GW501516 raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.
Reviewed 2026-08-01. 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.
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.
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 |
|---|---|---|
| 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. |
Cardarine is a common name for GW501516, also GW-1516, a synthetic compound developed as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. It belongs to a class of agents that modulate gene transcription related to lipid and energy metabolism. The compound was studied in preclinical and early clinical research for metabolic and cardiovascular conditions, but it did not progress to approved therapeutic use. Its name appears in fitness and sports contexts despite not being approved as a drug.
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.
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.
Femarelle is a dietary supplement range containing DT56a, a tofu-derived soy extract, together with additional ingredients including flaxseed powder, vitamins, and minerals. DT56a has been studied for its potential activity as a selective estrogen receptor modulator (SERM), meaning that it may interact selectively with estrogen receptors in different tissues. Femarelle has been evaluated in several clinical studies investigating its possible role in supporting women during menopause, including studies on menopausal symptoms, vaginal health, bone health, and safety profile. Some studies reported encouraging findings, including improvements in menopausal symptoms and a favorable safety profile compared with traditional hormone replacement therapy, although the published trials were generally limited by relatively small sample sizes and short study durations. In 2008, an application was submitted to the European Food Safety Authority (EFSA) regarding a health claim related to bone mineral density and osteoporosis risk. EFSA concluded that the available evidence at that time was insufficient to establish a cause-and-effect relationship between Femarelle consumption and improvements in bone mineral density or reduction of osteoporosis risk in postmenopausal women.
== Table of techniques == In the table below, ambient ionization techniques are classified in the categories "extraction" (a solid or liquid extraction processes dynamically followed by spray or chemical ionization), "plasma" (thermal or chemical desorption with chemical ionization), "two step" (desorption or ablation followed by ionization), "laser" (laser desorption or ablation followed by ionization), "acoustic" (acoustic desorption followed by ionization), multimode (involving two of the above modes), other (techniques that do not fit into the other categories).
Over the following decade, numerous Half-Life games were canceled, including Episode Three, a version of Half-Life 3, Borealis, a Source 2 VR spin-off, and games developed by Junction Point Studios and Arkane Studios. In 2020, after years of speculation, Valve released Half-Life: Alyx, which was developed exclusively for virtual reality headsets. It is a prequel set five years before Half-Life 2, where players control Freeman's eventual ally Alyx Vance in her quest to rescue her father from Combine forces and uncover their mysterious "super-weapon". The Half-Life series is recognized by critics and industry experts for producing some of the most influential first-person shooter games for the genre, both of which have been highlighted for their advancements towards immersive and varied gameplay, level design, storytelling, visuals and sound. Half-Life and Half-Life 2, as well as Portal and Portal 2, have in particular been cited by numerous publications in being considered among the greatest video games ever made.
Sources: en.wikipedia.org
=== Brown fat cells === Brown fat cells are polyhedral in shape. Brown fat is derived from dermatomyocyte cells. Unlike white fat cells, these cells have considerable cytoplasm, with several lipid droplets scattered throughout, and are known as multilocular cells. The nucleus is round and, although eccentrically located, it is not in the periphery of the cell. The brown color comes from the large quantity of mitochondria. Brown fat, also known as "baby fat," is used to generate heat.
Countercurrent exchange is a mechanism between two flowing bodies flowing in opposite directions to each other, in which there is a transfer of some property, usually heat or some chemical. The flowing bodies can be liquids, gases, or even solid powders, or any combination of those. For example, in a distillation column, the vapors bubble up through the downward flowing liquid while exchanging both heat and mass. It occurs in nature and is mimicked in industry and engineering. It is a kind of exchange using counter flow arrangement. The maximum amount of heat or mass transfer that can be obtained is higher with countercurrent than co-current (parallel) exchange because countercurrent maintains a slowly declining difference or gradient (usually temperature or concentration difference). In cocurrent exchange the initial gradient is higher but falls off quickly, leading to wasted potential. For example, in the adjacent diagram, the fluid being heated (exiting top) has a higher exiting temperature than the cooled fluid (exiting bottom) that was used for heating. With cocurrent or parallel exchange the heated and cooled fluids can only approach one another. The result is that countercurrent exchange can achieve a greater amount of heat or mass transfer than parallel under otherwise similar conditions. Countercurrent exchange when set up in a circuit or loop can be used for building up concentrations, heat, or other properties of flowing liquids.
