The short version of PPARδ fits in a sentence. The long version — which is the one that helps — is below.
Reviewed 2026-08-01. Anything still debated is marked as such rather than presented as settled.
GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.
Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.
Sporting authorities added GW501516 to prohibited lists after it appeared in athlete samples and online markets. The World Anti-Doping Agency classifies it as a hormone and metabolic modulator, and its use can lead to an anti-doping rule violation. Some early laboratory work suggested effects on fatty acid oxidation and endurance-related metabolism in animals, but those findings do not establish safe or effective use in people. Reports of adverse events in humans are scarce and often anecdotal, which complicates risk assessment.
Legal status varies by country. In some places, cardarine is controlled under medicines or psychoactive substances laws; in others, it may be sold with minimal oversight as a research chemical. Customs agencies have intercepted shipments, and several national health agencies have issued warnings about products marketed for bodybuilding or performance enhancement. The lack of a standardized pharmaceutical supply means identity, purity, and contamination levels can differ widely between samples. These factors make cardarine a regulatory and public health concern rather than a conventional prescription drug.
| Property | Value | Notes |
|---|---|---|
| Primary target | PPARδ | Nuclear receptor; not androgen receptor |
| Studied indications | Dyslipidemia; obesity; diabetes | Early clinical research; development discontinued |
| Rodent toxicity | Tumor formation in multiple tissues | Dose-dependent findings in some studies |
| Human approval | None | No approved therapeutic use |
| Typical analytical method | LC-MS/MS | Used for identity and quantification |
Laboratory detection of GW501516 commonly uses liquid chromatography coupled with tandem mass spectrometry. The method can identify the parent compound or its metabolites in urine and blood after sample cleanup. Protein precipitation, solid-phase extraction, or enzymatic hydrolysis may precede analysis, depending on the matrix. Reference standards are required for accurate quantification and confirmation. Because the compound is not approved, testing often occurs in anti-doping, forensic, or research settings rather than routine clinical care. Results are reported with limits of detection and quantification.
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.
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.
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.
More divergent allele pairs enable presentation of a broader and less redundant repertoire of peptides, thereby potentially enhancing immune recognition. This concept, sometimes referred to as MHC or HLA evolutionary divergence, extends classical models of MHC diversity and heterozygote advantage by treating allelic variation as a continuum rather than a binary state. MHC diversity has also been suggested as a possible indicator for conservation, because large, stable populations tend to display greater MHC diversity than smaller, isolated populations. Small, fragmented populations that have experienced a population bottleneck typically have lower MHC diversity. For example, relatively low MHC diversity has been observed in the cheetah (Acinonyx jubatus), Eurasian beaver (Castor fiber), and giant panda (Ailuropoda melanoleuca). In 2007 low MHC diversity was attributed a role in disease susceptibility in the Tasmanian devil (Sarcophilus harrisii), native to the isolated island of Tasmania, such that an antigen of a transmissible tumor, involved in devil facial tumour disease, appears to be recognized as a self antigen. To offset inbreeding, efforts to sustain genetic diversity in populations of endangered species and of captive animals have been suggested. In ray-finned fish like rainbow trout, allelic polymorphism in MHC class II is reminiscent of that in mammals and predominantly maps to the peptide binding groove.
== Adverse effects == Adverse effects include hypersensitivity reactions and allergic reactions, immune system disorders, skin disorders including hives, oedema and widespread rashes. Additionally, the following adverse effects have been reported: heartburn, indigestion, tiredness, diarrhoea, constipation, loss of appetite, general malaise, dizziness, insomnia, headache, and decreased pulse rate. It does not have systemic anticholinergic side effects. Mebeverine can, on highly rare occasions, cause drug-induced acute angle closure glaucoma. In a urine drug-screening test, mebeverine can affect a false positive result for amphetamines.
==== Deep anterior lamellar keratoplasty ==== In this procedure, the anterior layers of the central cornea are removed and replaced with donor tissue. Endothelial cells and the Descemets membrane are left in place. This technique is used in cases of anterior corneal opacifications, scars, and ectatic diseases such as keratoconus.
The first genuine decay of atoms of oganesson was observed in 2002 at the Joint Institute for Nuclear Research (JINR) in Dubna, Russia, by a joint team of Russian and American scientists. Headed by Yuri Oganessian, a Russian nuclear physicist of Armenian ethnicity, the team included American scientists from the Lawrence Livermore National Laboratory in California. As the decay energy of 294Og matched that of 212mPo, a common impurity produced in fusion reactions aimed at producing superheavy elements, the announcement of the discovery was delayed until after a 2005 confirmatory experiment aimed at producing more oganesson atoms. The 2005 experiment used a different beam energy (251 MeV instead of 245 MeV) and target thickness (0.34 mg/cm2 instead of 0.23 mg/cm2). On 9 October 2006, the researchers announced that they had indirectly detected a total of three (possibly four) nuclei of oganesson-294 (one or two in 2002 and two more in 2005) produced via collisions of californium-249 atoms and calcium-48 ions.
Sources: en.wikipedia.org
The uprising had a significant effect on the decisions in Versailles that granted Poland not only the area won by the insurrectionists but also major cities with a significant German population like Bydgoszcz (Bromberg), Leszno (Lissa) and Rawicz (Rawitsch), as well as the lands of the Polish Corridor, which were also part of the Polish–Lithuanian Commonwealth before the First Partition of Poland in 1772 and connected Poland to the Baltic Sea. Germany's territorial losses following the Treaty of Versailles incited German revanchism, and created unresolved problems such as the status of the independent Free City of Danzig and of the Polish Corridor between East Prussia and the rest of Germany. This revanchism was not a popular political idea in the Weimar Republic. Attending to these issues was part of Adolf Hitler's political platform, but failed to gain any traction in the 1920s. The idea was relegated to the political margins, until the Nazis seized power. Nevertheless, Nazi Germany effectively recognised Poland's new borders in the German–Polish declaration of non-aggression of 1934, which normalised relations between the two countries. However, after the death of Polish leader Józef Piłsudski (who was admired by Hitler), the German Anschluss with Austria and the German occupation of Czechoslovakia, Hitler unilaterally withdrew from the German-Polish Non-Aggression Pact and invaded Poland in 1939, which led to the outbreak of World War II.
==== Granuloma ==== Drug-induced hepatic granulomas are usually associated with granulomas in other tissues and patients typically have features of systemic vasculitis and hypersensitivity. More than 50 drugs have been implicated.
== Structure-function relationship == The structure of lysine carboxypeptidase can explain its preferences for the P1' and P1 residues. The aspartic acid (its orientation determined by the cis-peptide bond between the adjacent proline and tyrosine) that is located near the S1' pocket of the active site is responsible for the preference of lysine over arginine as the P1' residue. Unlike arginine, lysine can approach this area frontally which sets the peptide bond up for an easier break. Meanwhile, the phenolic side chains near pocket S1 cause the enzyme to prefer more medium sized P1 residues over larger ones; this reduces the amount of shifting that needs to occur. This explains the enzyme's preference of alanine and methionine over glycine.
Sources: en.wikipedia.org
It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.
Rodent studies found dose-dependent tumors in several organs. The sponsor discontinued the program over cancer concerns. Human risk from long-term use remains unknown.
Controlled human endurance trials are lacking. Animal studies show increased exercise capacity under some conditions. Anecdotal reports are not equivalent to clinical evidence.
No. Major drug regulators have not approved GW501516 for treating any medical condition. Products sold as cardarine are typically unapproved research chemicals or supplements, so their contents and safety are not assured.