This is a working overview of PPARδ, written for readers who want more than a one-paragraph summary but less than a textbook.
Reviewed 2025-09-21. Anything still debated is marked as such rather than presented as settled.
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.
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.
Detection of GW501516 in biological samples generally relies on liquid chromatography coupled with tandem mass spectrometry. Urine is a common matrix in anti-doping analysis, while blood or plasma may be used in research settings. Sample preparation can involve enzymatic hydrolysis, protein precipitation, or solid-phase extraction before instrumental analysis. Because the compound undergoes metabolism, assays may target the parent molecule, one or more metabolites, or both. Detection windows are not fixed; they depend on factors such as dose, route, individual metabolism, and assay sensitivity. Reference standards are required for accurate identification and quantification.
Handling and quality assessment of cardarine reference material follow general laboratory practices for poorly characterized compounds. It typically appears as a white to off-white powder and is sparingly soluble in water but soluble in organic solvents such as dimethyl sulfoxide and ethanol. Storage recommendations usually specify a cool, dry, dark place, with long-term storage at low temperature and desiccation. Purity may be checked by high-performance liquid chromatography with ultraviolet detection, while identity is confirmed by mass spectrometry and nuclear magnetic resonance. No pharmacopeial monograph exists, so reported purity and stability depend on the supplier’s methods.
GW501516 acts as a selective agonist at PPARδ, a nuclear receptor that regulates transcription of genes involved in lipid handling and energy metabolism. Activation of PPARδ in preclinical models increases fatty acid oxidation, mitochondrial biogenesis, and exercise endurance in rodents. These effects have made the compound a subject of metabolic research and also a target for sport anti-doping rules. In humans, however, controlled studies are limited, and whether similar endurance or metabolic changes occur at tolerated exposures remains an open question. The receptor’s broad tissue distribution also means downstream effects may vary by organ and condition.
| Property | Value | Notes |
|---|---|---|
| Common synonyms | GW501516, GW-501516, GW 501516, endurobol | Names vary in research and anti-doping documents. |
| Chemical class | Synthetic PPARδ agonist | Small-molecule nuclear receptor ligand. |
| CAS Registry Number | 317318-70-0 | Identifier commonly associated with GW501516. |
| Appearance | White to off-white powder | Typical for purified research material. |
| Solubility | Low in water; soluble in DMSO and ethanol | Organic solvents are common for laboratory stock solutions. |
== History == Oxymorphone was first developed in Germany in 1914, and patented in the US by Endo Pharmaceuticals in 1955. It was introduced in the United States in January 1959 and other countries around the same time.
Temozolomide, sold under the brand name Temodar among others, is an anticancer medication used to treat brain tumors such as glioblastoma and anaplastic astrocytoma. It is taken by mouth or via intravenous infusion. The most common side effects with temozolomide are nausea, vomiting, constipation, loss of appetite, alopecia (hair loss), headache, fatigue, convulsions (seizures), rash, neutropenia or lymphopenia (low white-blood-cell counts), and thrombocytopenia (low blood platelet counts). People receiving the solution for infusion may also have injection-site reactions, such as pain, irritation, itching, warmth, swelling and redness, as well as bruising. Temozolomide is an alkylating agent used to treat serious brain cancers; most commonly as second-line treatments for astrocytoma and as the first-line treatment for glioblastoma. Olaparib in combination with temozolomide demonstrated substantial clinical activity in relapsed small cell lung cancer. It is available as a generic medication.
== Metabolism == Telithromycin is metabolized mainly in the liver, the main elimination route being the bile, a small portion is also excreted into the urine. About one third is excreted unchanged in bile and urine, the biliary route being favoured. Telithromycin's half-life is approximately ten hours.
For psoriasis, UVB phototherapy has been shown to be effective. A feature of psoriasis is localized inflammation mediated by the immune system. Ultraviolet radiation is known to suppress the immune system and reduce inflammatory responses. Light therapy for skin conditions like psoriasis usually use 313 nanometer UVB though it may use UVA (315–400 nm wavelength) or a broader spectrum UVB (280–315 nm wavelength). UVA combined with psoralen, a drug taken orally, is known as PUVA treatment. In UVB phototherapy the exposure time is very short, seconds to minutes depending on intensity of lamps and the person's skin pigment and sensitivity.
