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Cardarine As Investigational Pparδ Agonist — Reference Sheet

By Editorial Desk · published 2026-03-21 · last reviewed 2026-05-12 · Wiki

Everything below concerns LC-MS/MS. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Updated 2026-05-12. Numbers and descriptions here follow the published literature rather than marketing material.

Cardarine as Investigational PPARδ Agonist

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.

Mechanism and Detection

Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.

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.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516, GW-501516, GW 501516, endurobolNames vary in research and anti-doping documents.
Chemical classSynthetic PPARδ agonistSmall-molecule nuclear receptor ligand.
CAS Registry Number317318-70-0Identifier commonly associated with GW501516.
AppearanceWhite to off-white powderTypical for purified research material.
SolubilityLow in water; soluble in DMSO and ethanolOrganic solvents are common for laboratory stock solutions.

Regulation and Detection

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.

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.

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Background and Regulatory Status

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.

Identity and Pharmacological Classification

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.

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.

Mechanism and Detection 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.

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.

Background from the literature

The atomic radii of the alkali metals increase going down the group. Because of the shielding effect, when an atom has more than one electron shell, each electron feels electric repulsion from the other electrons as well as electric attraction from the nucleus. In the alkali metals, the outermost electron only feels a net charge of +1, as some of the nuclear charge (which is equal to the atomic number) is cancelled by the inner electrons; the number of inner electrons of an alkali metal is always one less than the nuclear charge. Therefore, the only factor which affects the atomic radius of the alkali metals is the number of electron shells. Since this number increases down the group, the atomic radius must also increase down the group. The ionic radii of the alkali metals are much smaller than their atomic radii. This is because the outermost electron of the alkali metals is in a different electron shell than the inner electrons, and thus when it is removed the resulting atom has one fewer electron shell and is smaller. Additionally, the effective nuclear charge has increased, and thus the electrons are attracted more strongly towards the nucleus and the ionic radius decreases.

Absinthe's popularity grew steadily through the 1840s, when it was given to French troops in Algeria as a malaria preventive, and the troops brought home their taste for it. Absinthe became so popular in bars, bistros, cafés, and cabarets by the 1860s that the hour of 5 pm was called l'heure verte 'the green hour'. It was favoured by all social classes, from the wealthy bourgeoisie to poor artists and ordinary working-class people. By the 1880s, mass production had caused the price to drop sharply, and the French were drinking 36 million litres (9,500,000 US gal) per year by 1910. Absinthe was exported widely from France and Switzerland and attained some degree of popularity in other countries, including Spain, the United Kingdom, the United States, and the Czech Republic. It was never banned in Spain or Portugal, and its production and consumption have never ceased. It gained a temporary popularity spike during the early 20th century, corresponding with the Art Nouveau and Modernism aesthetic movements. New Orleans has a cultural association with absinthe and is credited as the birthplace of the Sazerac, perhaps the earliest absinthe cocktail. The Old Absinthe House bar on Bourbon Street began selling absinthe in the first half of the 19th century. Its Catalan lease-holder, Cayetano Ferrer, named it the Absinthe Room in 1874 due to the drink's popularity, which was served in the Parisian style. It was frequented by Mark Twain, Oscar Wilde, Franklin Delano Roosevelt, Aleister Crowley, and Frank Sinatra.

==== In males ==== It is secreted from the Sertoli cells, located in the seminiferous tubules inside the testes. Androgens stimulate inhibin production; this protein may also help to locally regulate spermatogenesis.

The militias emerged in the mid-late 1990s, being composed mainly of off-duty police officers and ex-military, in many cases also receiving assistance from local businessmen and residents looking for protection from criminal groups. The Comando Vermelho, as a response, began carrying out terrorist attacks against civilian targets between 27 and 31 December 2006, during these attacks, 19 people died, being 10 civilians, 2 policemen and 7 gang members. As retaliation, the militias conducted several raids against the Comando Vermelho, killing more than 100 gang members. These groups launched several attacks between January 2007 and March 2008 against Comando Vermelho, conquering the Cidade Alta favela on 4 February, three days later it was recaptured by the Comando Vermelho commanded by Gilberto Martins da Silva (known as "Mineiro da Cidade Alta"), with at least 20 gang members being killed in subsequent clashes. The militias obtained a "Caveirão" (an armored vehicle used by the Battalion of Special Police Operations (BOPE) for high-risk operations) in January of the same year. According to some investigations, the militias mainly finance their armed struggle with illegal activities, such as extortion, kidnapping, loan sharking, racketeering, gambling, pimping, contract killing and arms trafficking. In May 2008, the militias, commanded by Coronel Jairo, kidnapped and tortured a group of journalists from the Brazilian newspaper O Dia who were reporting the criminal activities perpetrated by the militiamen. After 7 hours of torture, they were released.

