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Background And Research Context — Complete Guide

By Editorial Desk · published 2026-02-02 · last reviewed 2026-03-10 · News

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.

Updated 2026-03-10. Numbers and descriptions here follow the published literature rather than marketing material.

Background and Research Context

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.

Identity and Regulatory Status

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 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
CAS Registry Number317318-70-0Unique identifier for the compound.
Chemical classPPARδ agonistSynthetic ligand for peroxisome proliferator-activated receptor delta.
AppearanceWhite to off-white solidTypical form of research-grade material.
SolubilitySoluble in DMSO and ethanolPoorly soluble in water.
Typical storage-20°CRecommended for long-term storage of stock solutions.

Identity and Pharmacological Classification

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.

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.

Related pages on this site

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.

Reference notes

Anne-Claude Gingras is a senior investigator at Lunenfeld-Tanenbaum Research Institute, and a professor in the department of molecular genetics at the University of Toronto. She is an expert in mass spectrometry based proteomics technology that allows identification and quantification of protein from various biological samples. Gingras was born on Île d'Orléans, Quebec. She earned her undergraduate degree at Université Laval in Quebec. She completed her PhD in biochemistry at McGill University in Montreal, studying how 4E-BP1 regulated translation initiation, under the mentorship of Nahum Sonenberg. After graduating in 2001, she began postdoctoral research in Seattle at the Institute for Systems Biology in the lab of Ruedi Aebersold, where she studied proteomics for three years. In 2005, Gingras moved to Toronto and joined the Lunenfeld-Tanenbaum Research Institute, and in 2006, she began teaching at the University of Toronto in the department of molecular genetics.

7-Dehydrocholesterol (7-DHC) is a zoosterol that functions in the serum as a cholesterol precursor, and is photochemically converted to vitamin D3 in the skin, therefore functioning as provitamin-D3. The presence of this compound in human skin enables humans to manufacture vitamin D3 (cholecalciferol). Upon exposure to ultraviolet UV-B rays in the sun light, 7-DHC is converted into vitamin D3 via previtamin D3 as an intermediate isomer. It is also found in the milk of several mammalian species. Lanolin, a waxy substance that is naturally secreted by wool-bearing mammals, contains 7-DHC which is converted into vitamin D by sunlight and then ingested during grooming as a nutrient. In insects 7-dehydrocholesterol is a precursor for the hormone ecdysone, required for reaching adulthood. 7-DHC was discovered by Nobel-laureate organic chemist Adolf Windaus.

Akin to ordinary ink printers, bioprinters have three major components to them. These are the hardware used, the type of bio-ink, and the material it is printed on (biomaterials). Bio-ink is a material made from living cells that behaves much like a liquid, allowing people to 'print' it in order to create the desired shape. To make bio-ink, scientists create a slurry of cells that can be loaded into a cartridge and inserted into a specially designed printer, along with another cartridge containing a gel known as bio-paper. In bioprinting, there are three major types of printers that have been used. These are inkjet, laser-assisted, and extrusion printers. Inkjet printers are mainly used in bioprinting for fast and large-scale products. One type of inkjet printer, called drop-on-demand inkjet printer, prints materials in exact amounts, minimizing cost and waste. Printers that use lasers provide high-resolution printing; however, these printers are often expensive. Extrusion printers print cells layer-by-layer, just like 3D printing to create 3D constructs. In addition to just cells, extrusion printers may also use hydrogels infused with cells.

In the periodic table, nobelium is located to the right of the actinide mendelevium, to the left of the actinide lawrencium, and below the lanthanide ytterbium. Nobelium metal has not yet been prepared in bulk quantities, and bulk preparation is currently impossible. Nevertheless, a number of predictions and some preliminary experimental results have been done regarding its properties. The lanthanides and actinides, in the metallic state, can exist as either divalent (such as europium and ytterbium) or trivalent (most other lanthanides) metals. The former have fns2 configurations, whereas the latter have fn−1d1s2 configurations. In 1975, Johansson and Rosengren examined the measured and predicted values for the cohesive energies (enthalpies of crystallization) of the metallic lanthanides and actinides, both as divalent and trivalent metals. The conclusion was that the increased binding energy of the [Rn]5f136d17s2 configuration over the [Rn]5f147s2 configuration for nobelium was not enough to compensate for the energy needed to promote one 5f electron to 6d, as is true also for the very late actinides: thus einsteinium, fermium, mendelevium, and nobelium were expected to be divalent metals, although for nobelium this prediction has not yet been confirmed.

