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Identity And Regulatory Status — Evidence Review

By Editorial Desk · published 2025-10-23 · last reviewed 2025-11-29 · Faq

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

This page was last updated on 2025-11-29 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.

Cardarine as Investigational PPARδ Agonist

The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.

Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.

Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.

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

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.

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Mechanism and Laboratory Detection

Published human data are sparse and mostly come from early-phase trials. Those studies examined short-term changes in lipids, glucose, and exercise capacity, but they were not large enough to establish efficacy or long-term safety. Some animal experiments reported increased running endurance, yet such findings do not prove a performance benefit in people. Anti-doping laboratories detect GW501516 and its metabolites in urine or blood using liquid chromatography-tandem mass spectrometry. Detection windows depend on dose, sample type, and individual metabolism. The method is sensitive enough to identify trace residues in tested samples.

Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.

GW501516 binds and activates PPARδ, a nuclear receptor that influences transcription of genes involved in fatty acid oxidation and energy use. Activation shifts some metabolic pathways in preclinical models, which is why the compound has been studied for lipid disorders and exercise-related endpoints. The exact downstream effects in humans are incompletely mapped. PPARδ is expressed in many tissues, including skeletal muscle, liver, and adipose tissue, so broad activation may have varied consequences. Researchers continue to examine how selective or partial activation might alter the balance between benefits and risks.

Reference notes

A quadrupole mass analyzers uses four parallel metal rods to create a quadrupole electrical field oscillating at radio frequency (RF), to selectively stabilize or destabilize the paths of ions passing through. With each oscillation pattern, the ions passing through would undergo a helical motion. If the ion has m/z within a certain range, the helical motion is stable. Otherwise, the helical motion will increase in amplitude until the ion collides with the rods. This means that only ions with m/z within a narrow range can go through it. The full spectrogram can be swept through by changing the potentials on the rods, continuously or in a succession of discrete hops. They are typically of low resolution ~1000, but they are cheap and small, so are good for "desktop" mass spectrometers. The quadrupole mass filter is closely related to the quadrupole ion trap, particularly the linear quadrupole ion trap except that it is designed to pass the untrapped ions rather than collect the trapped ones, and is for that reason referred to as a transmission quadrupole. The quadrupole ion trap itself can be used as an analyzer, as in ion trap analyzers. A common variation of the transmission quadrupole is the triple quadrupole mass spectrometer. The "triple quad" has three consecutive quadrupole stages, the first acting as a mass filter to transmit a particular incoming ion to the second quadrupole, a collision chamber, wherein that ion can be broken into fragments. The third quadrupole also acts as a mass filter, to transmit a particular fragment ion to the detector.

Religious leaders or sheikhs from Mount Carmel, the Galilee and the Golan Heights take the opportunity to discuss religious issues. The Cave of Elijah is a grotto that appears in the Hebrew Bible, where the prophet Elijah took shelter during a journey into the wilderness (1 Kings 19:8). The exact location of the cave is unknown. There is a "Cave of Elijah" on Mount Carmel approximately 40 m above sea level in Haifa. For centuries it has been a pilgrimage destination for Jewish, Christian, Druze, and Muslim people. Another cave associated with Elijah is located nearby, under the altar of the main church of the Stella Maris Monastery, also on Mount Carmel.

To reduce the cost to the military of maintaining stockpiles of certain pharmaceuticals, the United States Department of Defense (DoD) and the Food and Drug Administration (FDA) operate a joint initiative known as the Shelf Life Protection Program (SLEP), which evaluates the long-term effectiveness of medications stockpiled by the DoD and other government agencies. Under the program, medications are tested for safety and stability for extended periods of time in controlled storage conditions. In many cases, medications tested were found to be effective for years past their printed expiry dates; a 2006 study by the Journal of Pharmaceutical Sciences found that two-thirds of 122 medications tested through SLEP remained effective for an average of at least four additional years. In 2016, the DoD reported that the program had helped save the department US$2.1 billion on replacing stockpiled medications. While testing and stability assessment found that 88% of the lots were effective at least one year after their expiration date, with an average extension of 66 months, the additional stability period was very variable. For antibiotics studied, the mean extension for ciprofloxacin was 55 months, and for amoxicillin 23 months.

The successful incorporation of a third base pair is a significant breakthrough toward the goal of greatly expanding the number of amino acids which can be encoded by DNA, from the existing 20 amino acids to a theoretically possible 172, thereby expanding the potential for living organisms to produce novel proteins. In the future, these unnatural base pairs could be synthesised and incorporated into oligonucleotides via DNA printing methods.

Sources: en.wikipedia.org

Reference notes

government study conducted by the Substance Abuse and Mental Health Services Administration concluded that, in the US, benzodiazepines are recreationally the most frequently used pharmaceuticals due to their widespread availability, accounting for 35% of all drug-related visits to hospital emergency and urgent care facilities. Men and women are equally likely to use benzodiazepines recreationally. The report found that alprazolam is the most common benzodiazepine for recreational use, followed by clonazepam, lorazepam, and diazepam. The number of emergency department visits due to benzodiazepines increased by 36% between 2004 and 2006.

== January 5, 1982 (Tuesday) == The U.N. General Assembly voted, 86 to 21 with 34 abstentions, to approve a non-binding resolution calling all members of the United Nations to end aid, trade, and diplomatic ties with Israel to punish it for annexing the Golan Heights. The U.S. used its power, as a permanent member of the UN Security Council, and vetoed the resolution on January 20. South Korea ended a nationwide curfew that had been in place since 1945, and permitted citizens the freedom to be outside from midnight to 4:00 in the morning, a period previously off limits. The curfew remained in effect, however, for areas bordering North Korea. President Chun Doo-hwan said in a statement that South Koreans were "more mature" and that the curfew was no longer necessary. The sinking of the Japanese fishing trawler Akebono Maru No.28 killed 32 members of its crew. The ship was at least 130 miles (210 km) away from Adak Island, one the Aleutian Islands off of the coast of the U.S. state of Alaska when it capsized. Serial killer Charles Jackson Jr. raped and murdered his final victim, Joan Stewart, a biology professor at San Francisco City College near Montclair, California. Jackson, suspected of murdering seven other people in the Bay Area from 1975 to 1981, would be convicted of the murder of Stewart and sentenced to life imprisonment and would die in 2002, before the extent of his killings would be revealed by DNA profiling not available in 1982. Born: Faiza Hasan, Pakistani television actress; in Karachi.

Although Phineas Gage's brain injuries, caused by a several-foot-long tamping rod driven completely through his skull, caused him to become temporarily disabled, descriptions of his aberrant behavior in later life are disputed, contradicting other claims that he recovered fully.

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 an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.

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