If you have been reading about Nuclear receptor and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.
Updated 2026-02-27. Numbers and descriptions here follow the published literature rather than marketing material.
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.
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.
Cardarine is frequently described as a fat-burning or endurance-enhancing supplement, but these claims exceed the available evidence. The compound is not a hormone, steroid, or selective androgen receptor modulator. Research articles discuss it as a tool compound for studying PPARδ biology, while anti-doping literature focuses on its abuse and detection. Quality of unapproved products is uncertain, and independent analyses have found impurities or incorrect labeling. Open questions include whether human cancer risk resembles that seen in rodents and how often non-athletes use the substance.
| Property | Value | Notes |
|---|---|---|
| Molecular target | PPAR delta (NR1C2) | Ligand-activated nuclear receptor. |
| Primary tissues studied | Skeletal muscle, liver, adipose | Effects on fatty acid oxidation and energy use. |
| Typical detection matrix | Urine | Used in anti-doping analysis. |
| Common analytical method | LC-MS/MS | Detects parent compound and metabolites. |
| Sport regulatory class | Prohibited at all times | Listed as a metabolic modulator by WADA. |
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.
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.
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.
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.
Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.
Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.
In June 1911, while attending a conference in Stettin, Hahn met Edith Junghans (1887–1968), a student at the Royal School of Art in Berlin. They saw each other again in Berlin, and became engaged in November 1912. On 22 March 1913 the couple were married in Stettin, where Edith's father, Paul Ferdinand Junghans, was a high-ranking law officer and President of the City Parliament until his death in 1915. After a honeymoon at Punta San Vigilio on Lake Garda in Italy, they visited Vienna, and then Budapest, where they stayed with George de Hevesy. They had one child, Hanno Hahn, who was born on 9 April 1922. Hanno enlisted in the army in 1942, and served on the Eastern Front in World War II as a panzer commander. He lost an arm in combat. After the war he became an art historian and architectural researcher (at the Hertziana in Rome), known for his discoveries in the early Cistercian architecture of the 12th century. In August 1960, while on a study trip in France, Hanno died in a car accident, together with his wife and assistant Ilse Hahn née Pletz. They left a fourteen-year-old son, Dietrich Hahn. In 1990, the Hanno and Ilse Hahn Prize for outstanding contributions to Italian art history was established in memory of Hanno and Ilse Hahn to support young and talented art historians. It is awarded biennially by the Bibliotheca Hertziana – Max Planck Institute for Art History in Rome.
==== Autonomous republics ==== All sixteen republics under the Russian SFSR Crimean ASSR under Ukraine Karakalpak ASSR under Uzbekistan Abkhaz SSR (former ASSR under Georgia, which had declared independence)
Meanwhile, workers in the platelet, extracellular matrix, and cell surface fields were also working on multi-subunit receptors. The platelet receptor for fibrinogen contained two glycoprotein subunits termed IIb and IIIa. A monoclonal antibody to a cell surface receptor that blocked cell adhesion to laminin and fibronectin reacted with three distinct subunits in the same molecular weight range as αLβ, αMβ, αXβ, and IIb/IIIa. Proteins with high molecular weight, sharing a common subunit, were identified on lymphocytes and non-hematopoietic cells. After the discovery that an RGD motif in fibronectin is sufficient for recognition by its receptor and common to other extracellular proteins, the fibronectin and vitronectin receptors were isolated and their sequences determined and platelet protein IIb/IIIa was also shown to recognize RGD. Sequences of these receptors showed that their alpha subunit sequences were homologous to one another and to those earlier reported for LFA-1 (αLβ) and Mac-1 (αMβ). A large number of other papers appeared in 1986-1987 reporting further sequences and relationships among these receptors, including from the Springer lab on the β-subunit shared by LFA-1 (αLβ), Mac-1 (αMβ), and αXβ. Richard Hynes chaired the 1987 Gordon Research Conference on Fibronectin. Hynes had worked on fibronectin, and in 1986 his group isolated a cDNA encoding a subunit recognized by an antibody to the laminin and fibronectin receptors, which he named integrin.
As anti-angiogenic cancer therapies have achieved widespread use, there has been increased interest in non-invasive monitoring of angiogenesis. One of the most extensively examined targets of angiogenesis is integrin αVβ3. Radiolabeled peptides containing RGD show high affinity and selectivity for integrin αVβ3 and are being investigated as tools to monitor treatment response of tumors via PET imaging. These include 18F-Galacto-RGD, 18F-Fluciclatide-RGD, 18F-RGD-K5, 68Ga-NOTA-RGD, 68Ga-NOTA-PRGD2, 18F-Alfatide, 18F-Alfatide II, and 18F-FPPRGD2. In a meta-analysis of studies using PET/CT in patients with cancer, it was shown that this diagnostic method may be very useful for detecting malignancies and predicting short-term outcomes, although larger-scale studies are needed.
Sources: en.wikipedia.org
Canagliflozin, sold under the brand name Invokana among others, is a medication used to treat type 2 diabetes. It is used together with exercise and diet. It is not recommended in type 1 diabetes. It is taken by mouth. Common side effects include vaginal yeast infections, nausea, constipation, and urinary tract infections. Serious side effects may include low blood sugar, Fournier's gangrene, leg amputation, kidney problems, high blood potassium, and low blood pressure. Diabetic ketoacidosis may occur despite nearly normal blood sugar levels. Use in pregnancy and breastfeeding is not recommended. Canagliflozin is a sodium-glucose cotransporter-2 (SGLT2) inhibitor. It works by increasing the amount of glucose lost in the urine. Canagliflozin was approved for medical use in the United States, in the European Union, and in Australia in 2013. It is on the World Health Organization's List of Essential Medicines.