Sources: en.wikipedia.org

Reference notes

Concerns regarding the sustainability of Chinese-financed projects, environmental impacts, and the lack of transparency in their investments call for a careful assessment of these collaborations. Iranian President Mahmoud Ahmadinejad met with Mahama in 2013 to hold discussions on strengthening the Non-Aligned Movement and also co–chair a bilateral meeting between Ghana and Iran at the Ghanaian presidential palace Flagstaff House. The Sustainable Development Goals (SDG) were integrated into Ghana's development agenda and the budget. According to reports, the SDGs were implemented through a decentralized planning approach. This allows for stakeholders' participation, such as in UN agencies, traditional leaders, civil society organizations, academia, and others. The 17 SDGs are a global call to action to end poverty among others, and the UN and its partners in the country are working towards achieving them. According to the President Nana Akufo-Addo, Ghana was "the first Sub-Saharan African country to achieve the goal of halving poverty, as contained in Goal 1 of the Millennium Development Goals".

The American Journal of Clinical Pathology is a monthly peer-reviewed medical journal covering clinical pathology. It was established in 1931 and is published by Oxford University Press. It is the official journal of the American Society for Clinical Pathology and the Academy of Clinical Laboratory Physicians and Scientists. The editor-in-chief is Steven H. Kroft (Medical College of Wisconsin). According to the Journal Citation Reports, the journal has a 2020 impact factor of 2.493.

=== Opioid agonist === β-Endorphin is an agonist of the opioid receptors; it preferentially binds to the μ-opioid receptor. Evidence suggests that it serves as a primary endogenous ligand for the μ-opioid receptor, the same receptor to which the chemicals extracted from opium, such as morphine, derive their analgesic properties. β-Endorphin has the highest binding affinity of any endogenous opioid for the μ-opioid receptor. Opioid receptors are a class of G-protein coupled receptors, such that when β-endorphin or another opioid binds, a signaling cascade is induced in the cell. Acetylation of the N-terminus of β-endorphin, however, inactivates the neuropeptide, preventing it from binding to its receptor. The opioid receptors are distributed throughout the central nervous system and within the peripheral tissue of neural and non-neural origin. They are also located in high concentrations in the periaqueductal gray, locus coeruleus, and the rostral ventromedial medulla. In addition to the full-length peptide, brain and pituitary tissue also contain shorter β-endorphin fragments such as β-endorphin(1–27), which can act as a competitive antagonist at μ-opioid receptors and attenuate the analgesic effects of β-endorphin(1–31) in experimental models. Voltage-dependent calcium channels (VDCCs) are important membrane proteins that mediate the depolarization of neurons, and play a major role in promoting the release of neurotransmitters. When endorphin molecules bind to opioid receptors, G proteins activate and dissociate into their constituent Gα and Gβγ sub-units.

Benzodiazepines developed in the former Soviet Union (e.g. phenazepam, gidazepam etc.) Benzodiazepines predominantly used only in Japan (e.g. nimetazepam, flutoprazepam etc.) 4,5-cyclised benzodiazepines (e.g. ketazolam, cloxazolam etc.), and other compounds not researched by Roche Benzodiazepines developed more recently (e.g. remimazolam, QH-ii-066, Ro48-6791 etc.) "Designer" benzodiazepines for which in vitro binding data are unavailable (e.g. flubromazolam, pyrazolam etc.) While binding or activity data are available for most of these compounds also, the assay conditions vary between sources, meaning that in many cases the values are not suitable for a direct comparison. Many older sources used animal measures of activity (i.e. sedation or anticonvulsant activity) but did not measure in vitro binding to benzodiazepine receptors. See for instance Table 2 vs Table 11 in the Chem Rev paper, Table 2 lists in vitro pIC50 values matching those below, while Table 11 has pEC50 values derived from in vivo assays in mice, which show the same activity trends but cannot be compared directly, and includes data for compounds such as diclazepam and flubromazepam which are not available in the main data set. Also note;

=== 5-methylcytosine === Spontaneous deamination of 5-methylcytosine results in thymine and ammonia. This is the most common single nucleotide mutation. In DNA, this reaction, if detected prior to passage of the replication fork, can be corrected by the enzyme thymine-DNA glycosylase, which removes the thymine base in a G/T mismatch. This leaves an abasic site that is repaired by AP endonucleases and polymerase, as with uracil-DNA glycosylase.