Sources: en.wikipedia.org

Further detail

== Management == D. dadantii is a member within the genus that is able to produce the pigment indigoidine. Rapid identification of this species utilizes this water-insoluble blue pigment appearing in the bacterial colonies as a chemotaxonomic trait. The presence of a soft rot may be an indication of a bacterial disease. However, many other organisms and plant disorders may appear as various soft rot or black lesions. Proper identification is important for treatment and control measures. Thus a differential media is used to culture Dickeya species and isolate or identify D. dadantii. Researchers at Fu Jen Catholic University in Taiwan developed a medium that differentiates D. dadantii from other species. This NGM medium contains nutrient agar (NA) and glycerol medium supplemented with MnCl2 :4H2O. To make this media, mix 23 g of nutrient agar, 10 ml glycerol (1% v/v), and 0.4 g MnCl2:4H2O (2 mM) to 1.0 liter of water. Note the pH of this media is 6.5 and it has a light brown base color. The proper temperature for culturing D. dadantii is 28 degrees Celsius. A positive result occurs when a bacterial streak produces a brownish blue color on the agar plate. Further isolation and extraction of the indigoidine pigment is possible using the methods described by Chatterejee and Brown. Currently there are no effective chemical controls for D. dadantii. The most important practices involve lowering the prevalence of disease by proper sanitation of materials, exclusion of infected materials, and avoiding environments conducive to disease.

The expression of genes is influenced by how the DNA is packaged in chromosomes, in a structure called chromatin. Base modifications can be involved in packaging, with regions that have low or no gene expression usually containing high levels of methylation of cytosine bases. DNA packaging and its influence on gene expression can also occur by covalent modifications of the histone protein core around which DNA is wrapped in the chromatin structure or else by remodeling carried out by chromatin remodeling complexes (see Chromatin remodeling). There is, further, crosstalk between DNA methylation and histone modification, so they can coordinately affect chromatin and gene expression. For one example, cytosine methylation produces 5-methylcytosine, which is important for X-inactivation of chromosomes. The average level of methylation varies between organisms—the worm Caenorhabditis elegans lacks cytosine methylation, while vertebrates have higher levels, with up to 1% of their DNA containing 5-methylcytosine. Despite the importance of 5-methylcytosine, it can deaminate to leave a thymine base, so methylated cytosines are particularly prone to mutations. Other base modifications include adenine methylation in bacteria, the presence of 5-hydroxymethylcytosine in the brain, and the glycosylation of uracil to produce the "J-base" in kinetoplastids.

=== Industrial === Industrial biotechnology (known mainly in Europe as white biotechnology) is the application of biotechnology for industrial purposes, including industrial fermentation. It includes the practice of using cells such as microorganisms, or components of cells like enzymes, to generate industrially useful products in sectors such as chemicals, food and feed, detergents, paper and pulp, textiles and biofuels. In the current decades, significant progress has been done in creating genetically modified organisms (GMOs) that enhance the diversity of applications and economical viability of industrial biotechnology. By using renewable raw materials to produce a variety of chemicals and fuels, industrial biotechnology is actively advancing towards lowering greenhouse gas emissions and moving away from a petrochemical-based economy. Synthetic biology is considered one of the essential cornerstones in industrial biotechnology due to its financial and sustainable contribution to the manufacturing sector. Jointly biotechnology and synthetic biology play a crucial role in generating cost-effective products with nature-friendly features by using bio-based production instead of fossil-based. Synthetic biology can be used to engineer model microorganisms, such as Escherichia coli, by genome editing tools to enhance their ability to produce bio-based products, such as bioproduction of medicines and biofuels. For instance, E.

Gorgonzola blue cheese takes its name from the village of Gorgonzola in Italy where it was first made. Belonging to the family of Stracchino cheeses, Gorgonzola is a whole milk, white, and "uncooked" cheese. This blue cheese is inoculated with Penicillium glaucum which, during ripening, produces the characteristic of blue-green veins. There are two variants with different odor: natural and creamy Gorgonzola. 63 components in natural Gorgonzola cheese and 52 components in creamy Gorgonzola cheese contribute to odor with 2-nonanone, 1-octen-3-ol, 2-heptanol, ethyl hexanoate, methylanisole and 2-heptanone being the prominent compounds for odor in both cheeses.

While there is a lack of geochemical observations to constrain the exact composition of the prebiotic atmosphere, recent models point to an early "weakly reducing" atmosphere; that is, early Earth's atmosphere was likely dominated by CO2 and N2 and not CH4 and NH3 as used in the original Miller–Urey experiment. This is explained, in part, by the chemical composition of volcanic outgassing. Geologist William Rubey was one of the first to compile data on gases emitted from modern volcanoes and concluded that they are rich in CO2, H2O, and likely N2, with varying amounts of H2, sulfur dioxide (SO2), and H2S. Therefore, if the redox state of Earth's mantle — which dictates the composition of outgassing – has been constant since formation, then the atmosphere of early Earth was likely weakly reducing, but there are some arguments for a more-reducing atmosphere for the first few hundred million years. While the prebiotic atmosphere could have had a different redox condition than that of the Miller–Urey atmosphere, the modified Miller–Urey experiments described in the above section demonstrated that amino acids can still be abiotically produced in less-reducing atmospheres under specific geochemical conditions.

