogy Project, University of Hannvoer Homepage - Austrian South East Asian University Partnership Networks (ASEA-UNINET) Theoretical Chemistry Genealogy Project Archived 2014-05-20 at the Wayback Machine MOLVISION - Visualization of Chemical Systems APA - Austrian Press Agency: "Hochleistungscomputer für indonesische Partneruniversität"[link removed], published on April, 2nd 2014. Retrieved on May, 23rd 2014 Website of Dr. Heinz Fischer, President of Austria: "Wissenschaftstag" in Ho-Chi-Minh-Stadt, dem früheren Saigon" published by Austrian Press Agency (APA), on May, 31st 2012, retrieved on June, 19th 2014.

== Metabolism == Metabolic activation is required for PhIP to function as a mutagen. Therefore, the cancer risk posed by PhIP depends on the extent at which PhIP is metabolized. After absorption, PhIP is converted to a genotoxic metabolite in the liver by Phase I enzyme N-oxidation by Cytochrome P-450 1A2 (CYP1A2). PhIP can be further metabolized into a more potent metabolite through O-acetylation by hepatic or colonic N-acetyltransferase 1 (NAT1) and N-acetyltransferase 2 (NAT2), or by sulfotransferases. However, PhIP may also undergo a detoxification pathway through Phase II conjugation reaction via UDP-glucuronosyltransferases (UGTs) to form N-glucuronide conjugates. PhIP's nitrenium ion intermediate is a powerful electrophile that has propensity to form C-8 guanine adducts with the DNA. In addition, some of these metabolic enzymes are inducible and have polymorphic variation. CYP1A2 displays a 40-fold variation in expression among humans and can be induced by smoking, diet, and chronic hepatitis. The expression of UGTs also displays inducibility; however, NATs do not. Individuals can be classified as either rapid or slow N-oxidizers and O-acetylators by assessing CYP1A2 and NAT2 activities. Individuals with the rapid phenotype of either CYP1A2 or NAT2 metabolize PhIP more effectively and are therefore at greater risk of PhIP's carcinogenic metabolite and could be at a higher risk of cancer.

== See also == Desmoteplase Antistasin Tick Anticoagulant Peptide (TAP) Ecotin P-aminobenzamidine (pAB) Factor X (FXa) Vampire Bats Glycosylation WGA PNA antigenic properties immune response mutagenesis Ornithodoros moubata Haementeria officinalis E. coli

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. 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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