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 2025-12-15. Numbers and descriptions here follow the published literature rather than marketing material.
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.
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.
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.
| 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. |
== Use == Like other alkylalkanolamines, N-methylethanolamine is used in water- and solvent-based paints and coatings as a solubilizer for other components, such as pigments and as a stabilizer. In cathodic dip-coating, N-methylaminoethanol serves as cation neutralizer for the partial neutralization of the epoxy resin. It also serves as a chain extender in the reaction of high molecular weight polyepoxides with polyols. Being a base, N-methylaminoethanol forms neutral salts with fatty acids, which are used as surfactants (soaps) with good emulsifying properties and find applications in textile and personal care cleansing products. When bleaching cotton-polyester blends, NMEA is used as a brightener. By methylation of N-methylaminoethanol, dimethylaminoethanol and choline [(2-hydroxyethyl)-trimethyl-ammonium chloride] can be prepared. In the reaction of N-methylaminoethanol with fatty acids, long-chain N-methyl-N-(2-hydroxyethyl)amides are formed upon elimination of water. These are used as neutral surfactants. Such amides also act as flow improvers and pour point depressants in heavy oils and middle distillates. By catalytic oxidation of N-methylaminoethanol, the non-proteinogenic amino acid sarcosine is obtained. N-methylaminoethanol plays a role as a building block for the synthesis of crop protection compounds and pharmaceuticals, such as in the first stage of the reaction sequence to the antihistamine and antidepressant mianserin (Tolvin) and to the non-analgesic Nefopam (Ajan).
edulis in Sweden after 1818, and is honoured in the local vernacular name Karljohanssvamp, as well as the Danish name Karl Johan svamp. The monarch cultivated the fungus about his residence, Rosersberg Palace.
Therefore, it has been hypothesized that the presence of supercritical CO2 in Hadean hydrothermal vents played an important role in the origin of life. There is some evidence that links the origin of life to alkaline hydrothermal vents in particular. The pH conditions of these vents may have made them more suitable for emerging life. One current theory is that the naturally occurring proton gradients at these deep sea vents supplemented the lack of phospholipid bilayer membranes and proton pumps in early organisms, allowing ion gradients to form despite the lack of cellular machinery and components present in modern cells. There is some discourse around this topic. It has been argued that the natural pH gradients of these vents playing a role in the origin of life is actually implausible. The counter argument relies, among other points, on what the author describes as the unlikelihood of the formation of machinery which produces energy from the pH gradients found in hydrothermal vents without/before the existence of genetic information. This counterpoint has been responded to by Nick Lane, one of the researchers whose work it focuses on. He argues that the counterpoint largely misinterprets both his work and the work of others. Another reason that the view of deep sea hydrothermal vents as an ideal environment for the origin of life remains controversial is the absence of wet-dry cycles and exposure to UV light, which promote the formation of membranous vesicles and synthesis of many biomolecules.
Sources: en.wikipedia.org
== History == Acetone peroxide (specifically, triacetone triperoxide) was discovered in 1895 by a German chemist, Richard Wolffenstein. Wolffenstein combined acetone and hydrogen peroxide. Then he allowed the mixture to stand for a week at room temperature, during which time a small quantity of crystals precipitated, which had a melting point of 97 °C (207 °F). In 1899, Adolf von Baeyer and Victor Villiger described the first synthesis of the dimer and described use of acids for the synthesis of both peroxides. Baeyer and Villiger prepared the dimer by combining potassium persulfate in diethyl ether with acetone, under cooling. After separating the ether layer, the product was purified and found to melt at 132–133 °C (270–271 °F). They found that the trimer could be prepared by adding hydrochloric acid to a chilled mixture of acetone and hydrogen peroxide. By using the depression of freezing points to determine the molecular weights of the compounds, they also determined that the form of acetone peroxide that they had prepared via potassium persulfate was a dimer, whereas the acetone peroxide that had been prepared via hydrochloric acid was a trimer, like Wolffenstein's compound. Work on this methodology and on the various products obtained, was further investigated in the mid-20th century by Milas and Golubović.
=== Inhibin === Quantification of inhibin A is part of the prenatal quad screen that can be administered during pregnancy at a gestational age of 16–18 weeks. An elevated inhibin A (along with an increased beta-hCG, decreased AFP, and a decreased estriol) is suggestive of the presence of a fetus with Down syndrome. As a screening test, abnormal quad screen test results need to be followed up with more definitive tests. It also has been used as a marker for ovarian cancer. Inhibin B may be used as a marker of spermatogenesis function and male infertility. The mean serum inhibin B level is significantly higher among fertile men (approximately 140 pg/mL) than in infertile men (approximately 80 pg/mL). In men with azoospermia, a positive test for inhibin B slightly raises the chances for successfully achieving pregnancy through testicular sperm extraction (TESE), although the association is not very substantial, having a sensitivity of 0.65 (95% confidence interval [CI]: 0.56–0.74) and a specificity of 0.83 (CI: 0.64–0.93) for prediction the presence of sperm in the testes in non-obstructive azoospermia.
