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Cardarine Identity And Mechanism — What the Evidence Shows

By Editorial Desk · published 2025-11-21 · last reviewed 2025-12-21 · Guide

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

Updated 2025-12-21. Numbers and descriptions here follow the published literature rather than marketing material.

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.

Identity and Regulatory Status

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 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.

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.

Supporting material

==== Natural "trans fats" in dairy products ==== Some trans fatty acids occur in natural fats and traditionally processed foods. Vaccenic acid occurs in breast milk, and some isomers of conjugated linoleic acid (CLA) are found in meat and dairy products from ruminants. Butter, for example, contains about 3% trans fat.

Protein occurs in a wide range of food. On a worldwide basis, plant protein foods contribute over 60% of the per capita supply of protein. In North America, animal-derived foods contribute about 70% of protein sources. Insects are a source of protein in many parts of the world. In parts of Africa, up to 50% of dietary protein derives from insects. It is estimated that more than 2 billion people eat insects daily. Protein powders—such as casein, whey, egg, rice, soy and cricket flour—are processed and manufactured sources of protein. People eating a balanced diet do not need protein supplements. The table below presents food groups as protein sources.

The Gulf War began with an extensive aerial bombing campaign on 16 January 1991. For 42 consecutive days and nights, the coalition forces subjected Iraq to one of the most intensive air bombardments in military history. The coalition flew over 100,000 sorties, dropping 88,500 tonnes of bombs, which widely destroyed military and civilian infrastructure. Iraqi anti-aircraft defenses, including man-portable air-defense systems, were surprisingly ineffective against enemy aircraft, and the coalition suffered only 75 aircraft losses in over 100,000 sorties, 44 due to Iraqi action. Two of these losses are the result of aircraft colliding with the ground while evading Iraqi ground-fired weapons. One of these losses is a confirmed air-air victory.

=== Origins and Controversy === The original work seen on eSimoa was done by David R. Walt's team at Harvard University, who published their work in 2020. However, the claim to the development of the technology is contested by Chi-An Cheng at National Taiwan University (NTU) in 2023 and 2024, who has claimed that her team developed the technology.

Precondition for repetitious manufacturing of porous glass is the knowledge about structure determining and structure controlling parameters. The composition of the initial glass is a structure controlling parameter. The manufacturing of the initial glass, mainly the cooling process, the temperature and time of thermal treatment, and the after treatment are structure determining parameters. The phase diagram for sodiumborosilica glass shows a miscibility gap for certain glass compositions. The upper critical temperature lies at about 760 °C and the lower one at about 500 °C. O.S. Moltschanova was the first person who exactly described the definition of the exsolution. For a phase separation the initial glass composition must lie in the miscibility gap of the ternary Na2O-B2O3-SiO2 glass system. By a thermal treatment, an interpenetration structure is generated, which results from a spinodal decomposition of the sodium-rich borate phase and the silica phase. This procedure is called primary decomposition. Using an initial glass composition, which lies on the line of anomaly, it is possible to attain a maximum decomposition, which is almost strainless. As both phases have a different resistances to water, mineral acids, and inorganic salt solutions, the sodium-rich borate phase in these mediums can be removed by extraction. Optimal extraction is possible only if the initial glass composition and thermal treatment are chosen such that combine structures form, and not droplet structures.

Sources: en.wikipedia.org

Related pages on this site

Notes from published material

2 December The Gold Brush - Paint's Green Revolution, narrated by Gavin Weightman, produced by Michael Wills, directed by Jill Freeman, made by Juniper Productions 9 December Towards a Cure for Cancer, about the possibilities of hexamethylene bisacetamide (HMBA); Paul Marks and Richard Rifkind of the Memorial Sloan Kettering Cancer Center; chemist Ronald Breslow of Columbia University and HMBA; Charlotte Friend made a discovery in 1970, staining a cell with dimethyl sulfoxide (DMSO), where it made cancer cells make hemoglobin; Lorraine Baltzer, a research nurse; tretinoin was found to work in 1988, and first prescribed in September 1990; Bruce Chabner of the National Cancer Institute; differentiation therapy and Protein kinase C (PKC), signal transduction and biochemical cascades; tests on HL60 did not work; another compound was suberic bishydroxamic acid (SBHA). Narrated by Derek Cooper, directed by Karl Sabbath, made by InCA with WTTW 16 December School's Out, about developments in educational technology and the history of educational psychology, with cognitive psychologist Kristina Hooper Woolsey, educationalist Stephen Heppell, computer scientist Alan Kay, works such as the Beethoven's Ninth Symphony CD-ROM by Professor of Music at UCLA, Robert Winter; the Italian educator Maria Montessori; the Swiss child psychologist Jean Piaget; educational psychologist Jerome Bruner; computer scientist Seymour Papert.

