A practical reference on Nuclear receptor: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
This page was last updated on 2026-01-14 and is reviewed periodically as new material appears.
Cardarine is a common name for GW501516, an investigational compound developed in the 1990s for metabolic conditions. It acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in lipid and energy metabolism. The compound is frequently mislabeled as a selective androgen receptor modulator, or SARM, but its molecular target is different. GW501516 reached early clinical testing before development was discontinued. It has no approved therapeutic use in any country. The name cardarine is not a formal international nonproprietary name.
Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.
Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.
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.
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.
| Property | Value | Notes |
|---|---|---|
| Common synonyms | GW501516; GW-1516; endurobol | GW501516 is the research code |
| Drug class | PPARδ agonist | Not a selective androgen receptor modulator |
| Molecular formula | C21H18F3NO3S2 | Established chemical formula |
| Molar mass | 453.5 g/mol | Calculated from the formula |
| Regulatory status | Prohibited in sport; not approved as medicine | Status varies by country |
GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.
Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.
Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.
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.
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.
Met-enkephalin, also known as metenkefalin (INN), sometimes referred to as opioid growth factor (OGF), is a naturally occurring, endogenous opioid peptide that has opioid effects of a relatively short duration. It is one of the two forms of enkephalin, the other being leu-enkephalin. The enkephalins are considered to be the primary endogenous ligands of the δ-opioid receptor, due to their high potency and selectivity for the site over the other endogenous opioids.
LC-MS is particularly amenable to detecting hydrophobic molecules (lipids, fatty acids) and peptides while GC-MS is best for detecting small molecules (<500 Da) and highly volatile compounds (esters, amines, ketones, alkanes, thiols). Unlike the genome or even the proteome, the metabolome is a highly dynamic entity that can change dramatically, over a period of just seconds or minutes. As a result, there is growing interest in measuring metabolites over multiple time periods or over short time intervals using modified versions of NMR or MS-based metabolomics.
Activation of this M2 receptor then activates a protein called a G-protein (in particular Gi protein, i for inhibitory). Activation of this G-protein blocks the cAMP pathway, reducing its effects, therefore inhibiting sympathetic activity and slowing action potential production. The G-protein also activates a potassium channel GIRK-1 and GIRK-4, which allows K+ to flow out of the cell, making the membrane potential more negative and slowing the pacemaker potential, therefore decreasing the rate of action potential production and therefore decreasing heart rate. A decrease in heart rate is known as negative chronotropy. The first cell to produce the action potential in the SA node isn't always the same; this is known as pacemaker shift. In certain species of animals—for example, in dogs—a superior shift (i.e., the cell that produces the fastest action potential in the SA node is higher than previously) usually produces an increased heart rate whereas an inferior shift (i.e. the cell producing the fastest action potential within the SA node is further down than previously) produces a decreased heart rate.
== Growth and morphology == In nature, P. digitatum adopts a filamentous vegetative growth form, producing narrow, septate hyphae. The hyphal cells are haploid, although individual hyphal compartments may contain many genetically identical nuclei. During the reproductive stages of its life cycle, P. digitatum reproduces asexually via the production of asexual spores or conidia. Conidia are borne on a stalk called a conidiophore that can emerge either from a piece of aerial hyphae, or from a soil-embedded network of hyphae. The conidiophore is usually an asymmetrical, delicate structure with smooth, thin walls. Sizes can range from 70–150 μm in length. During development, the conidiophore can branch into three rami to produce a terverticillate structure, although biverticillate and other irregular structures are often observed. At the end of each rami, another set of branches called metulae are found. The number of metulae varies from 15–30, with their sizes ranging from 4–6 μm. At the distal end of each metula, conidium-bearing structures called phialides form. Phialides can range in shape from flask-shaped to cylindrical, and can be 10–20 μm long. The conidia produced, in turn, are smooth, with a shape that can range from spherical to cylindrical, although an oval shape is frequently seen. They are 6–15 μm long and are produced in chains, with the youngest at the base of each chain. Each conidium is haploid and bears only one nucleus. Sexual reproduction in P. digitatum has not been observed. Penicillium digitatum can also grow on a variety of laboratory media.
Sources: en.wikipedia.org
== Structure and bonds == Conjugated proteins always have a prosthetic group that is highly associated with the polypeptide chain. Association can occur either through covalent bonding or strong noncovalent interactions like hydrogen bonding, ionic bonding, or coordination bonding. Depending on whether the prosthetic group is a carbohydrate or phosphate, covalent bonds would involve the formation of either glycoside linkage between the carbohydrate and amino acids or ester linkage between the phosphate residue and the protein.
== Mode of action == For its immunotoxic properties, a low concentration of MCD peptide can cause mast cell degranulation by releasing histamine; at higher concentrations it displays anti-inflammatory activities. Through its effect on ionic channels, MCD peptide can induce long term potentiation (LTP) in CA1 region of hippocampus. It binds and inactivates voltage-dependent K+ channels, including fast-inactivating (A-type) and slow-inactivating (delayed rectifier) K+ channels. The binding site of the MCD peptide on the K+ ion channel protein complex is a multimeric protein, consisting of polypeptide chains of molecular weight between 76,000 and 80,000 and 38,000 daltons. By blocking potassium channels, the MCD peptide can increase the duration of action potentials and increase neuronal excitability.
The 1578 death of King Sebastian in battle and the subsequent 1580 death of King Henry without a named heir, precipitated a succession crisis. Philip II of Spain, whose mother was Isabella of Portugal, was one of the candidates for the throne. In 1581 he was acclaimed king of Portugal, creating a personal union between the two kingdoms. This deprived Portugal of an independent foreign policy and led to the Dutch-Portuguese War. In 1641, John, Duke of Braganza, was proclaimed king by the Cortes after an uprising led by some nobles in the year before, ending the Iberian Union under the House of Habsburg, and beginning the rule of the House of Braganza. Following the Portuguese Restoration War, Spain recognised Afonso VI as king of Portugal. During the reign of John V, the large influx of Brazilian gold into the royal treasury, chiefly through the royal fifth, produced a resource curse that weakened industry and cereal production, created a gold rush from Portugal to Brazil, and led to prolonged economic stagnation, permanent reduction of income growth, and the interruption of the institutional and economic progress achieved in the 17th century. After the depletion of gold revenues, Portugal was left with a weak industrial base and backward institutional and educational structures. This condition was exacerbated by Sebastião José de Carvalho e Melo, 1st Marquis of Pombal, who emerged as the country's de facto ruler in the aftermath of the 1755 earthquake and tsunami, one of the kingdom's worst recorded natural disaster.
Sources: en.wikipedia.org
No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.
No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.
Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.
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.