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Identity And Pharmacological Classification — Field Notes

By Editorial Desk · published 2025-10-19 · last reviewed 2025-11-23 · Guide

If you have been reading about GW501516 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 2025-11-23. Numbers and descriptions here follow the published literature rather than marketing material.

Identity and Pharmacological Classification

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.

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.

Detection and Regulatory Landscape

Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.

A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.

Cardarine at a glance

PropertyValueNotes
Chemical classPPARδ agonistNot an anabolic steroid.
Common synonymsGW501516, GW-1516Cardarine is an informal name.
AppearanceWhite to off-white powderTypical for research-grade solid.
Solubility classPoorly soluble in water; soluble in some organic solventsSuch as DMSO or ethanol in laboratory settings.
Typical storage temperatureCool, dry, protected from lightSpecific conditions vary by supplier and form.

Mechanism and Detection Methods

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.

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.

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Regulatory Status and Detection Context

A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.

Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.

Regulation and Analytical Detection

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.

Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.

Reference notes

Individual transmembrane adenylyl cyclase isoforms have been linked to numerous physiological functions. Soluble adenylyl cyclase (sAC, AC10) has a critical role in sperm motility. Adenylyl cyclase has been implicated in memory formation, functioning as a coincidence detector. AC-IV was first reported in the bacterium Aeromonas hydrophila, and the structure of the AC-IV from Yersinia pestis has been reported. These are the smallest of the AC enzyme classes; the AC-IV (CyaB) from Yersinia is a dimer of 19 kDa subunits with no known regulatory components (PDB: 2FJT​). AC-IV forms a superfamily with mammalian thiamine-triphosphatase called CYTH (CyaB, thiamine triphosphatase). These forms of AC have been reported in specific bacteria (Prevotella ruminicola O68902 and Rhizobium etli Q8KY20, respectively) and have not been extensively characterized. There are a few extra members (~400 in Pfam) known to be in class VI. Class VI enzymes possess a catalytic core similar to the one in Class III.

The difference between enzymatically active and inactive homologues has been noted (and in some cases, understood when comparing catalytically active and inactive proteins residing in recognisable families) for some time at the sequence level, owing to the absence of key catalytic residues. Some pseudoenzymes have also been referred to as 'prozymes' when they were analysed in protozoan parasites. The best studied pseudoenzymes reside amongst various key signalling superfamilies of enzymes, such as the proteases, the protein kinases, protein phosphatases and ubiquitin modifying enzymes. The role of pseudoenzymes as "pseudo scaffolds" has also been recognised and pseudoenzymes are now beginning to be more thoroughly studied in terms of their biology and function, in large part because they are also interesting potential targets (or anti-targets) for drug design in the context of intracellular cellular signalling complexes. Kinase Pseudokinase Phosphatome Protein phosphatase "Patrick Eyers - University of Liverpool". Liverpool.ac.uk. Retrieved 2017-01-16.

That evidence bolstered the hypothesis that heavier elements are the product of nucleosynthesis in stars. More recently, such observations provided evidence that elements are formed by neutron capture in the s-process. Since that discovery, there have been many searches in terrestrial materials for natural sources of technetium. In 1962, technetium-99 was isolated and identified in pitchblende from the Belgian Congo in very small quantities (about 0.2 ng/kg), where it originates as a spontaneous fission product of uranium-238. The natural nuclear fission reactor in Oklo contains evidence that significant amounts of technetium-99 were produced and have since decayed into ruthenium-99.

Repaglinide is an antidiabetic drug in the class of medications known as meglitinides, and was invented in 1983. Repaglinide is a medication used in addition to diet and exercise for blood sugar control in type 2 diabetes. The mechanism of action of repaglinide involves promoting insulin release from β-islet cells of the pancreas; like other antidiabetic drugs, a main side effect concern is hypoglycemia. It is sold by Novo Nordisk under the name of Prandin in the United States, Gluconorm in Canada, Surepost in Japan, Repaglinide in Egypt, and Novonorm elsewhere. In Japan it is produced by Dainippon Sumitomo Pharma.

