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Cardarine Identity And Mechanism — Deep Dive

By Editorial Desk · published 2025-10-06 · last reviewed 2025-11-12 · Wiki

GW501516 is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.

Last reviewed on 2025-11-12. Where a claim depends on a specific study, the study is described rather than over-claimed.

Cardarine Identity and Mechanism

At the molecular level, GW501516 binds and activates PPARδ, a nuclear receptor that regulates transcription. Activation shifts expression of genes involved in fatty acid oxidation, energy expenditure, and lipid transport in skeletal muscle and liver. Animal studies report increased endurance and altered lipid profiles after exposure. Human data are limited to small trials and do not establish long-term safety or efficacy. PPARδ also has roles in cell proliferation, so the relationship between activation and cancer risk remains an open question.

Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.

Cardarine is the common name for GW501516, a synthetic compound studied as a peroxisome proliferator-activated receptor delta agonist. Researchers developed it to explore treatments for lipid disorders and metabolic conditions. It is not an approved medicine in any country. Early clinical work examined changes in HDL cholesterol and triglycerides, but development was discontinued after animal studies raised concerns about cancer. The compound remains available as a research chemical and appears in discussions of performance enhancement.

Identity and Regulatory Status

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.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineAlso called GW501516 and endurobol.
Chemical formulaC21H18F3NO3S2Molecular weight about 453.5 g/mol.
AppearanceWhite to off-white solidForm depends on synthesis and purity.
SolubilitySoluble in DMSO and ethanolLow solubility in water.
Typical storage-20 °C, desiccated, protected from lightCommon for research chemicals.

Background from the literature

Laser microprobe mass spectrometer Particulate matter sampler Aerosol impaction Particle size analysis Hartonen, Kari; Laitinen, Totti; Riekkola, Marja-Liisa (2011). "Current instrumentation for aerosol mass spectrometry". TrAC Trends in Analytical Chemistry. 30 (9): 1486–1496. doi:10.1016/j.trac.2011.06.007. ISSN 0165-9936. Centre for Atmospheric Science TOF-AMS resources Q-AMS resources List of publications using all versions of the AMS Glossary of AMS terms

While juxtaposed against free-radical polymerization, the application of automated synthesis can be utilized for controlled radical polymerization too. These methods have been used within reversible addition-fragmentation transfer (RAFT), atom-transfer radical (ATRP), and nitroxide-mediated polymerizations, demonstrating the ability of robots to improve efficiency and reduce the hardship of performing reactions. For example, with the automatic dispensation of reagents, Symyx Technologies Inc. was able to polymerize styrene and butyl acrylate through ATRP. In addition, this functionality was supported by Zhang et al. within their research, finding that reproducibility and comparability were equivalent to classical ATRP.

The American Society for Biochemistry and Molecular Biology (ASBMB) is a learned society that was founded on December 26, 1906, at a meeting organized by John Jacob Abel (Johns Hopkins University). The roots of the society were in the American Physiological Society, which had been formed some 20 years earlier. ASBMB is the US member of the International Union of Biochemistry and Molecular Biology. The ASBMB was originally called the American Society of Biological Chemists, before obtaining its current name in 1987. The society is based in Rockville, Maryland. ASBMB's mission is to advance the science of biochemistry and molecular biology through publication of scientific and educational journals, the organization of scientific meetings, advocacy for funding of basic research and education, support of science education at all levels, and by promoting the diversity of individuals entering the scientific workforce. The organization currently has over 12,000 members.

Sources: en.wikipedia.org

Related pages on this site

Further detail

GeneReviews/NCBI/NIH/UW entry on APC-Associated Polyposis Conditions OMIM entries on APC-Associated Polyposis Conditions[link removed] Adenomatous+Polyposis+Coli+Protein at the U.S. National Library of Medicine Medical Subject Headings (MeSH) GeneCard Database concerning peer-reviewed reports on cancer critical alteration in several genes including (APC (protein)), (TP53), (Beta-catenin|β-catenin) Human APC genome location and APC gene details page in the UCSC Genome Browser.

In the US, Aducanumab is indicated for the treatment of Alzheimer's disease. In July 2021, the US Food and Drug Administration (FDA) limited the indication to people with mild cognitive impairment or mild dementia stage of disease, the population in which treatment was initiated in clinical trials. Aducanumab is a monoclonal IgG1 antibody that binds to the amyloid beta protein at amino acids 3–7, which is posited to result in slowing the progression of Alzheimer's disease. The mechanism is based on the amyloid hypothesis, which posits that amyloid proteins cause Alzheimer's disease, hence removing amyloid should slow the progression of the disease. How the antibody accesses the plaques is under active research. One mechanism suggests the plaques are exposed to the lumen of blood vessels and the antibody accesses the plaques from the lumen side. This assumes the plaque formed as a result of a leaky blood brain barrier and may also explain why there is hemorrhage after the plaques are removed. The most common serious adverse reactions reported are:

An interesting feature of these phases is that both polar and nonpolar compounds can be retained over some range of mobile phase composition (organic/aqueous). The retention mechanism of polar compounds has recently been shown to be the result of the formation of a hydroxide layer on the surface of the silica hydride.[3] Thus positively charged analytes are attracted to the negatively charged surface and other polar analytes are likely to be retained through displacement of hydroxide or other charged species on the surface. This property distinguishes it from a pure HILIC (hydrophilic interaction chromatography) columns where separation by polar differences is obtained through partitioning into a water-rich layer on the surface, or a pure RP stationary phase on which separation by nonpolar differences in solutes is obtained with very limited secondary mechanisms operating. Another important feature of the hydride-based phases is that for many analyses it is usually not necessary to use a high pH mobile phase to analyze polar compounds such as bases. The aqueous component of the mobile phase usually contains from 0.1 to 0.5% formic or acetic acid, which is compatible with detector techniques that include mass spectral analysis.

