A practical reference on Nuclear receptor: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
This page was last updated on 2026-06-04 and is reviewed periodically as new material appears.
Cardarine is a common name for GW501516, a synthetic compound first described in the 1990s as a selective agonist of the peroxisome proliferator-activated receptor delta. It was studied in preclinical models for metabolic and cardiovascular conditions, but it has not been approved as a medicine in the United States, Europe, or other major jurisdictions. Retail products labeled as cardarine are generally research chemicals or supplements, not pharmaceutical formulations. Because human safety and efficacy data remain limited, regulatory agencies treat it as an unapproved substance rather than a therapeutic product.
Sporting authorities added GW501516 to prohibited lists after it appeared in athlete samples and online markets. The World Anti-Doping Agency classifies it as a hormone and metabolic modulator, and its use can lead to an anti-doping rule violation. Some early laboratory work suggested effects on fatty acid oxidation and endurance-related metabolism in animals, but those findings do not establish safe or effective use in people. Reports of adverse events in humans are scarce and often anecdotal, which complicates risk assessment.
Legal status varies by country. In some places, cardarine is controlled under medicines or psychoactive substances laws; in others, it may be sold with minimal oversight as a research chemical. Customs agencies have intercepted shipments, and several national health agencies have issued warnings about products marketed for bodybuilding or performance enhancement. The lack of a standardized pharmaceutical supply means identity, purity, and contamination levels can differ widely between samples. These factors make cardarine a regulatory and public health concern rather than a conventional prescription drug.
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.
| Property | Value | Notes |
|---|---|---|
| IUPAC name | {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid | Systematic name for GW501516 |
| CAS Registry Number | 317318-70-0 | Unique identifier for the parent compound |
| Molecular formula | C21H18F3NO3S2 | Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur |
| Molecular weight | 453.5 g/mol | Approximate value for the neutral form |
| Appearance | White to off-white powder | Typical description for purified laboratory material |
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.
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.
PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.
Published studies have examined GW501516 in animal models of obesity, insulin resistance, and exercise endurance. Early human trials reportedly ended, and development was discontinued after preclinical findings raised concerns about cancer in some rodent studies. Regulatory agencies have not approved cardarine for any medical use. Its availability through non-pharmaceutical channels raises questions about identity, purity, and legal status that are separate from its laboratory pharmacology. Those questions are often addressed through analytical testing rather than assumptions about product labels.
Graft copolymerization: The growing polystyrene chain reacts with a double bond of the polybutadiene. As a result, several polystyrene chains are attached to one polybutadiene. S represents in the figure the styrene repeat unit B the butadiene repeat unit. However, the middle block often does not consist of such depicted butane homo-polymer but of a styrene-butadiene co-polymer: SSSSSSSSSSSSSSSSSSSBBSBBSBSBBBBSBSSBBBSBSSSSSSSSSSSSSSSSSSSSSSSSSSSSSS By using a statistical copolymer at this position, the polymer becomes less susceptible to cross-linking and flows better in the melt. For the production of SBS, the first styrene is homopolymerized via anionic copolymerization. Typically, an organometallic compound such as butyllithium is used as a catalyst. Butadiene is then added and after styrene again its polymerization. The catalyst remains active during the whole process (for which the used chemicals must be of high purity). The molecular weight distribution of the polymers is very low (polydispersity in the range of 1.05, the individual chains have thus very similar lengths). The length of the individual blocks can be adjusted by the ratio of catalyst to monomer. The size of the rubber sections, in turn, depends on the block length. The production of small structures (smaller than the wavelength of the light) ensure transparency. In contrast to PS-I, however, the block copolymer does not form any particles but has a lamellar structure.
==== United Kingdom ==== In the United Kingdom, preparations containing only dextropropoxyphene were discontinued in 2004. In 2007, the Medicines and Healthcare products Regulatory Agency removed the licence for co-proxamol, also called distalgesic. From then on in the UK, co-proxamol is only available on a named patient basis, for long-term chronic pain and only to those who have already been prescribed this medicine. Its withdrawal from the UK market is a result of concerns relating to its toxicity in overdose (even small overdoses can be fatal), and dangerous reaction with alcohol. Recreational use in the UK is uncommon. Many patients have been prescribed alternative combinations of drugs as a replacement. The motivation for the withdrawal of co-proxamol was the reduction in suicides and a key part of the agency's justification of its decision was based upon studies showing co-proxamol was no more effective than paracetamol alone in pain management. The co-proxamol preparations available in the UK contained a subtherapeutic dose of paracetamol, 325 mg per tablet. Patients were warned not to take more than eight tablets in one day, a total dose of 2600 mg paracetamol per day. Despite this reduced level, patients were still at a high risk of overdose; coproxamol was second only to tricyclic antidepressants as the most common prescription drugs used in overdose. Following the reduction in prescribing in 2005–2007, prior to its complete withdrawal, the number of deaths associated with the drug dropped significantly.
