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Identity And Pharmacological Mechanism — Quick Reference

By Editorial Desk · published 2026-04-18 · last reviewed 2026-05-03 · News

Everything below concerns GW501516. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Last reviewed on 2026-05-03. Where a claim depends on a specific study, the study is described rather than over-claimed.

Identity and Pharmacological Mechanism

Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.

Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.

The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.

Regulation and Detection

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.

Cardarine at a glance

PropertyValueNotes
Chemical classSynthetic PPARδ agonistNot a steroid or a selective androgen receptor modulator.
Common synonymsCardarine, GW501516, GW-501516, endurobolNames vary by supplier and literature source.
AppearanceWhite to off-white powderConsistent with many small-molecule research chemicals.
SolubilityLow in water; soluble in DMSO and ethanolOften prepared in organic solvent for laboratory work.
Primary targetPPARδ (NR1C2)Nuclear receptor involved in lipid and energy metabolism.

Detection, Stability, and Quality

Stability of GW501516 depends on form, temperature, light exposure, and moisture. Solid reference material is typically stored frozen or refrigerated in a desiccator and protected from light. Solutions in organic solvents such as dimethyl sulfoxide are often kept frozen in aliquots to reduce freeze-thaw cycling. Aqueous solubility is low, so aqueous stock solutions can be difficult to prepare without cosolvents. Degradation may appear as changes in chromatographic purity or mass spectral signal. Stability studies are needed to establish shelf life for any specific preparation.

Quality assessment for cardarine samples usually combines identity, purity, and impurity testing. Nuclear magnetic resonance spectroscopy and mass spectrometry can confirm molecular structure, while high-performance liquid chromatography estimates purity. Certificates of analysis from testing laboratories may list these results, but they do not establish safety or legality. In the absence of approved manufacturing, products sold online may contain the wrong compound, variable amounts, or unlisted contaminants. Independent verification is therefore central to analytical work and to interpreting any reported biological activity.

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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.

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.

Further detail

The Druze strictly avoid iconography, but use five colors ("Five Limits" خمس حدود khams ḥudūd) as a religious symbol: green, red, yellow, blue, and white. The First limit (green), identified by Ismail at-Tamimi (d. 1030) in the Epistle of the Candle, represents either Hamza Ibn Ali or Jesus, symbolizing the "Universal Mind/Intelligence/Nous".

Peroxisomes are microbodies bounded by a single membrane. A peroxisome has no DNA or ribosomes and the proteins that it needs are encoded in the nucleus, and selectively imported from the cytosol. Some proteins enter via the endomembrane reticulum. They have enzymes that rid the cell of toxic peroxides. The enzymatic content of the peroxisomes varies widely across the species, as it can in an individual organism. The peroxisomes in animal cells are concentrated in the liver cells and adipocytes.

== Metabolism == Most members of the genus Haemophilus require at least one of these blood factors for growth: hemin (sometimes called 'X-factor') and/or nicotinamide adenine dinucleotide (NAD; sometimes called 'V-factor'); they usually will not grow on blood agar plates. While NAD is released into blood agar by red blood cells, hemin is bound to the blood cells and is unavailable to bacteria in this medium which prevents the growth of many Haemophilus species. They are unable to synthesize important parts of the cytochrome system needed for respiration, and they obtain these substances from the heme fraction of blood hemoglobin. Clinical laboratories use tests for the hemin and NAD requirement to identify the isolates as Haemophilus species. The species Haemophilus haemoglobinophilus is an exception to this, as it has been shown to grow well on both blood and chocolate agars. Chocolate agar is an excellent Haemophilus growth medium, as it allows for increased accessibility to these factors. Alternatively, Haemophilus is sometimes cultured using the "Staph streak" technique: both Staphylococcus and Haemophilus organisms are cultured together on a single blood agar plate. In this case, Haemophilus colonies will frequently grow in small "satellite" colonies around the larger Staphylococcus colonies because the metabolism of Staphylococcus produces the necessary blood factor byproducts required for Haemophilus growth.