Sources: en.wikipedia.org

Reference notes

=== Stage === The phrase "On the Bowery", which has since fallen into disuse, was a generic way to say one was down-and-out. It originated in the song "The Bowery" from the 1891 musical A Trip to Chinatown, which includes the chorus "The Bow'ry, The Bow'ry!/They say such things,/and they do strange things/on the Bow'ry, the Bow’ry!/I’ll never go there anymore.”". On the Bowery, an 1894 play starring Steve Brodie, supposed Brooklyn Bridge jumper and Bowery saloonkeeper. In Disney's Newsies, the showgirls featured in the song "I Never Planned on You/Don't Come a-Knocking" are called the Bowery Beauties.

Stress and physical inactivity and alcohol reduce hepatalin secretion. In pregnancy, the role of hepatalin changes throughout the period of gestation. Hepatalin action predominates in the first trimester of gestation when uterine and fetal protein metabolism is required. Insulin action predominates in the third trimester when maternal and fetal fat stores are needed. Alcohol consumption during pregnancy results in dose-related suppression of hepatalin secretion in the adult offspring. Hepatalin can be acutely turned off and on by manipulation of the mechanisms (i.e., the three necessary signals) regulating hepatalin secretion.

=== Enzyme activity === Enzyme activity is a measure of the quantity of active enzyme present and is thus dependent on various physical conditions, which should be specified. It is calculated using the following formula:

=== Medical guidelines and recommendations === In 2015, the scientific advisory panel of U.S. Department of Health and Human Services and U.S. Department of Agriculture for the 2015 iteration of the Dietary Guidelines for Americans dropped the previously recommended limit of consumption of dietary cholesterol to 300 mg per day with a new recommendation to "eat as little dietary cholesterol as possible", thereby acknowledging an association between a diet low in cholesterol and reduced risk of cardiovascular disease. A 2013 report by the American Heart Association and the American College of Cardiology recommended focusing on healthy dietary patterns rather than specific cholesterol limits, as they are hard for clinicians and consumers to implement. They recommend the DASH and Mediterranean diet, both of which are low in cholesterol. A 2017 review by the American Heart Association recommends switching saturated fats for polyunsaturated fats to reduce cardiovascular disease risk. Some supplemental guidelines have recommended doses of phytosterols in the order of 1.6‍–‍3.0 grams per day (Health Canada, EFSA, ATP III, FDA). A meta-analysis demonstrated a 12% reduction in LDL-cholesterol at a mean dose of 2.1 grams per day. The benefits of a diet supplemented with phytosterols have also been questioned.

An essential amino acid is an amino acid that is required by an organism but cannot be synthesized de novo by it, and therefore must be supplied in its diet. Out of the twenty standard protein-producing amino acids, nine cannot be endogenously synthesized by humans: phenylalanine, valine, threonine, tryptophan, methionine, leucine, isoleucine, lysine, and histidine.

Sources: en.wikipedia.org

Reference notes

Most serotonergic psychedelics act as non-selective agonists of serotonin receptors, including of the serotonin 5-HT2 receptors, but often also of other serotonin receptors, such as the serotonin 5-HT1 receptors. They are thought to mediate their hallucinogenic effects specifically by activation of serotonin 5-HT2A receptors. Psychedelics (including tryptamines like psilocin, DMT, and 5-MeO-DMT; phenethylamines like mescaline, DOM, and 2C-B; and ergolines and lysergamides like LSD) all act as agonists of the serotonin 5-HT2A receptors. Some psychedelics, such as phenethylamines like DOM and 2C-B, show high selectivity for the serotonin 5-HT2 receptors over other serotonin receptors. There is a very strong correlation between 5-HT2A receptor affinity and human hallucinogenic potency. In addition, the intensity of hallucinogenic effects in humans is directly correlated with the level of serotonin 5-HT2A receptor occupancy as measured with positron emission tomography (PET) imaging. Serotonin 5-HT2A receptor blockade with drugs like the semi-selective ketanserin and the non-selective risperidone can abolish the hallucinogenic effects of psychedelics in humans. However, studies with more selective serotonin 5-HT2A receptor antagonists, like pimavanserin, are still needed.

