The short version of unapproved substance fits in a sentence. The long version — which is the one that helps — is below.
Reviewed 2025-11-21. Anything still debated is marked as such rather than presented as settled.
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.
Cardarine has no approved therapeutic indication and is not marketed as a medicine. The World Anti-Doping Agency lists GW501516 as a prohibited substance at all times, covering both in-competition and out-of-competition periods. National laws vary: some countries treat it as an unapproved drug subject to import controls, while others have specific restrictions on sale for human consumption. It is often sold as a research chemical, a label that does not imply safety or legality. Enforcement actions have targeted online vendors and shipments.
Anti-doping laboratories identify GW501516 and related metabolites using liquid chromatography coupled with tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be analyzed. The method targets the parent compound and phase I and phase II metabolites, which extend the detection window. Because the substance is prohibited at all times, athletes can be tested outside competition. Detection limits and windows depend on the assay, sample type, and individual metabolism.
| 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 |
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 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.
== January 16, 1982 (Saturday) == The United Kingdom and Vatican City established diplomatic relations at the ambassadorial level for the first time. In the state of Kerala in India, 24 people were killed in the sinking of an overcrowded boat as it was crossing Sasthamcotta Lake in poor weather, followed by a sinking of a boat that had come to the survivors' rescue."41 years since the Sasthamkotta Lake disaster", www.madhyamam.com (in Malayalam) Random drawings were held by FIFA at the Palacio de Congresos (Madrid) in Madrid for the grouping of the 24 teams that had qualified for the 1982 FIFA World Cup to be held in Spain starting on June 13. Of the 24 teams, divided by lot into six 4-team groups, 14 were UEFA members from Europe, 4 were CONMEBOL members from South America, 2 were CONCACAF teams from Central America, two from Africa, one (New Zealand) from Oceania and one (Kuwait) from the Middle East. National teams appearing for the first time in the World Cup were Honduras, New Zealand, Algeria, Cameroon and Kuwait. Born: Birgitte Hjort Sørensen, Danish stage, film and television actress known as co-star of the political drama series Borgen; in Hillerød Died: Marcel Francisci, 62, French businessman and smuggler accused of being the mastermind of the French Connection narcotics trafficking network, was shot to death in Paris as he was preparing to get into his car. Mahmud Yunus, 82, Indonesian Muslim preacher and author of 75 theological books
"Magic" is a 1974 song by Scottish pop rock band Pilot and was the first hit single for the group. It was written by band members David Paton and Billy Lyall for their debut album From the Album of the Same Name.
The King's College Criteria or the King's College Hospital criteria were devised in 1989 to determine if there were any early indices of poor prognosis in patients with acute liver failure. Acute liver failure is defined as the onset of encephalopathy (altered mental status) or coagulopathy (altered bleeding tendencies) within 26 weeks of a patient diagnosed with liver disease. Patients with hepatitis B acquired at birth, Wilson's disease and autoimmune hepatitis are included if their disease was identified within the past 26 weeks. These patients are very ill, and have a very high risk of dying of their illness without adequate treatment which may include liver transplantation. It is important that physicians find ways of identifying patients with acute liver failure early in their course who will do poorly, and may require liver transplantation. The King's College Criteria have consistently shown excellent operating characteristics for determining prognosis in these patients. As liver transplantation becomes a more accessible option for patients with acute liver failure, the King's College Criteria serve a role in determining which patients may require transplantation.
Sources: en.wikipedia.org
=== Early developments === The first cold breakfast cereal, Granula, was invented in the United States in 1863 by James Caleb Jackson, operator of Our Home on the Hillside which was later replaced by the Jackson Sanatorium in Dansville, New York. The cereal never became popular, due to the inconvenient necessity of tenderizing the heavy bran and graham nuggets by soaking them overnight. George H. Hoyt created Wheatena circa 1879, during an era when retailers would typically buy cereal (the most popular being cracked wheat, oatmeal, and cerealine) in barrel lots, and scoop it out to sell by the pound to customers. Hoyt, who had found a distinctive process of preparing wheat for cereal, sold his cereal in boxes, offering consumers a more sanitary and consumer-friendly option.