Sources: en.wikipedia.org

Background from the literature

=== Authorizations of COVID-19 vaccines === The COVID-19 pandemic, and sequencing of the causative virus SARS-CoV-2 at the beginning of 2020, led to the rapid development of the first approved mRNA vaccines. BioNTech and Moderna in December of the same year obtained approval for their mRNA-based COVID-19 vaccines. In December 2020, the UK Medicines and Healthcare products Regulatory Agency (MHRA) became the first global medicines regulator in history to approve an mRNA vaccine, granting emergency authorization for Pfizer–BioNTech's BNT162b2 COVID-19 vaccine for widespread use. Also, in December 2020, the US Food and Drug Administration gave emergency use authorization for the Pfizer–BioNTech COVID-19 vaccine and the Moderna COVID-19 vaccine.

== External links == IUPHAR GPCR Database – GHRH receptor Archived 2016-03-03 at the Wayback Machine somatotropin+releasing+hormone+receptor at the U.S. National Library of Medicine Medical Subject Headings (MeSH)

By using computational phylogenomic and structure predictions, experimental structural analyses, and cell biological assays, it was proposed that half of Goddard's structure is disordered and the other half is composed by alpha-helical amino acids. These analyses also indicated that Goddard's orthologs show similar results. Goddard's structure therefore appears to have been mainly conserved since its emergence. It has been proposed, that these four putative de novo genes have diverged beyond the point at which they can be found. However, the evidential strength of proposed "hidden homology" remains unclear since the study relies on very relaxed BLAST thresholds (high E-values/low identity, i.e. the "twilight zone") and on structural resemblance that could also reflect convergent evolution. Overall, de novo proteins are often short and enriched in intrinsically disordered regions (IDRs), and many are predicted to lack stable tertiary structure when isolated. However, comparative genome-wide analyses in rice suggest that the structural properties of de novo proteins can evolve rapidly in some lineages, with predicted decreases in disorder and increases in structured elements over short evolutionary timescales and incorporation of de novo proteins into heteromeric multimers. In Drosophila, a genome-wide study combining gene-age dating and structural modeling reported little overall predicted structural change among Drosophilinae de novo candidates, and ancestral sequence reconstruction suggested that many potentially well-folded candidates may be born well-folded.

=== Technical limitations === When the patient's body has insufficient adipocyte tissue to harvest as injectable breast filler, a combination of fat grafting and breast implants might provide the desired outcome. Although non-surgical breast augmentation with fat graft injections is not associated with implant-related medical complications (filler leakage, deflation, visibility, palpability, capsular contracture), the achievable breast volumes are physically limited; the large-volume, global bust augmentations realised with breast implants are not possible with the method of structural fat grafting. Global breast augmentation contrasts with the controlled breast augmentation of fat-graft injection, in the degree of control that the plastic surgeon has in achieving the desired breast contour and volume. The controlled augmentation is realised by infiltrating and diffusing the fat grafts throughout the breast; and it is feather-layered into the adjacent pectoral areas until achieving the desired outcome of breast volume and contour. Nonetheless, the physical fullness-of-breast achieved with injected fat-grafts does not visually translate into the type of buxom fullness achieved with breast implants; hence, patients who had plentiful fat-tissue to harvest attained a maximum breast augmentation of one bra cup size in one session of fat grafting to the breast.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.

How does cardarine interact with the body?

It binds to and activates PPARδ, a nuclear receptor that regulates genes related to fatty acid oxidation and energy use. This activation alters transcription in tissues such as skeletal muscle and liver. The full range of downstream effects in humans is not fully established.

Is cardarine found naturally?

No, cardarine is not known to occur naturally in plants, animals, or humans. It is a synthetic molecule produced for laboratory research. Products labeled as cardarine should therefore be treated as manufactured chemicals with variable purity.

Is cardarine legal?

Legal status varies by country. It is not approved as a medicine, and it is prohibited in sport. Some jurisdictions restrict import, sale, or possession.

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