A DALY (Disability-Adjusted Life Year) is a measure that reflects the total burden of disease. It combines years of life lost (due to premature death) and years lived with disability (adjusted for the severity of the disability). The lower the DALY rates, the lower the burden of endocrine disorders in a country. The map shows that large parts of Asia have lower DALY rates (pale yellow), suggesting that endocrine disorders have a relatively low impact on overall health, whereas some countries in South America and Africa (specifically Suriname and Somalia) have higher DALY rates (dark orange to red), indicating a higher disease burden from endocrine disorders.

He then divested the trade he controlled, as it would be more efficient and less likely to be brought down in one law enforcement swoop. He sent his lawyer to convene the nation's top drug traffickers at a house in Acapulco where he designated plazas or territories. The Tijuana route would go to his nephews, the Arellano Felix brothers. The Ciudad Juárez route would go to the Carrillo Fuentes family. Miguel Caro Quintero would run the Sonora corridor. Meanwhile, Joaquín Guzmán Loera and Ismael Zambada García would take over Pacific coast operations, becoming the Sinaloa Cartel. Guzmán and Zambada brought veteran Héctor Luis Palma Salazar back into the fold. The control of the Matamoros, Tamaulipas corridor—then becoming the Gulf Cartel—would be left undisturbed to its founder, Juan García Ábrego, who was not a party to the 1989 pact. Félix Gallardo still planned to oversee national operations, as he maintained important connections, but he would no longer control all details of the business. When he was transferred to a high-security prison in 1993, he lost any remaining control over the other cartel leaders.

guanylyl cyclase-A (GC-A) also known as natriuretic peptide receptor-A (NPRA/ANPA) or NPR1 guanylyl cyclase-B (GC-B) also known as natriuretic peptide receptor-B (NPRB/ANPB) or NPR2 natriuretic peptide clearance receptor (NPRC/ANPC) or NPR3 NPR-A and NPR-B have a single membrane-spanning segment with an extracellular domain that binds the ligand. The intracellular domain maintains two consensus catalytic domains for guanylyl cyclase activity. Binding of a natriuretic peptide induces a conformational change in the receptor that causes receptor dimerization and activation. The binding of ANP to its receptor causes the conversion of GTP to cGMP and raises intracellular cGMP. As a consequence, cGMP activates a cGMP-dependent kinase (PKG or cGK) that phosphorylates proteins at specific serine and threonine residues. In the medullary collecting duct, the cGMP generated in response to ANP may act not only through PKG but also via direct modulation of ion channels. NPR-C functions mainly as a clearance receptor by binding and sequestering ANP from the circulation. All natriuretic peptides are bound by the NPR-C.

Although one-letter symbols are included in the table, IUPAC–IUBMB recommend that "Use of the one-letter symbols should be restricted to the comparison of long sequences". The one-letter notation was chosen by IUPAC-IUB based on the following rules:

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine also known as?

Cardarine is commonly known as GW501516 or GW-1516. These names refer to the same synthetic compound. It is not a brand-name approved medicine.

Is cardarine a steroid?

No, cardarine is not a steroid. It is classified as a PPARδ agonist. Its structure and receptor target differ from anabolic steroids.

Has cardarine been approved for human use?

No regulatory agency has approved cardarine as a medicine. It was investigated in early research but development was discontinued. It is not available as a prescription drug.

Is cardarine banned in sports?

Yes, WADA prohibits cardarine as a PPARδ agonist. It appears on the prohibited list and can be detected in urine or blood. Athletes using it risk sanctions.

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