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Identity And Pharmacological Classification — Deep Dive

By Editorial Desk · published 2026-04-17 · last reviewed 2026-05-22 · Wiki

A practical reference on PPARδ agonist: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

Reviewed 2026-05-22. Anything still debated is marked as such rather than presented as settled.

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.

Cardarine as Investigational PPARδ Agonist

Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.

Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.

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.

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.

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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.

Background from the literature

Insect pests such as the potato tuber moth and Colorado potato beetle, which are predicted to spread into areas currently too cold for them. Aphids which act as vectors for many potato viruses and will spread under increased temperatures. Pathogens causing potato blackleg disease (e.g. Dickeya) grow and reproduce faster at higher temperatures. Bacterial infections such as Ralstonia solanacearum will benefit from higher temperatures and spread more easily through flash flooding. Late blight benefits from higher temperatures and wetter conditions. Late blight is predicted to become a greater threat in some areas (e.g. in Finland) and become a lesser threat in others (e.g. in the United Kingdom).

=== Regulation === Careful regulation of NADPH oxidase activity is crucial to maintain a healthy level of ROS in the body. The enzyme is dormant in resting cells but becomes rapidly activated by several stimuli, including bacterial products and cytokines. Vascular NADPH oxidases are regulated by a variety of hormones and factors known to be important players in vascular remodeling and disease. These include thrombin, platelet-derived growth factor (PDGF), tumor necrosis factor (TNFa), lactosylceramide, interleukin-1, and oxidized LDL. It is also stimulated by agonists and arachidonic acid. Conversely, assembly of the complex can be inhibited by apocynin and diphenylene iodonium. Apocynin decreases influenza-induced lung inflammation in mice in vivo and so may have clinical benefits in the treatment of influenza. Ang-1 triggers NOX2, NOX4, and the mitochondria to release ROS and that ROS derived from these sources play distinct roles in the regulation of the Ang-1/Tie 2 signaling pathway and pro-angiogenic responses.

The mechanism of the Hofmeister series is not entirely clear, but seems to result mainly from effects on the solvent at higher salt concentrations (> 100 mM). Early members of the series increase solvent surface tension and decrease the solubility of nonpolar molecules (salt out); in effect, they strengthen the hydrophobic interaction. By contrast, later salts in the series increase the solubility of nonpolar molecules (salt in) and decrease the order in water; in effect, they weaken the hydrophobic effect. However, these salts also interact directly with proteins (which are charged and have strong dipole moments) and may even bind specifically (e.g., phosphate and sulfate binding to ribonuclease A). Ions that have a strong salting in effect such as I− and SCN− are strong denaturants, because they salt in the peptide group, and thus interact much more strongly with the unfolded form of a protein than with its native form. Consequently, they pull the unfolding reaction. Moreover, they may have direct interactions with some standard hydrophobic molecules, e.g., benzene. A quantum chemical investigation suggests an electrostatic origin of the Hofmeister series, which appears to quantify this qualitative series (at least for anions).

This can lead to excessive insulin levels in the blood (hyperinsulinemia), which can be responsible for multiple symptoms. Definitive genotype–phenotype correlation for insulin receptor defects is difficult to establish primarily due to the rarity of these syndromes. However, researchers believe more severe phenotype changes are due to a mutation in the alpha subunit of the receptor.

2-Oxoadipic acid, also known as α-ketoadipic acid, is an intermediate in the metabolism of lysine and tryptophan. The conjugate base and carboxylate is 2-oxoadipate or α-ketoadipate, which is the biochemically relevant form. Glutaric acid is naturally produced by chain extension of α-ketoglutarate to 2-oxoadipic acid.

Sources: en.wikipedia.org

Reference notes

==== Commercialization ==== The company announced in November 2021 that it aims to achieve mass-manufacturing in 2024 of its silicon batteries, having pouch-cell samples produced by its manufacturing partner EVE Energy sent to be tested by global car makers. The company announced in 2023 that its batteries will be commercially available in VinFast vehicles in 2025. The CEO said that the company does not plan to become a battery manufacturer or supplier, but instead plans to license its technology to major manufacturers or lease dedicated manufacturing capacity from existing suppliers, saying its silicon batteries can be manufactured using existing factories and manufacturing processes. StoreDot demonstrated its batteries in a prototype Polestar 5 sedan in 2024, however the 2025 model was not set to debut with StoreDot batteries but with batteries developed and manufactured by SK On. StoreDot batteries were still in the testing phase in October 2024 and they had not been incorporated into any upcoming vehicle platforms. StoreDot stated in 2026 it needs two more years of development in order to commercialize its product.

The MNHN continued to flourish during the 19th century, particularly under the direction of chemist Michel Eugène Chevreul, His research with animal fats revolutionised the manufacture of soap and of candles and led to his isolation of the heptadecanoic (margaric), stearic, and oleic fatty acids. In the medical field, he was first to demonstrate that diabetics excrete glucose. and to isolate creatine. His theories of colour "provided the scientific basis for Impressionist and Neo-Impressionist painting." Henri Becquerel held the chair for Applied Physics at the MNHN (1892–1908). By wrapping uranium salts in photographic paper, he first demonstrated the radioactive properties of uranium. In 1903, he shared the Nobel Prize in Physics with Pierre Curie and Marie Curie for the discovery of spontaneous radioactivity. Four generations of Becquerels held this chairmanship, from 1838 to 1948. As its collections grew, the MNHN was enlarged, with the construction of a new gallery of zoology. it was begun in 1877 and completed in 1889, for the 100th anniversary of the French Revolution. A new Gallery of Palaeontology and Comparative Anatomy was opened in 1898. The cost of construction drained the museum budget and it began to run short of funds. Its emphasis on teaching brought it into conflict with the University of Paris, which had better political connections. It gradually scaled back its program of teaching and focused primarily on research and the museum collections.

The Han nationalist revolutionary Sun Yat-sen made Han Chinese superiority a basic tenet of the 1911 Revolution. In Sun's revolutionary philosophical view, Han identity is exclusively possessed by the so-called civilized Hua Xia people who originated from the Central Plains, and were also the former subjects of the Celestial empire and evangelists of Confucianism. Restoring Chinese rule to the Han majority was one of the motivations for supporters of the 1911 Revolution to overthrow the Manchu-led Qing dynasty in 1912, which led to the establishment of the Han-dominated Republic of China. After the establishment of the republic, Sun went to offer sacrifices in Hongwu Emperor's Xiao Mausoleum:

an intermediate or building block in the synthesis of non-ionic and other surfactants and related functional additives; a component of lubricant and plastic additive systems, including thermoplastic polyurethanes, where long-chain alcohols are used to modify flexibility and permeability; a minor constituent of policosanol-type mixtures employed in cosmetics and personal-care products as part of the lipid phase of creams and emulsions. Because of its chain length and structural similarity to other fatty alcohols, 1-heneicosanol is also used as a reference compound and analytical standard in studies of plant waxes, policosanol mixtures and related lipid fractions. Available safety data sheets describe 1-heneicosanol as a low-volatility solid that is not classified as hazardous under European CLP regulations, but which may cause mild irritation to the skin, eyes and respiratory tract on contact or inhalation of dust. Standard laboratory precautions such as avoiding dust formation, using local exhaust ventilation and wearing eye and skin protection are recommended.

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.

What is cardarine?

Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.

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