Sources: en.wikipedia.org
=== As feed === The larvae of the litter beetle, like certain other larvae of darkling beetles such as mealworms, are used as animal feed, e.g., fed to captive reptiles. They have been reported as a good first food for Central American wood turtle (Rhinoclemmys pulcherrima mannii) hatchlings, because they are more active than common mealworms and their movement stimulates feeding behavior.
== June 6, 1915 (Sunday) == Third Battle of Krithia — British general Aylmer Hunter-Weston managed to reorganize the Allied forces into an effective defense on the coast of Gallipoli and beat back the Ottoman defense, inflicting 3,000 casualties and forcing a stalemate. Second Battle of Artois — The French captured the main road leading to Neuville-Saint-Vaast, France. British carrier SS Immingham was lost in the Mediterranean Sea. Switzerland held a referendum on a war tax with most voters, over 450,000 (94 percent of electorate), in favor on implementing the one-off tax and over 27,000 against (about 6 percent). It was the first time a referendum has passed in every Swiss canton. The BHP Newcastle Steelworks opened in Newcastle, New South Wales, Australia. The London Underground extended the Bakerloo line with a new tube station at Maida Vale. The Icelandic sports club Þór Akureyri was established, and now encompasses teams for association football, basketball, handball and taekwondo.
target site The site or locus upon another molecule at which a protein performs a particular biochemical activity; e.g. the nucleotide motif at which a restriction endonuclease cleaves a DNA molecule, often but not necessarily the same as the enzyme's recognition site (i.e. a restriction enzyme may recognize one motif, known as a restriction site, and cleave at another).
== Co-discovery of insulin == Best moved in 1915 to Toronto, Ontario, where he started studying towards a bachelor of arts degree at University College, University of Toronto. In 1918, he enlisted in the Canadian Army serving with the 2nd Canadian Tank Battalion. After the war, he completed his degree in physiology and biochemistry. As a 22-year-old medical student at the University of Toronto he worked as an assistant to the surgeon Dr. Frederick Banting and contributed to the discovery of the pancreatic hormone insulin, which led to an effective treatment for diabetes. In the spring of 1921, Banting travelled to Toronto to visit John Macleod, professor of physiology at the University of Toronto, and asked Macleod if he could use his laboratory to isolate pancreatic extracts from dogs. Macleod was initially sceptical, but eventually agreed before leaving on holiday for the summer. Before leaving for Scotland he supplied Banting with ten dogs for experiment and two medical students, Charles Best and Edward Clark Noble, as lab assistants. It was reported that Best and Noble flipped a coin to see who would assist Banting during the first period of four weeks. According to Best, however, this was the product of a journalist’s imagination, or "newspaper fiction". Nonetheless, Frederick Banting is known to have mentioned this story when discussing the discovery of insulin.
For the Cossack elite, noble status within the empire came at the price of their old liberties in the 18th century. Advancing agricultural settlement began to force the Cossacks to give up their traditional nomadic ways and adopt new forms of government. The government steadily changed the entire culture of the Cossacks. Peter the Great increased Cossack service obligations, and mobilized their forces to fight in far-off wars. Peter began establishing non-Cossack troops in fortresses along the Yaik River. In 1734, construction of a government fortress at Orenburg gave Cossacks a subordinate role in border defense. When the Yaik Cossacks sent a delegation to Peter with their grievances, Peter stripped the Cossacks of their autonomous status, and subordinated them to the War College rather than the College of Foreign Affairs. This consolidated the Cossacks' transition from border patrol to military servicemen. Over the next fifty years, the central government responded to Cossack grievances with arrests, floggings, and exiles. Under Catherine the Great, beginning in 1762, the Russian peasants and Cossacks again faced increased taxation, heavy military conscription, and grain shortages, as before Razin's rebellion. Peter III had extended freedom to former church serfs, freeing them from obligations and payments to church authorities, and had freed other peasants from serfdom, but Catherine did not follow through on these reforms. In 1767, the Empress refused to accept grievances directly from the peasantry.
Sources: en.wikipedia.org
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.
No. Cardarine is not a steroid hormone; it targets the nuclear receptor PPARδ. Its classification in anti-doping rules differs from anabolic steroids, though it remains prohibited in sport.
Early rodent studies reported tumor formation at multiple sites, which raised safety concerns. Sponsors stopped clinical development, and no approved human product exists.
Cardarine targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not bind the androgen receptor in the way SARMs do.