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Identity And Regulatory Status — Beginner to Advanced

By Editorial Desk · published 2025-09-18 · last reviewed 2025-10-25 · Faq

Everything below concerns Nuclear receptor. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Last reviewed on 2025-10-25. Where a claim depends on a specific study, the study is described rather than over-claimed.

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.

Mechanism and Detection

Anti-doping laboratories identify GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the usual matrix, and detection can occur after the parent compound has cleared from blood. The exact detection window depends on dose, formulation, individual metabolism, and assay sensitivity. Because the compound is prohibited at all times, athletes are subject to testing in and out of competition. Analytical methods continue to improve as new metabolites and designer analogs are characterized.

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.

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

Identity and Pharmacological Mechanism

The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.

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.

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Cardarine as Investigational PPARδ Agonist

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.

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.

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.

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.

Notes from published material

=== Chymotrypsin-like === The S1 pocket of chymotrypsin-like enzymes is more hydrophobic than in trypsin-like proteases. This results in a specificity for medium to large sized hydrophobic residues, such as tyrosine, phenylalanine and tryptophan.

=== Australia === Nando's has been in continuous operation within Australia since 1990, when the first restaurant opened in Tuart Hill in Western Australia. As of August 2021, there were 155 restaurants in Australia; 63 in Victoria, 36 in Western Australia, 30 in Queensland, 16 in New South Wales, four in South Australia, two in the Northern Territory, three in Tasmania and two in the Australian Capital Territory. Per city, there are 59 in Melbourne, 34 in Perth, 20 in Brisbane, 15 in Sydney, four each in Adelaide and the Gold Coast, three in Ipswich, two each in Hobart, Canberra and Darwin and one each in Ballarat, Bunbury, Geelong, Kalgoorlie, Launceston, Newcastle, Rockhampton, Shepparton, the Sunshine Coast, Townsville and Traralgon. There have been various public battles between the parent company and its Australian franchisees.

=== Red peppercorns === Red peppercorns usually consist of ripe peppercorn drupes preserved in brine and vinegar. Ripe red peppercorns can also be dried using the same colour-preserving techniques used to produce green pepper.

Ribonucleoprotein Networks Analyzed by Mutational Profiling (RNP-MaP) is a strategy for probing RNA-protein networks and protein binding sites at a nucleotide resolution. Information about RNP assembly and function can facilitate a better understanding of biological mechanisms. RNP-MaP uses NHS-diazirine (SDA), a hetero-bifunctional crosslinker, to freeze RNA-bound proteins in place. Once the RNA-protein crosslinks are formed, MaP reverse transcription is then conducted to reversely transcribe the protein-bound RNAs as well as introduce mutations at the site of RNA-protein crosslinks. Sequencing results of the cDNAs reveal information about both protein-RNA interaction networks and protein binding sites.

Education in Hong Kong is managed primarily by the Hong Kong Education Bureau. It is largely modelled on that of the United Kingdom, particularly the English system. Children are required to attend school from age 6 until the completion of secondary education, generally at age 18. At the end of secondary schooling, local school students take a public examination and are awarded the Hong Kong Diploma of Secondary Education upon successful completion of the exam. Of residents aged 15 and older, 81% completed lower-secondary education, 66% graduated from an upper secondary school, 32% attended a non-degree tertiary program, and 24% earned a bachelor's degree or higher. Mandatory education within the city has contributed to an adult literacy rate of around 99.9%. Comprehensive schools fall into three categories: government-run public schools; subsidised schools, including government-aided and grant schools; and private schools, often run by religious organisations, that base admissions on academic merit. These schools are subject to the Education Bureau's curriculum guidelines. Private schools subsidised under the Direct Subsidy Scheme, and international schools fall outside of this system and may elect to use differing curricula and teach using other languages. Hong Kong students perform exceptionally well in global benchmarks. In PISA 2022 (latest available results), Hong Kong ranked in the top tier worldwide; 4th in mathematics and top 10 in reading and science. This places it well above the OECD average and among the highest-performing systems globally.

Sources: en.wikipedia.org

Background from the literature

is called an attenuation constant (a term used in various fields where a signal is transmitted though a medium) or coefficient. The amount of light transmitted decreases exponentially with distance. Taking the natural logarithm in the above equation, we get

In the 337 participants with non-small cell lung cancer, the median age was 56 years (range: 26 to 83); 56% female; 76% Asian, 15% White, 0.6% Black or African American, 8% unknown or other races; and 1.8% were of Hispanic or Latino ethnicity. The number of participants representing efficacy findings differs from the number of participants representing safety findings due to different groups of study participants analyzed for efficacy and safety. The FDA granted the application for taletrectinib priority review, breakthrough therapy, and orphan drug designations.