Brazilian literature dates back to the 16th century, to the writings of the first Portuguese explorers in Brazil, such as Pero Vaz de Caminha, filled with descriptions of fauna, flora and commentary about the indigenous population that fascinated European readers. Brazil produced significant works in Romanticism—novelists such as Joaquim Manuel de Macedo and José de Alencar wrote novels about love and pain. Alencar, in his long career, also treated indigenous people as heroes in the Indigenist novels O Guarani, Iracema and Ubirajara. Machado de Assis, one of his contemporaries, wrote in virtually all genres and continues to gain international prestige from critics worldwide. Brazilian Modernism, evidenced by the Modern Art Week in 1922, was concerned with a nationalist avant-garde literature, while Post-Modernism brought a generation of distinct poets such as João Cabral de Melo Neto, Carlos Drummond de Andrade, Vinicius de Moraes, Cora Coralina, Graciliano Ramos, Cecília Meireles, and internationally known writers dealing with universal and regional subjects such as Jorge Amado, João Guimarães Rosa, Clarice Lispector and Manuel Bandeira. Brazil's most significant literary award is the Camões Prize, which it shares with the rest of the Portuguese-speaking world. As of 2016, Brazil has eleven recipients of the prize. Brazil also holds its own literary academy, the Brazilian Academy of Letters, a non-profit cultural organization aimed at perpetuating the care of the national language and literature.
=== Brain === Broad generalizations are often made in popular psychology about certain brain functions being lateralized, or more predominant in one hemisphere than the other. These claims are often inaccurate or overstated. The human brain, particularly the prefrontal cortex, does not reach "full maturity" or "full development" at any particular age (e.g. 16, 18, 21, 25, 30). Changes in structure and myelination of gray matter are recorded to continue with relative consistency all throughout life including until death. Different mental abilities peak earlier or later in life. Humans do not generate all of the brain cells they will ever have by the age of two years. Although this belief was held by medical experts until 1998, it is now understood that new neurons can be created after infancy in some parts of the brain into late adulthood. People do not use only 10% of their brains. While it is true that a small minority of neurons in the brain are actively firing at any one time, a healthy human will normally use most of their brain over the course of a day, and the inactive neurons are important as well. The idea that activating 100% of the brain would allow someone to achieve their maximum potential and/or gain various psychic abilities is common in folklore and fiction, but doing so in real life would likely result in a fatal seizure. This misconception was attributed to late 19th century leading thinker William James, who apparently used the expression only metaphorically.
Sources: en.wikipedia.org
=== Properties === In terms of molecular structure, synephrine has a phenethylamine skeleton, with a phenolic hydroxy- group, an alcoholic hydroxy- group, and an N-methylated amino-group. Alternatively, synephrine might be described as a phenylethanolamine with an N-methyl and p-hydroxy substituent. The amino-group confers basic properties on the molecule, whereas the phenolic –OH group is weakly acidic: the apparent (see original article for discussion) pKas for protonated synephrine are 9.55 (phenolic H) and 9.79 (ammonium H). Common salts of racemic synephrine are its hydrochloride, C9H13NO2.HCl, m.p. 150–152°, the oxalate (C9H13NO2)2.C2H2O4, m.p. 221–222 °C, and the tartrate (Sympatol), (C9H13NO2)2.C4H6O6, m.p. 188–190 °C. The presence of the hydroxy-group on the benzylic C of the synephrine molecule creates a chiral center, so the compound exists in the form of two enantiomers, d- and l- synephrine, or as the racemic mixture, d,l- synephrine. The dextrorotatory d-isomer corresponds to the (S)-configuration, and the levorotatory l-isomer to the (R)-configuration. Racemic synephrine has been resolved using ammonium 3-bromo-camphor-8-sulfonate. The enantiomers were not characterized as their free bases, but converted to the hydrochloride salts, with the following properties: (S)-(+)-C9H13NO2.HCl: m.p. 178 °C; [α] = +42.0°, c 0.1 (H2O); (R)-(−)-C9H13NO2.HCl: m.p. 176 °C; [α] = −39.0°, c 0.2 (H2O) (−)-Synephrine, as the free base isolated from a Citrus source, has m.p. 162–164 °C (with decomposition). The X-ray structure for synephrine has been determined.