5-HTP is decarboxylated to serotonin (5-hydroxytryptamine or 5-HT) by the enzyme aromatic-L-amino-acid decarboxylase with the help of vitamin B6. This reaction occurs both in nervous tissue and in the liver. 5-HTP crosses the blood–brain barrier, while 5-HT does not. Excess 5-HTP, especially when administered with vitamin B6, is thought to be metabolized and excreted. Though 5-HTP is found in food only in insignificant quantities, it is a chemical involved intermediately in the metabolism of tryptophan, an amino acid found in all unfractionated foods, with lower total amino acid content correlating with increased tryptophan absorption.

Sources: en.wikipedia.org

Supporting material

The Society holds an annual conference in late May or early June as well as topical conferences (at Asilomar State Beach in California and Sanibel Island, Florida) and a fall workshop, which is also focused on a single topic. Conferences on Mass Spectrometry and Allied Topics have been held yearly since 1953. International Mass Spectrometry Foundation List of female mass spectrometrists ASMS website

Amino acids have been considered as components of biodegradable polymers, which have applications as environmentally friendly packaging and in medicine in drug delivery and the construction of prosthetic implants. An interesting example of such materials is polyaspartate, a water-soluble biodegradable polymer that may have applications in disposable diapers and agriculture. Due to its solubility and ability to chelate metal ions, polyaspartate is also being used as a biodegradable antiscaling agent and a corrosion inhibitor. The commercial production of amino acids usually relies on mutant bacteria that overproduce individual amino acids using glucose as a carbon source. Some amino acids are produced by enzymatic conversions of synthetic intermediates. 2-Aminothiazoline-4-carboxylic acid is an intermediate in one industrial synthesis of L-cysteine for example. Aspartic acid is produced by the addition of ammonia to fumarate using a lyase.

Aspartate has many other biochemical roles. It is a metabolite in the urea cycle and participates in gluconeogenesis. It carries reducing equivalents in the malate-aspartate shuttle, which utilizes the ready interconversion of aspartate and oxaloacetate, which is the oxidized (dehydrogenated) derivative of malic acid. Aspartate donates one nitrogen atom in the biosynthesis of inosine, the precursor to the purine bases. In addition, aspartic acid acts as a hydrogen acceptor in a chain of ATP synthase. Dietary L-aspartic acid has been shown to act as an inhibitor of Beta-glucuronidase, which serves to regulate enterohepatic circulation of bilirubin and bile acids. Click on genes, proteins and metabolites below to link to respective articles. Aspartate (the conjugate base of aspartic acid) stimulates NMDA receptors, though not as strongly as the amino acid neurotransmitter L-glutamate does. Aspartate is the "A" in NMDA (N-methyl-D-aspartate receptor).

Nanoghosts are nanosized vesicles containing a chosen drug delivery payload manufactured from extracted leukocyte membranes with the cell cytoplasm content removed. The use of biological membranes serves to mask the particles from the immune system to reduce the likelihood of an immunogenic response, as well as to extend circulation of the particles in the blood. They are produced by homogenizing the cells to remove the cytosol, and then sonicating the empty cell membranes to create nanoghosts between 100 and 200 nm in diameter. Membranes used to make nanoghosts harvested form red blood cells have been shown to circulate for about 120 days and avoid phagocytotic cells. Neutrophil based nanoghosts retain the chemotaxis capacity of neutrophils to sites of inflammation, which encourages tumor targeting. NK based nanoghosts exhibit metastatic cancer targeting behavior. Monocyte based nanoghosts are effective at infiltrating the tumor microenvironment. Mesenchymal stem cell derived nanoghosts exhibit cancer targeting properties.

Biodiversity informatics deals with the collection and analysis of biodiversity data, such as taxonomic databases, or microbiome data. Examples of such analyses include phylogenetics, niche modelling, species richness mapping, DNA barcoding, or species identification tools. A growing area is also macro-ecology, i.e. the study of how biodiversity is connected to ecology and human impact, such as climate change. The enormous number of published literature makes it virtually impossible for individuals to read every paper, resulting in disjointed sub-fields of research. Literature analysis aims to employ computational and statistical linguistics to mine this growing library of text resources. For example: Abbreviation recognition – identify the long-form and abbreviation of biological terms Named-entity recognition – recognizing biological terms such as gene names Protein–protein interaction – identify which proteins interact with which proteins from text The area of research draws from statistics and computational linguistics.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is a common name for the investigational compound GW501516. It acts as a PPARδ agonist and is not approved for human use. It is prohibited in sport.

How does cardarine work?

It activates PPARδ, a nuclear receptor that influences gene expression related to lipid and energy metabolism. Animal studies show changes in endurance and lipid levels. Human effects and risks are not well established.

Is cardarine a steroid?

No, cardarine is not a steroid. It belongs to a different chemical class, the PPARδ agonists. It is also not a selective androgen receptor modulator.

Is cardarine a SARM?

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.

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