=== Selected articles === Ajayaghosh, Ayyappanpillai, Subi J. George (2001). “First phenylenevinylene based organogels: self-assembled nanostructures via cooperative hydrogen bonding and π-stacking”. J. Am. Chem. Soc. 2001, 123, 21, 5148-5149. https://doi.org/10.1021/ja005933+. Ajayaghosh, Ayyappanpillai, Priya Carol, and Sivaramapanicker Sreejith (2005) “A Ratiometric Fluorescence Probe for Selective Visual Sensing of Zn2+”. J. Am. Chem. Soc. 2005, 127, 43, 14962-14963. https://doi.org/10.1021/ja054149s. Ajayaghosh, Ayyappanpillai, Vakayil K. Praveen, Chakkooth Vijayakumar, Subi J. George (2007). “Molecular Wire Encapsulated into π Organogels: Efficient Supramolecular Light-Harvesting Antennae with Color-Tunable Emission”. Angew. Chem. Int. Ed. 2007, 46, 6260-6265. https://doi.org/10.1002/anie.200701925. Ajayaghosh, Ayyappanpillai, Vakayil K. Praveen (2008). “π-Organogels of Self-Assembled p-Phenylenevinylenes: Soft Materials with Distinct Size, Shape, and Functions”. Acc. Chem. Res. 2007, 40, 8, 644-656. https://doi.org/10.1021/ar7000364 Vijayakumar, Chakkooth; Praveen, Vakayil K.; Kartha, Kalathil K.; Ajayaghosh, Ayyappanpillai (2011). "Excitation energy migration in oligo(p-phenylenevinylene) based organogels: structure-property relationship and FRET efficiency". Physical Chemistry Chemical Physics. 13 (11): 4942–4949. Bibcode:2011PCCP...13.4942V. doi:10.1039/C0CP02110E. PMID 21321716. S2CID 19328938. Kartha, Kalathil K.; Babu, Sukumaran S.; Srinivasan, Sampath; Ajayaghosh, Ayyappanpillai (2012).

Clomipramine may interact with monoamine oxidase inhibitors (MAOIs) such as isocarboxazid, moclobemide, phenelzine, selegiline, and tranylcypromine. These combinations are generally avoided due to the severe risk of adverse reactions. The medication also interacts with antiarrhythmic agents because tricyclic antidepressants (TCAs) can significantly alter cardiac conduction. A specific pharmacokinetic interaction exists with quinidine; since clomipramine is metabolized by the enzyme CYP2D6 in vivo, quinidine can impede this process and raise drug levels. Similarly, diuretics pose a secondary risk; by potentially inducing hypokalaemia (low blood potassium), they increase the likelihood of QT interval prolongation and the life-threatening heart rhythm known as torsades de pointes. Furthermore, clomipramine reacts with selective serotonin reuptake inhibitors (SSRIs) through two distinct mechanisms. First, there is a risk of additive serotonergic effects that can lead to serotonin syndrome. Second, a pharmacokinetic interaction occurs with SSRIs that inhibit CYP2D6—specifically fluoxetine and paroxetine—which can lead to toxic levels of clomipramine in the bloodstream. This risk of serotonin toxicity or serotonin syndrome extends to other serotonergic agents, including triptans, other tricyclic antidepressants, and tramadol. Fluvoxamine increases the serotonergic effects of clomipramine and, likewise, clomipramine increases fluvoxamine levels.

=== DEA classification === Vicoprofen was initially scheduled as a schedule III drug, but was later reclassified to a schedule II drug based on the DEA reclassification of products containing hydrocodone, effective October 2014.

=== Weight loss industry === There is a substantial market for products which claim to make weight loss easier, quicker, cheaper, more reliable, or less painful. These include books, DVDs, CDs, cremes, lotions, pills, rings and earrings, body wraps, body belts and other materials, fitness centers, clinics, personal coaches, weight loss groups, and food products and supplements. Dietary supplements, though widely used, are not considered a healthy option for weight loss, and have no clinical evidence of efficacy. Herbal products have not been shown to be effective. In 2008, between US$33 billion and $55 billion was spent annually in the US on weight-loss products and services, including medical procedures and pharmaceuticals, with weight-loss centers taking between 6 and 12 percent of total annual expenditure. Over $1.6 billion per year was spent on weight-loss supplements. About 70 percent of Americans' dieting attempts are of a self-help nature. In Western Europe, sales of weight-loss products, excluding prescription medications, topped €1,25 billion (£900 million/$1.4 billion) in 2009. The scientific soundness of commercial diets by commercial weight management organizations varies widely, being previously non-evidence-based, so there is only limited evidence supporting their use, because of high attrition rates. Commercial diets result in modest weight loss in the long term, with similar results regardless of the brand, and similarly to non-commercial diets and standard care.

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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