The discovery was made throughout a series of experiments in the 1960s that discovered that reduced and denatured RNase in its unfolded form could refold into the native tertiary form. The tertiary structure of a protein is a fully folded polypeptide chain with all hydrophobic R-groups folded into the interior of the protein to maximize entropy with interactions between secondary structures such as beta sheets and alpha helixes. Since the structure of proteins determines its function, it is critical that a protein be folded correctly into its tertiary form so that the protein will function properly. However, it is important to note that polypeptide chains may differ vastly in primary structure, but be very similar in tertiary structure and protein function.
The Bowery () is a street and neighborhood in Lower Manhattan in New York City, New York. The street runs from Chatham Square at Park Row, Worth Street, and Mott Street in the south to Cooper Square at 4th Street in the north. The eponymous neighborhood runs roughly from the Bowery east to Allen Street and First Avenue, and from Canal Street north to Cooper Square/East Fourth Street. The neighborhood roughly overlaps with Little Australia. To the south is Chinatown, to the east are the Lower East Side and the East Village, and to the west are Little Italy and NoHo. It has historically been considered a part of the Lower East Side of Manhattan. In the 17th century, the road branched off Broadway north of Fort Amsterdam at the tip of Manhattan to the homestead of Peter Stuyvesant, director-general of New Netherland. The street was known as Bowery Lane prior to 1807. "Bowery" is an anglicization of the Dutch bouwerie, derived from an antiquated Dutch word for "farm": In the 17th century the area contained many large farms. The New York City Subway's Bowery station, serving the BMT Nassau Street Line (J and Z trains), is located close to the Bowery's intersection with Delancey and Kenmare Streets. There is a tunnel under the Bowery at Confucius Plaza, intended for use by a never-completed portion of the Second Avenue Subway. The M103 bus runs on the entire Bowery.
=== Calcium ion channels === Calcium channels are important for certain cell-signaling cascades as well as neurotransmitter release at axon terminals. A variety of different types of calcium ion channels are found in excitable cells. As with sodium ion channels, calcium ion channels have been isolated and cloned by chromatographic purification techniques. It is notable, as with the case of neurotransmitter release, that calcium channels can interact with intracellular proteins and plays a strong role in signaling, especially in locations such as the sarcoplasmic reticulum of muscle cells.
high in certain proteinase inhibitors that suppress appetite - e.g. potatoes solid (which takes longer to digest than liquid foods, though liquids have high satiety for a short period) The protein leverage hypothesis posits that human beings will prioritize the consumption of protein in food over other dietary components, and will eat until protein needs have been met, regardless of energy content, thus leading of over-consumption of foodstuffs when their protein content is low. Sugar-sweetened beverages showed lower satiety compared to isocaloric semi-skimmed milk. Alcoholic beverages tend to have a lower satiety per calorie. Fruit juice with and without pulp was shown to result in lower satiety than comparable amounts of fruits.
Sources: en.wikipedia.org
=== Protein === Additional research on sponge proteins found that of 42 sponge proteins that were analysed, all of them had homologous proteins that are found in humans. An identity score of 53% was given to the similarity among sponge and human proteins, compared to a score of 42% when the same sequence was compared to that of C. elegans.
The treatment of choice for this condition is the surgical application of epidural blood patches, which has a higher success rate than conservative treatments of bed rest and hydration. Through the injection of a person's own blood into the area of the hole in the dura, an epidural blood patch uses blood's clotting factors to clot the sites of holes. The volume of autologous blood and number of patch attempts for patients is highly variable. One-quarter to one-third of those with a sCSFL patients do not have relief of symptoms from epidural blood patching. Finding the location of a cerebrospinal fluid leak is not required prior to using an epidural blood patch as initial lumbar epidural blood patches often provide relief of symptoms and resolve the leak without further intervention.
== Analytical method == Protein deamidation has been commonly analyzed by reverse-phase liquid chromatography (RPLC) through peptide mapping. Recently reported novel ERLIC-MS/MS method would enhance the separation of deamidated and non-deamidated peptides with increased identification and quantitation quantification. Mass spectrometry is commonly used to characterize deamidation states of proteins, including therapeutic monoclonal antibodies. The technique is especially useful for deamidation analysis due to its high sensitivity, speed, and specificity. This allows site-specific deamidation analysis. A major challenge of using mass spectrometry is the formation of deamidation artifacts during sample preparation. These artifacts significantly skew results because they suggest greater rates of spontaneous deamidation than what is truly observed. This can prove problematic in the case of therapeutic proteins which can be mischaracterized in QC protocols if a large percentage of detected deamidation is due to artifacts. Recent studies indicate that lower pH can reduce the rate of deamidation artifacts.
3 April The U.S. Department of Defense announced that the death toll for American soldiers in the war had exceeded the 32,629 who had died in the Korean War, based on 312 additional deaths during the week from March 22 to March 28 to bring the toll to 33,641. Laird announced that the U.S. sought to "Vietnamize" the war as quickly as possible but that troop withdrawals would not take place while the PAVN/VC was conducting attacks.
Sources: en.wikipedia.org
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.
Early-stage trials examined lipid and glucose markers, but the development program was discontinued. Published human results are limited and do not support approved use for any indication. Claims of performance or health benefits remain unproven.
Yes. Laboratories use LC-MS/MS to detect GW501516 and its metabolites in urine. Detection depends on timing and sensitivity, but the substance is banned at all times.
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.