Sources: en.wikipedia.org

Supporting material

Although the manufacturer of Cytomel states half-life to be 2.5 days the half-life variability is great and can vary depending on the thyroid status of the patient. Newer studies have found the pharmacokinetics of T3 to be complex and the half-life to vary between 10 – 22 hours.

== Uses == Niosomes are used as biodegradable and non-immunogenic drug delivery compounds, as they have a low toxicity risk in biological systems. They can also be used to entrap hydrophilic pharmaceuticals within aqueous compartments or lipophilic drugs into vesicular bilayer membranes. Niosomes shield drug molecules from the biological environment, which can be utilized to improve the therapeutic performance of various drug molecules. Additionally, they can be used in a sustained drug delivery system to more directly affect target cells and delay clearance from circulation. Niosomes are used in a variety of applications, including gene delivery, drug targeting, antineoplastic treatment, delivery of peptide drugs, carriers for hemoglobin, transdermal drug delivery systems, and cosmetics. They are also being studied for their potential use as a treatment for different forms of leishmaniasis In one 2022 in vitro study, tamoxifen-loaded niosomes exhibited pH-dependent release and induced apoptosis and cell-cycle arrest in two breast cancer cell lines .

In addition to polycondensation, automated synthesis has been applied to the various methods of radical polymerization, such as ring-opening and polyolefins. This includes free-radical polymerization, such as the development of an automated process to synthesize and evaluate molecularly imprinted polymers (MIPs). Through thermal initiation, around sixty polymers could be prepared in parallel and evaluated through their binding constants to the imprinted analytes. Furthermore, adding another approach to the repertoire, Long et al. demonstrated the abilities of robotic systems and their use with varying the monomer for the synthesis of poly(styrene-co-methyl methacrylate) and poly(styrene-co-butyl methacrylate). After automatically precipitating, the products were characterized with standard analytics and added to the polymer library. Another example includes the method described by Symyx Technologies Inc. with the application of an ink-jet printer, delivering different ratios of styrene and acrylonitrile, which was used as the terminator. While these are examples of suspension polymerization, the first instance of automated synthesis for parallel emulsion was reported by Voorn et al. with five parallel reactors containing well-defined systems of styrene and vinyl acetate. After optimizing the vortex speed, the results between the methods of automated synthesis and classical stirring for emulsion polymerization were compared, which found that the products were comparable.

The first fast reactor built and operated was the Los Alamos Plutonium Fast Reactor ("Clementine") in Los Alamos, NM. Clementine was fueled by Ga-stabilized delta-phase Pu and cooled with mercury. It contained a 'window' of Th-232 in anticipation of breeding experiments, but no reports were made available regarding this feature. Another proposed fast reactor is a fast molten salt reactor, in which the molten salt's moderating properties are insignificant. This is typically achieved by replacing the light metal fluorides (e.g. LiF, BeF2) in the salt carrier with heavier metal chlorides (e.g., KCl, RbCl, ZrCl4). Several prototype FBRs have been built, ranging in electrical output from a few light bulbs' equivalent (EBR-I, 1951) to over 1,000 MWe. As of 2006, the technology is not economically competitive to thermal reactor technology, but India, Japan, China, South Korea, and Russia are all committing substantial research funds to further development of fast breeder reactors, anticipating that rising uranium prices will change this in the long term. Germany, in contrast, abandoned the technology due to safety concerns. The SNR-300 fast breeder reactor was completed in 1985 but did not obtain authorization to start up. The project was cancelled in March 1991.

In cases of tumor-related hyperprolactinemia, prolactinoma is the most common culprit of consistently high levels of prolactin as well as the most common type of pituitary tumor. For non-tumor related hyperprolactinemia, the most common cause is medication-induced prolactin secretion. Particularly, antipsychotics have been linked to a majority of non-tumor related hyperprolactinemia cases due to their prolactin-rising and prolactin-sparing mechanisms. Typical antipsychotics have been shown to induce significant, dose-dependent increases in prolactin levels up to 10-fold the normal limit. Atypical antipsychotics vary in their ability to elevate prolactin levels; however, medications in this class, such as risperidone and paliperidone, carry the highest potential to induce hyperprolactinemia in a dose-dependent manner similar to typical antipsychotics.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

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.

Is cardarine a steroid?

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.

Why was cardarine not developed further?

Early rodent studies reported tumor formation at multiple sites, which raised safety concerns. Sponsors stopped clinical development, and no approved human product exists.

How does cardarine work in the body?

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.

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