=== Claims of innocence === Norris appealed against his conviction in 2009. Originally, Norris planned to appeal on the grounds that the trial judge had shown a "lack of balance", but then scrapped these plans and sacked his legal team. He subsequently appealed on the grounds that the judge had "misdirected" the jury in his final summary but he lost this appeal, with judge Lord Justice Aikens ruling the convictions were "safe" and saying that the case against Norris was "very strong indeed". The appeal court rejected both grounds of the appeal, saying that the judge's directions "cannot validly be criticised" and that there was no misdirection to the jury. The appeal court instead said that the judge's summary in the original case was an exemplary "tour de force". The judges also refused to believe that the deaths were "coincidental". Norris's defence team had argued that the deaths could have been the result of 'naturally' raised insulin levels caused by severe spontaneous hypoglycaemia, but the judges rejected this possibility. On 4 October 2011, the BBC reported that retired Professor Vincent Marks – a leading expert on insulin poisoning – was concerned about Norris's conviction. He had been asked by the Norris family to find evidence in the case. He claimed the jury at Norris's trial was wrongly led to believe by experts that a cluster of hypoglycaemic episodes, among people who were not diabetic, was sinister. After carrying out his own studies, he said: "Looking at all the evidence, all I can say is I think Colin Norris's conviction is unsafe".
=== REM sleep deprivation === Norepinephrine prevents REM sleep, and lack of REM sleep increases noradrenaline secretion as a result of the locus coeruleus not ceasing producing it. It causes neurodegeneration if its loss is sustained for several days.
Sources: en.wikipedia.org
She was paired with antiques expert James Braxton and they purchased six items; a teddy bear, a tea trolley, a 9 carat gold bracelet, a silver charm bracelet, a Georg Jensen A/S silver broach and earrings, and a Baccarat caviar bowl, the latter of which Collins purchased for £30 and sold for £240, ultimately winning her the episode and finishing with an overall amount of £524.86. In December 2023, she appeared on The Real Full Monty: Jingle Balls in which celebrities strip naked and perform to raise money for various cancer charities. Collins decided to take part in the show after her mother found a lump in her breast and said "the thought of my mum, my best friend, having cancer blew my world apart." [...] adding that she was "so lucky to sit here today with [her mother's] breast cancer in remission and that she was doing [The Real Full Monty] for her mum to show her what an absolute queen she was [during treatment]." The same month, she appeared on an episode of Blankety Blank.
=== Pharmacodynamics === Gabapentin is a ligand of the α2δ calcium channel subunit. The α2δ-1 protein is coded by the CACNA2D1 gene. α2δ was first described as an auxiliary protein connected to the main α1 subunit (the channel-forming protein) of high voltage activated voltage-dependent calcium channels (L-type, N-type, P/Q type, and R-type). The same α2δ protein has more recently been shown to interact directly with some NMDA-type and AMPA-type glutamate receptors at presynaptic sites and also with thrombospondin (an extracellular matrix protein secreted by astroglial cells). Gabapentin is not a direct calcium channel blocker: it exerts its actions by disrupting the regulatory function of α2δ and its interactions with other proteins. Gabapentin reduces delivery of intracellular calcium channels to the cell membrane, reduces the activation of the channels by the α2δ subunit, decreases signaling to lead to neurotransmitters release, and disrupts interactions of α2δ with voltage gated calcium channels but also with NMDA receptors, neurexins, and thrombospondin. These proteins are found as mutually interacting parts of the presynaptic active zone, where numerous protein molecules interact with each other to enable and to regulate the release of neurotransmitters from presynaptic vesicles into the synaptic space. Out of the four known isoforms of α2δ protein, gabapentin binds with similar high affinity to two: α2δ-1 and α2δ-2. All of the pharmacological properties of gabapentin tested to date are explained by its binding to just one isoform – α2δ-1.
=== Synthetic analogues === Many vitamin B1 analogues, such as Benfotiamine, fursultiamine, and sulbutiamine, are synthetic derivatives of thiamine. Most were developed in Japan in the 1950s and 1960s as forms that were intended to improve absorption compared to thiamine. Some are approved for use in some countries as a drug or non-prescription dietary supplement for treatment of diabetic neuropathy or other health conditions.
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.
Legal status varies by country. It is not approved as a medicine, and it is prohibited in sport. Some jurisdictions restrict import, sale, or possession.