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Sources: en.wikipedia.org
== Tissues distribution == Studies have reported that humans express FFAR3 in their: (a) enteroendocrine L cells and K cells of the intestines; (b) endothelium of blood vessels in the frontal cortex of the brain, pancreatic β-cells, and adipose. i.e., fat, tissue (but not in mouse adipose tissue); (c) the vascular endothelium of the myometrium, the epithelium of the amnion, chorion and placenta, and certain immune cells in these tissues of pregnant women; (d) the hippocampus of the brain; (e) sympathetic ganglia, i.e., autonomic ganglia of the sympathetic nervous system; (f) certain types of immune cells, i.e., blood monocytes (but not mouse monocytes), basophils, dendritic cells derived from human monocytes isolated from whole blood, and the tissues containing these blood cells, i.e., the bone marrow, spleen, lymph nodes, and thymus; and (g) alveolar macrophages, and macrophages in various other tissues; and (h) certain immortalised cell lines, i.e., MCF-7 breast cancer, HCT116 colorectal cancer, HEK293 embryonic kidney, U937 leukemic promonocyte, THP-1 leukemic monocyte, EoL-1 leukemic eosinophil, Jurcat leukemic T lymphocyte, MOLT-4 T lymphoblast leukemic, and HL60 acute myeloid leukemia cells (but only when the HL60 cells are pre-treated with phorbol 12-myristate 13-acetate to promote their cellular differentiation). As noted, the expression of FFAR3 in the cells and tissues of animals are not always the same as those in humans.
=== Liquid chromatography === Liquid chromatography (LC) is a method that in some ways is more powerful than GC, but can be coupled to mass spectrometry just as easily. In LC, the concerns involving sample preparation can be minimal. In LC, both the stationary and mobile phase can affect the separation, whereas in GC only the stationary phase should be influential. This allows for the sample preparation to be minimal if one is willing to adjust the stationary phase or mobile phase before running the sample. The primary concern is the concentration of analyte. If the concentration is too high then separation can be unsuccessful, but mass spectrometry as a detection method does not need complete separation, showing another benefit of coupling LC to a mass spectrometer. LC can be coupled to mass spectrometry through the vaporization of the liquid samples as they enter the mass spectrometer. This method can allow for ionization methods that require gaseous samples to be used, such as CI or PI, particularly atmospheric-pressure chemical ionization or atmospheric pressure photoionization, which allows for more interactions and more ionization. Other ionization methods may not require the liquid sample to be vaporized, and can analyze the liquid sample itself. One example is fast-atom bombardment ionization which can allow for liquid samples separated by the LC to flow into the ionization chamber and be ionized easily.
== Structure and function == Many structural domains have been conserved through evolution, as prokaryotic initiation factors share similar structures with eukaryotic factors. The prokaryotic initiation factor, IF3, assists with start site specificity, as well as mRNA binding. This is in comparison with the eukaryotic initiation factor, eIF1, who also performs these functions. The elF1 structure is similar to the C-terminal domain of IF3, as they each contain a five-stranded beta sheet against two alpha helices. The prokaryotic initiation factors IF1 and IF2 are also homologs of the eukaryotic initiation factors eIF1A and eIF5B. IF1 and eIF1A, both containing an OB-fold, bind to the A site and assist in the assembly of initiation complexes at the start codon. IF2 and eIF5B assist in the joining of the small and large ribosomal subunits. The eIF5B factor also contains elongation factors. Domain IV of eIF5B is closely related to the C-terminal domain of IF2, as they both consist of a beta-barrel. The elF5B also contains a GTP-binding domain, which can switch from an active GTP to an inactive GDP. This switch helps to regulate the affinity of the ribosome for the initiation factor.
An RF value will always be in the range 0 to 1; if the substance moves, it can only move in the direction of the solvent flow, and cannot move faster than the solvent. For example, if particular substance in an unknown mixture travels 2.5 cm and the solvent front travels 5.0 cm, the retardation factor would be 0.50. One can choose a mobile phase with different characteristics (particularly polarity) in order to control how far the substance being investigated migrates. An RF value is characteristic for any given compound (provided that the same stationary and mobile phases are used). It can provide corroborative evidence as to the identity of a compound. If the identity of a compound is suspected but not yet proven, an authentic sample of the compound, or standard, is spotted and run on a TLC plate side by side (or on top of each other) with the compound in question. Note that this identity check must be performed on a single plate, because it is difficult to duplicate all the factors which influence RF exactly from experiment to experiment.
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.
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.