Confirmatory testing: compounds that were found active against the selected target are re-tested using the same assay conditions used during the HTS to make sure that the activity is reproducible. Dose response curve: the compound is tested over a range of concentrations to determine the concentration that results in half maximal binding or activity (IC50 or EC50 value respectively). Orthogonal testing: confirmed hits are assayed using a different assay which is usually closer to the target physiological condition or using a different technology. Secondary screening: confirmed hits are tested in a functional cellular assay to determine efficacy. Synthetic tractability: medicinal chemists evaluate compounds according to their synthesis feasibility and other parameters such as up-scaling or cost of goods. Biophysical testing: nuclear magnetic resonance (NMR), isothermal titration calorimetry (ITC), dynamic light scattering (DLS), surface plasmon resonance (SPR), dual polarisation interferometry (DPI), microscale thermophoresis (MST) are commonly used to assess whether the compound binds effectively to the target, the kinetics, thermodynamics, and stoichiometry of binding, any associated conformational change and to rule out promiscuous binding. Hit ranking and clustering: Confirmed hit compounds are then ranked according to the various hit confirmation experiments. Freedom to operate evaluation: hit structures are checked in specialized databases to determine if they are patentable.
Sources: en.wikipedia.org
== External links == Ashton CH (2002). Benzodiazepines: how they work & how to withdraw (aka The Ashton Manual). Archived from the original on 17 July 2023. Retrieved 4 May 2024. Ashton CH (2007). "Benzodiazepine equivalence table". Fruchtengarten L (April 1998). Ruse M (ed.). "Benzodiazepines". Poisons Information Monograph (Group monograph) G008. International Programme on Chemical Safety INCHEM. Retrieved 9 June 2009. Longo LP, Johnson B (April 2000). "Addiction: Part I. Benzodiazepines—side effects, abuse risk and alternatives". American Family Physician. 61 (7): 2121–2128. PMID 10779253. Archived from the original on 12 May 2008. Retrieved 25 May 2008.
80 K-H Phosphoprotein (Protein Kinase C Substrate) (AGE-R2): The 80 K-H phosphoprotein, also known as protein kinase C substrate (AGE-R2), is involved in the intracellular signaling response to AGE exposure. AGE-R2 plays a role in regulating pathways that help cells adapt to oxidative stress by modulating protein kinase C (PKC) activity. This regulation aids in maintaining cellular homeostasis and mitigating the harmful effects of AGEs on cellular structures, ultimately contributing to the cell's resilience against oxidative stress. Galectin-3 (AGE-R3): Galectin-3, a member of the lectin family, is a multifunctional receptor that binds to AGEs and helps clear them from the extracellular space. This receptor is known for its involvement in modulating apoptosis, cell proliferation, and immune responses. Upon binding AGEs, Galectin-3 activates downstream signaling pathways, including those involving mitogen-activated protein kinases (MAPKs) and nuclear factor kappa B (NF-κB), which are crucial for inflammatory regulation. By mediating these pathways, Galectin-3 reduces the pro-inflammatory effects of AGE accumulation and helps maintain tissue integrity. Its role in regulating apoptosis and immune cell recruitment further contributes to limiting AGE-induced tissue damage, thus playing a protective role in chronic inflammatory and fibrotic conditions. LOX-1 (Lectin-like Oxidized Low-Density Lipoprotein Receptor-1): LOX-1 is primarily known for binding oxidized low-density lipoproteins (oxLDL) but also binds AGEs.
=== 2019 car accident handling === In June 2019, Morgan was involved in a minor collision in his newly purchased Bugatti Veyron, and he was captured on video slamming on the other driver's window and yelling, "Bitch, get out of the car". According to Mercury News, the other driver was traumatized by Morgan's conduct. A CBS News reporter visited Morgan to get his side of the story and Morgan allowed the reporter through his gate, answered the door himself, but refused to talk.
The two components of the proton-motive force are thermodynamically equivalent: In mitochondria, the largest part of energy is provided by the potential; in alkaliphile bacteria the electrical energy even has to compensate for a counteracting inverse pH difference. Inversely, chloroplasts operate mainly on ΔpH. However, they also require a small membrane potential for the kinetics of ATP synthesis. In the case of the fusobacterium Propionigenium modestum it drives the counter-rotation of subunits a and c of the FO motor of ATP synthase. The amount of energy released by oxidative phosphorylation is high, compared with the amount produced by fermentation. Glycolysis produces only 2 ATP molecules, but somewhere between 30 and 36 ATPs are produced by the oxidative phosphorylation of the 10 NADH and 2 succinate molecules made by converting one molecule of glucose to carbon dioxide and water, while each cycle of beta oxidation of a fatty acid yields about 14 ATPs. These ATP yields are theoretical maximum values; in practice, some protons leak across the membrane, lowering the yield of ATP.
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.