If you have been reading about PPARδ agonist and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.
Updated 2026-02-08. Numbers and descriptions here follow the published literature rather than marketing material.
GW501516 acts on PPARδ, a nuclear receptor that helps regulate fatty acid oxidation and energy homeostasis. In animal studies, activation of this receptor was associated with increased endurance and changes in lipid metabolism. Human trials examined effects on blood lipids and other metabolic markers, but the compound did not advance to approval. Rodent studies later reported tumors in multiple tissues at doses used in those experiments. Whether those findings translate to human risk remains uncertain, and the clinical relevance of the animal data is still debated.
Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.
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.
| Property | Value | Notes |
|---|---|---|
| Common name | Cardarine | Common internet and media name. |
| Research code | GW501516 | Also written GW-1516. |
| Drug class | PPARδ agonist | Not a selective androgen receptor modulator. |
| Development status | Discontinued | Clinical development halted after rodent cancer findings. |
| Regulatory status | Prohibited in sport | Listed by WADA; not approved as medicine. |
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.
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 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 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.
The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.
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.
== Further reading == Marshall JD, Beck S, Maffei P, Naggert JK (2007). "Alström syndrome". Eur. J. Hum. Genet. 15 (12): 1193–202. doi:10.1038/sj.ejhg.5201933. PMID 17940554. Alfonso Ortigado., et al. "Semaglutide in Alström Syndrome: An Improvement in the Natural Course of Cardiomyopathy". EC Paediatrics 14.7 (2025): 01-07. Berkower C. Voice of the Patient Report [Internet]. Alstrom Syndrome International; 2022 [cited 2024 Aug 22]. Available from: https://www.alstrom.org/wp-content/uploads/2023/05/ASI-EL-PFDD_FINAL_8May23.pdf Knorz VJ, Spalluto C, Lessard M, Purvis TL, Adigun FF, Collin GB, Hanley NA, Wilson DI, Hearn T (2010): Centriolar association of ALMS1 and likely centrosomal functions of the ALMS motif-containing proteins C10orf90 and KIAA1731. Mol Biol Cell (21):3617-3629. Koc E, Bayrak G, Suher M, Ensari C, Aktas D, Ensari A (2006): Rare case of Alstrom syndrome without obesity and with short stature, diagnosed in adulthood. Nephrology11(2):81-84. Roy A, Patel L, Yuan M, O'Shea C, Alvior AMB, Charalambides M, Moxon D, Baig S, Bunting KV, Gehmlich K, Geberhiwot T, Steeds RP. Defining the cardiovascular phenotype of adults with Alström syndrome. Int J Cardiol. 2024 Aug 15;409:132212. doi: 10.1016/j.ijcard.2024.132212. Epub 2024 May 26. PMID 38806112.
=== Purification of a tagged protein === Another way to tag proteins is to engineer an antigen peptide tag onto the protein, and then purify the protein on a column or by incubating with a loose resin that is coated with an immobilized antibody. This particular procedure is known as immunoprecipitation. Immunoprecipitation is capable of generating an extremely specific interaction which usually results in binding only the desired protein. The purified tagged proteins can then easily be separated from the other proteins in solution and later eluted back into clean solution. When the tags are not needed anymore, they can be cleaved off by a protease. This often involves engineering a protease cleavage site between the tag and the protein. Self-cleaving tags eliminate the need for proteases to separate tag from target protein of interest during purification process (e.g. iCapTag™). The main component of the tag is an intein, which cleaves off simply after a pH change. Tagless and pure target protein is then released into the elution buffer. Emerging methods in synthetic biology explore chromatography-free alternatives by harnessing liquid-liquid phase separation to create synthetic organelles within bacterial cells, such as E. coli. These approaches use phase-separated RNA structures to compartmentalize proteins, enabling in-cell organization, self-cleavage via inteins, and direct release of tag-free proteins, which leads to enhanced efficiency in recombinant protein workflows.
A glycosidic bond is formed between the hemiacetal or hemiketal group of a saccharide (or a molecule derived from a saccharide) and the hydroxyl group of some compound such as an alcohol. A substance containing a glycosidic bond is a glycoside. The term 'glycoside' is now extended to also cover compounds with bonds formed between hemiacetal (or hemiketal) groups of sugars and several chemical groups other than hydroxyls, such as -SR (thioglycosides), -SeR (selenoglycosides), -NR1R2 (N-glycosides), or even -CR1R2R3 (C-glycosides). Particularly in naturally occurring glycosides, the compound ROH from which the carbohydrate residue has been removed is often termed the aglycone, and the carbohydrate residue itself is sometimes referred to as the 'glycone'.