Sources: en.wikipedia.org

Notes from published material

== Etymology == Choroid plexus translates from the Latin plexus chorioides, which mirrors Ancient Greek χοριοειδές πλέγμα. The word chorion was used by Galen to refer to the outer membrane enclosing the fetus. Both meanings of the word plexus are given as pleating, or braiding. As often happens language changes and the use of both choroid or chorioid is both accepted. Nomina Anatomica (now Terminologia Anatomica) reflected this dual usage.

2 HNO3 ⇌ H2NO+3 + NO−3 ⇌ H2O + [NO2]+ + [NO3]− Two hydrates, HNO3·H2O and HNO3·3H2O, are known that can be crystallised. It is a strong acid and concentrated solutions are strong oxidising agents, though gold, platinum, rhodium, and iridium are immune to attack. A 3:1 mixture of concentrated hydrochloric acid and nitric acid, called aqua regia, is still stronger and successfully dissolves gold and platinum, because free chlorine and nitrosyl chloride are formed and chloride anions can form strong complexes. In concentrated sulfuric acid, nitric acid is protonated to form nitronium, which can act as an electrophile for aromatic nitration:

==== Cubans call for Urquía Carreño to resign ==== On January 12, 2024, after the document was sent out by the Board to the larger community of Cuban Freemasons, a group of 18 Lodge Masters from all over Cuba demanded the immediate resignation of Urquía Carreño. When the robbery was made public, Llansó received large donations of food from other Freemasons and the Daughters of Acacia. Urquía Carreño refused to step down, and asked the Freemasons of Cuba to remain patient while the investigation was underway. Instead of stepping down, Urquía Carreño sent all 18 of those Lodge Masters to be sent in front of the Supreme Court of Masonic Justice for trials and investigations, and also ordered Viñas Alonso to be tried by the Supreme Court.

In Australia and New Zealand, it leads to eligibility for fellowship of the Royal Australasian College of Physicians, the Royal Australasian College of Surgeons, or a number of similar bodies. In Canada, once medical doctors successfully complete their residency program, they become eligible for certification by the Royal College of Physicians and Surgeons of Canada or the College of Family Physicians of Canada (CFPC) if the residency program was in family medicine. Many universities now offer "enhanced skills" certifications in collaboration with the CFPC, allowing family physicians to receive training in various areas such as emergency medicine, palliative care, maternal and child health care, and hospital medicine. Additionally, successful graduates of the family medicine residency program can apply to the "Clinical Scholar Program" in order to be involved in family medicine research. In Mexico, after finishing their residency, physicians obtain the degree of "Specialist", which renders them eligible for certification and fellowship, depending on the field of practice. In Nigeria, physicians are awarded the Fellowship of their respective postgraduate medical college. This fellowship is a prerequisite for recognition as a consultant specialist in Nigeria and many West African countries. Graduates may receive any of the following postgraduate qualifications: 'FMCP', 'FMCS', 'FMCR', 'FMCPath', etc. – conferred by the National Postgraduate Medical College of Nigeria (NPMCN) depending on specialty. 'FWACP' – Fellow of the West African College of Physicians.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist developed for research. It has not been approved as a medication in any country. It is classified as an unapproved drug and a prohibited substance in sport.

Is cardarine a steroid?

No. Cardarine is not an anabolic steroid; it belongs to a different chemical class that targets PPARδ. Steroids act primarily through androgen receptors, while cardarine acts through a nuclear receptor involved in metabolism.

What did animal studies find?

Some rodent studies reported increased endurance and changes in fat metabolism after cardarine exposure. Long-term studies in animals also raised concerns about cancer in certain tissues. Human trial data are limited, so these findings cannot be directly translated to people.

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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