==== Legion number and title (cognomen) ==== The numbering of the legions is confusing, since several legions shared the same number with others. Augustus numbered the legions he founded himself from I, but also inherited numbers from his predecessors. Each emperor normally numbered the legions he raised himself starting from I. However, even this practice was not consistently followed. For example, Vespasian kept the same numbers as before for legions he raised from disbanded units. Trajan's first legion was numbered XXX because there were 29 other legions in existence at the time it was raised; but the second Trajanic legion was given the sequential number II. XVII, XVIII and XIX, the numbers of the legions annihilated in the Teutoburg Forest, were never used again. (These three legions are without titles, suggesting that in disgrace their titles may have been deliberately forgotten or left unmentioned.) As a result of this somewhat chaotic evolution, the legion's title became necessary to distinguish between legions with the same number. Legions often carried several titles, awarded after successive campaigns, normally by the ruling emperor e.g. XII Fulminata was also awarded: paterna (fatherly), victrix (victorious), antiqua (venerable), certa constans (reliable, steadfast) and Galliena (Gallienus '). Pia fidelis (loyal and faithful), fidelis constans and others were titles awarded to several legions, sometimes several times to the same legion. Only the most established, commonly used titles are displayed on this table. The geographical titles indicate

The organic compound citrulline is a non-essential α-amino acid. Its name is derived from citrullus, the Latin word for watermelon. Although named and described by gastroenterologists since the late 19th century, it was first isolated from watermelon in 1914 by Japanese researchers Yatarō Koga and Ryō Ōtake, and further codified in 1930. Citrulline has the formula H2NC(O)NH(CH2)3CH(NH2)CO2H. It is a key intermediate in the urea cycle, the pathway by which mammals excrete ammonia by converting it into urea. Citrulline is also produced as a byproduct of the enzymatic production of nitric oxide from the amino acid arginine, catalyzed by nitric oxide synthase.

=== Synthesis === Mescaline was the first ever psychedelic drug synthesized by chemists. Ernst Späth's 1919 total synthesis started from 3,4,5-trimethoxy­benzoyl chloride. Several approaches using different starting materials have been developed since, including the following:

Sources: en.wikipedia.org

Reference notes

== Function == All interferons share several common effects: they are antiviral agents and they modulate functions of the immune system. Administration of Type I IFN has been shown experimentally to inhibit tumor growth in animals, but the beneficial action in human tumors has not been widely documented. A virus-infected cell releases viral particles that can infect nearby cells. However, the infected cell can protect neighboring cells against a potential infection of the virus by releasing interferons. In response to interferon, cells produce large amounts of an enzyme known as protein kinase R (PKR). This enzyme phosphorylates a protein known as eIF-2 in response to new viral infections; the phosphorylated eIF-2 forms an inactive complex with another protein, called eIF2B, to reduce protein synthesis within the cell. Another cellular enzyme, RNAse L—also induced by interferon action—destroys RNA within the cells to further reduce protein synthesis from both viral and host genes. Inhibited protein synthesis impairs both virus replication and infected host cells. In addition, interferons induce production of hundreds of other proteins—known collectively as interferon-stimulated genes (ISGs)—that have roles in combating viruses and other actions produced by interferon. They also limit viral spread by increasing p53 activity, which kills virus-infected cells by promoting apoptosis. The effect of IFN on p53 is also linked to its protective role against certain cancers.

According to DSST, alcohol causes a decrease in performance on their standardized tests, and caffeine causes a significant improvement. When alcohol and caffeine are consumed jointly, the effects of the caffeine are changed, but the alcohol effects remain the same. For example, consuming additional caffeine does not reduce the effect of alcohol. However, the jitteriness and alertness given by caffeine is decreased when additional alcohol is consumed. Alcohol consumption alone reduces both inhibitory and activational aspects of behavioral control. Caffeine antagonizes the effect of alcohol on the activational aspect of behavioral control, but has no effect on the inhibitory behavioral control. The Dietary Guidelines for Americans recommend avoidance of concomitant consumption of alcohol and caffeine, as taking them together may lead to increased alcohol consumption, with a higher risk of alcohol-associated injury.

== Role in bone decomposition == Diagenesis alters the proportions of organic collagen and inorganic components (hydroxyapatite, calcium, magnesium) of bone exposed to environmental conditions, especially moisture. This is accomplished by the exchange of natural bone constituents, deposition in voids or defects, adsorption onto the bone surface and leaching from the bone.

=== Abnormal collagen === Abnormal collagen fibrils are often found in diabetes. Due to increased levels of lysyl oxidase, collagen increases cross-linking. This thickens the basement membrane, another hallmark of NL.

Curium pnictides show ferromagnetic transitions upon cooling: 244CmN and 244CmAs at 109 K, 248CmP at 73 K and 248CmSb at 162 K. The lanthanide analog of curium, gadolinium, and its pnictides, also show magnetic transitions upon cooling, but the transition character is somewhat different: Gd and GdN become ferromagnetic, and GdP, GdAs and GdSb show antiferromagnetic ordering. In accordance with magnetic data, electrical resistivity of curium increases with temperature – about twice between 4 and 60 K – and then is nearly constant up to room temperature. There is a significant increase in resistivity over time (~10 μΩ·cm/h) due to self-damage of the crystal lattice by alpha decay. This makes uncertain the true resistivity of curium (~125 μΩ·cm). Curium's resistivity is similar to that of gadolinium, and the actinides plutonium and neptunium, but significantly higher than that of americium, uranium, polonium and thorium. Under ultraviolet illumination, curium(III) ions show strong and stable yellow-orange fluorescence with a maximum in the range of 590–640 nm depending on their environment. The fluorescence originates from the transitions from the first excited state 6D7/2 and the ground state 8S7/2. Analysis of this fluorescence allows monitoring interactions between Cm(III) ions in organic and inorganic complexes.

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 to and activates PPAR delta, a nuclear receptor that controls expression of genes related to fatty acid oxidation. This mechanism can alter energy metabolism in animal models. It is not a direct stimulant or fat-burning enzyme.

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