Bromine is significantly less abundant in the crust than fluorine or chlorine, comprising only 2.5 parts per million of the Earth's crustal rocks, and then only as bromide salts. It is significantly more abundant in the oceans, resulting from long-term leaching. There, it makes up 65 parts per million, corresponding to a ratio of about one bromine atom for every 660 chlorine atoms. Salt lakes and brine wells may have higher bromine concentrations: for example, the Dead Sea contains 0.4% bromide ions. It is from these sources that bromine extraction is mostly economically feasible. Bromine is the tenth most abundant element in seawater. The main sources of bromine production are Israel and Jordan. The element is liberated by halogen exchange, using chlorine gas to oxidise Br− to Br2. This is then removed with a blast of steam or air, and is then condensed and purified. Today, bromine is transported in large-capacity metal drums or lead-lined tanks that can hold hundreds of kilograms or even tonnes of bromine. The bromine industry is about one-hundredth the size of the chlorine industry. Laboratory production is unnecessary because bromine is commercially available and has a long shelf life.
== Substrate immobilization == Another widely used application of the immobilization approach together with enzymes has been the enzymatic reactions on immobilized substrates. This approach facilitates the analysis of enzyme activities and mimics the performance of enzymes on e.g. cell walls.
Sources: en.wikipedia.org
== Distribution coefficient and log D == The distribution coefficient, log D, is the ratio of the sum of the concentrations of all forms of the compound (ionized plus un-ionized) in each of the two phases, one essentially always aqueous; as such, it depends on the pH of the aqueous phase, and log D = log P for non-ionizable compounds at any pH. For measurements of distribution coefficients, the pH of the aqueous phase is buffered to a specific value such that the pH is not significantly perturbed by the introduction of the compound. The value of each log D is then determined as the logarithm of a ratio—of the sum of the experimentally measured concentrations of the solute's various forms in one solvent, to the sum of such concentrations of its forms in the other solvent; it can be expressed as
In the first reaction the bidentate ligand ethylene diamine forms a chelate complex with the copper ion. Chelation results in the formation of a five-membered ring. In the second reaction the bidentate ligand is replaced by two monodentate methylamine ligands of approximately the same donor power, meaning that the enthalpy of formation of Cu–N bonds is approximately the same in the two reactions. Under conditions of equal copper concentrations and when the concentration of methylamine is twice the concentration of ethylenediamine, the concentration of the bidentate complex will be greater than the concentration of the complex with 2 monodentate ligands. The effect increases with the number of chelate rings so the concentration of the EDTA complex, which has five chelate rings, is much higher than a corresponding complex with two monodentate nitrogen donor ligands and four monodentate carboxylate ligands. Thus, the phenomenon of the chelate effect is a firmly established empirical fact: under comparable conditions, the concentration of a chelate complex will be higher than the concentration of an analogous complex with monodentate ligands. The thermodynamic approach to explaining the chelate effect considers the equilibrium constant for the reaction: the larger the equilibrium constant, the higher the concentration of the complex.
=== Grafting techniques === Grafting copolymers to a surface can be envisioned as fixing polymeric chains to a structurally different polymer substrate with the intention of changing surface functionality while preserving bulk mechanical properties. The nature and degree of surface functionalization is determined by both the choice of copolymer and the type and extent of grafting.
Vitamin C has a definitive role in preventing and treating scurvy, which is a disease caused by vitamin C deficiency. Beyond that, a role for vitamin C as prevention or treatment for various diseases is disputed, with reviews often reporting conflicting results. No effect of vitamin C supplementation reported for overall mortality. It is on the World Health Organization's List of Essential Medicines and on the World Health Organization's Model Forumulary. In 2023, it was the 226th most commonly prescribed medication in the United States, with more than 1 million prescriptions.
Sources: en.wikipedia.org
No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.
Preclinical rodent studies reported cancers, including liver and bladder tumors, at tested doses. The human relevance of those findings is uncertain, but development was discontinued. No approved human product resulted.
No. It remains an investigational compound without approved therapeutic labeling. Sports regulators prohibit its use, and health agencies have warned against consuming it.
Legal status varies by country, but cardarine is not approved as a medicine in major jurisdictions. It is often sold as a research chemical, a category that may not be lawful for human use. Buyers should check local laws and product labels carefully.