== Patterns of amino acid replacement == Evolution of proteins is slower than DNA since only nonsynonymous mutations in DNA can result in amino acid replacements. Most mutations are neutral to maintain protein function and structure. Therefore, the more similar amino acids are, the more probable that they will be replaced. Conservative replacements are more common than radical replacements, since they can result in less important phenotypic changes. On the other hand, beneficial mutations, enhancing protein functions are most likely to be radical replacements. Also, the physicochemical distances, which are based on amino acids properties, are negatively correlated with probability of amino acids substitutions. Smaller distance between amino acids indicates that they are more likely to undergo replacement.
==== Tax descriptions ==== The federal personal income tax is progressive, meaning a higher marginal tax rate is applied to higher ranges of income. For example, in 2010 the tax rate that applied to the first $17,000 in taxable income for a couple filing jointly was 10%, while the rate applied to income over $379,150 was 35%. The top marginal tax rate has declined considerably since 1980. For example, the top tax rate was lowered from 70% to 50% in 1980 and reached as low as 28% in 1988. The Bush tax cuts of 2001 and 2003, extended by President Obama in 2010, lowered the top rate from 39.6% to 35%. The American Taxpayer Relief Act of 2012 raised the income tax rates for individuals earning over $400,000 and couples over $450,000. There are numerous exemptions and deductions, that typically result in a range of 35–40% of U.S. households owing no federal income tax. The recession and tax cut stimulus measures increased this to 51% for 2009, versus 38% in 2007. In 2011 it was found that 46% of households paid no federal income tax, however the top 1% contributed about 25% of total taxes collected. In 2014, the top 1% paid approximately 46% of the federal income taxes, excluding payroll taxes. The federal payroll tax (FICA) partially funds Social Security and Medicare. For the Social Security portion, employers and employees each pay 6.2% of the workers gross pay, a total of 12.4%. The Social Security portion is capped at $118,500 for 2015, meaning income above this amount is not subject to the tax.
== History == 2C-EF was originally named by Alexander Shulgin in his 1991 book PiHKAL (Phenethylamines I Have Known and Loved). However, he only speculated about it and never actually synthesized or tested it himself. Subsequently, 2C-EF was synthesized and tested by others such as Daniel Trachsel.
== Reform and replacement == The Local Transport Act 2008 reconstituted it as the Greater Manchester Integrated Transport Authority. The integrated transport authority was replaced by Transport for Greater Manchester in 2011, which is accountable to the Greater Manchester Combined Authority.
Sources: en.wikipedia.org
=== Chemical properties === Doxycycline, doxycycline monohydrate and doxycycline hyclate are yellow, crystalline powders with a bitter taste. The latter smells faintly of ethanol, a 1% aqueous solution has a pH of 2–3, and the specific rotation is
The International Standard for the Prohibited List is the standard published by the World Anti-Doping Agency (WADA) that lists substances prohibited in competitive sport. It is updated at least once per year as required by the World Anti-Doping Code. The adoption of the first World Anti-Doping Code (the Code) occurred at the 2nd World Conference on Doping in Sport in March 2003 in Copenhagen, Denmark. It was there that WADA assumed the responsibility of maintaining, updating, and publishing the List of Prohibited Substances and Methods (the List) in sport. The List is to be updated and published by WADA at least annually. WADA specifies that the List generally includes any substance that meets any two of the following criteria: it enhances sport performance, it represents a health risk to the athlete, it violates the spirit of sport (as defined in the WADA Code). Substances and techniques that are prohibited by WADA fall into the following categories: S0 non-approved substances; S1 anabolic agents; S2 peptide hormones, growth factors, related substances, and mimetics; S3 beta-2 agonists; S4 hormone and metabolic modulators; S5 diuretics and masking agents; prohibited methods (M1 blood doping, M2 manipulation of samples, M3 gene doping); S6 stimulants; S7 narcotics; S8 cannabinoids; S9 glucocorticoids; P1 beta-blockers.
== P == Paraphilic Disorder Peritoneum disorders Personality disorders Pervasive developmental disorders Post-traumatic stress disorders Psychiatric disorders, i.e., mental illness Psychoactive substance abuse disorders Psychological disorders, i.e., mental illness Psychotic disorders Puerperal disorders
A mammary gland is a specific type of apocrine gland specialized for manufacture of colostrum (first milk) when giving birth. Mammary glands can be identified as apocrine because they exhibit striking "decapitation" secretion. Many sources assert that mammary glands are modified sweat glands.
Sources: en.wikipedia.org
No. Major drug regulators have not approved GW501516 for treating any medical condition. Products sold as cardarine are typically unapproved research chemicals or supplements, so their contents and safety are not assured.
It is prohibited by the World Anti-Doping Agency as a hormone and metabolic modulator. Athletes who test positive for GW501516 can face sanctions, including suspensions and loss of results.
Cardarine is a common or trade-style name, while GW501516 is the research code for the same chemical entity. Some sources also use Endurobol or GSK-516. The names refer to the same compound, not distinct drugs.
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.