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Identity And Regulatory Status — Research Overview

By Editorial Desk · published 2026-01-02 · last reviewed 2026-02-04 · News

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

This page was last updated on 2026-02-04 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.

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.

Mechanism and Safety Research

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.

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.

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, Stability, and Quality

Stability of GW501516 depends on form, temperature, light exposure, and moisture. Solid reference material is typically stored frozen or refrigerated in a desiccator and protected from light. Solutions in organic solvents such as dimethyl sulfoxide are often kept frozen in aliquots to reduce freeze-thaw cycling. Aqueous solubility is low, so aqueous stock solutions can be difficult to prepare without cosolvents. Degradation may appear as changes in chromatographic purity or mass spectral signal. Stability studies are needed to establish shelf life for any specific preparation.

Quality assessment for cardarine samples usually combines identity, purity, and impurity testing. Nuclear magnetic resonance spectroscopy and mass spectrometry can confirm molecular structure, while high-performance liquid chromatography estimates purity. Certificates of analysis from testing laboratories may list these results, but they do not establish safety or legality. In the absence of approved manufacturing, products sold online may contain the wrong compound, variable amounts, or unlisted contaminants. Independent verification is therefore central to analytical work and to interpreting any reported biological activity.

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Detection and Regulatory Landscape

Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.

Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.

A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.

Background from the literature

is the molar latent heat of melting. In most substances, the volume increases when melting occurs, so the melting temperature increases with pressure. However, because ice is less dense than water, the melting temperature decreases. In glaciers, pressure melting can occur under sufficiently thick volumes of ice, resulting in subglacial lakes. The Clausius-Clapeyron relation also applies to the boiling point, but with the liquid/gas transition the vapor phase has a much lower density than the liquid phase, so the boiling point increases with pressure. Water can remain in a liquid state at high temperatures in the deep ocean or underground. For example, temperatures exceed 205 °C (401 °F) in Old Faithful, a geyser in Yellowstone National Park. In hydrothermal vents, the temperature can exceed 400 °C (752 °F). At sea level, the boiling point of water is 100 °C (212 °F). As atmospheric pressure decreases with altitude, the boiling point decreases by 1 °C every 274 meters. High-altitude cooking takes longer than sea-level cooking. For example, at 1,524 metres (5,000 ft), cooking time must be increased by a fourth to achieve the desired result. Conversely, a pressure cooker can be used to decrease cooking times by raising the boiling temperature. In a vacuum, water will boil at room temperature.

==== 2025 ==== UPF1 was found to decline significantly during cellular senescence. The findings suggest that the fall in UPF1 accelerates senescence by slowing down nonsense-mediated mRNA decay. The study was conducted by scientists at Chungnam National University, the Korea Research Institute of Bioscience and Biotechnology, the Korea Advanced Institute of Science and Technology, and the US National Institute on Aging. Scientists at the University of California, Berkeley managed to extend the lifespans of elderly male mice by 73% with a 14% increase in overall lifespan with the Alk5 inhibitor OT+A5i. Researchers at RWTH Aachen University discovered that four senolytic compounds – JQ1, RG7112, nutlin-3a, and AMG232 – can decrease epigenetic age in in vitro blood samples. Researchers at the University of Osaka discovered that the protein AP2A1 may regulate cellular senescence, finding that suppressing the protein in older cells reversed senescence and promoted rejuvenation, whereas overexpression of the protein in young cells advanced senescence. A study by scientists at University College London, Stanford University, Inserm, and the University of Helsinki found that accelerated aging in specific organs could be predictors for diseases across the entire body, not just those affecting that particular organ. A study at the University of Texas at Austin identified the exposure of osteocytes to senescent cells as a key driver of aging in bones.

X chromosome One of two sex chromosomes present in organisms which use the XY sex-determination system, and the only sex chromosome in the X0 system. The X chromosome is found in both males and females and typically contains much more gene content than its counterpart, the Y chromosome.

Sources: en.wikipedia.org

Further detail

As chemical reactions involve the valence electrons, elements with similar outer electron configurations may be expected to react similarly and form compounds with similar proportions of elements in them. Such elements are placed in the same group, and thus there tend to be clear similarities and trends in chemical behaviour as one proceeds down a group. As analogous configurations occur at regular intervals, the properties of the elements thus exhibit periodic recurrences, hence the name of the periodic table and the periodic law. These periodic recurrences were noticed well before the underlying theory that explains them was developed.

Social work in mental health, also called psychiatric social work, is a process where an individual in a setting is helped to attain freedom from overlapping internal and external problems (social and economic situations, family and other relationships, the physical and organizational environment, psychiatric symptoms, etc.). It aims for harmony, quality of life, self-actualization and personal adaptation across all systems. Psychiatric social workers are mental health professionals that can assist patients and their family members in coping with both mental health issues and various economic or social problems caused by mental illness or psychiatric dysfunctions and to attain improved mental health and well-being. They are vital members of the treatment teams in Departments of Psychiatry and Behavioral Sciences in hospitals. They are employed in both outpatient and inpatient settings of a hospital, nursing homes, state and local governments, substance use clinics, correctional facilities, health care services, private practice, etc. In the United States, social workers provide most of the mental health services. According to government sources, 60 percent of mental health professionals are clinically trained social workers, 10 percent are psychiatrists, 23 percent are psychologists, and 5 percent are psychiatric nurses. Mental health social workers in Japan have professional knowledge of health and welfare and skills essential for person's well-being.

Physicians began to think of "the pill" as an excellent means of birth control for young women. Stimulants such as Ritalin (methylphenidate) came to be pervasive tools for behavior management and modification in young children. Ritalin was first marketed in 1955 for narcolepsy; its potential users were middle-aged and the elderly. It was not until some time in the 1980s along with hyperactivity in children that Ritalin came onto the market. Medical use of methylphenidate is predominantly for symptoms of attention deficit hyperactivity disorder (ADHD). Consumption of methylphenidate in the U.S. out-paced all other countries between 1991 and 1999. Significant growth in consumption was also evident in Canada, New Zealand, Australia, and Norway. Currently, 85% of the world's methylphenidate is consumed in America. The first minor tranquilizer was meprobamate. Only fourteen months after it was made available, meprobamate had become the country's largest-selling prescription drug. By 1957, meprobamate had become the fastest-growing drug in history. The popularity of meprobamate paved the way for Librium and Valium, two minor tranquilizers that belonged to a new chemical class of drugs called the benzodiazepines. These were drugs that worked chiefly as anti-anxiety agents and muscle relaxants. The first benzodiazepine was Librium. Three months after it was approved, Librium had become the most prescribed tranquilizer in the nation. Three years later, Valium hit the shelves and was ten times more effective as a muscle relaxant and anti-convulsant.

is the detected radiation that results from the de-excitation of the product species. The advantages of this technique include multi-element analysis, excellent sensitivity, and high selectivity, and no time-consuming separation procedures. One disadvantage is the requirement of a nuclear reactor for sample preparation.

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 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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