If you have been reading about Cardarine 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.
Last reviewed on 2026-02-25. Where a claim depends on a specific study, the study is described rather than over-claimed.
Cardarine is the common name for GW501516, a synthetic compound studied as a peroxisome proliferator-activated receptor delta agonist. Researchers developed it to explore treatments for lipid disorders and metabolic conditions. It is not an approved medicine in any country. Early clinical work examined changes in HDL cholesterol and triglycerides, but development was discontinued after animal studies raised concerns about cancer. The compound remains available as a research chemical and appears in discussions of performance enhancement.
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.
Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.
A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.
Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.
| Property | Value | Notes |
|---|---|---|
| Common name | Cardarine | Also called GW501516 and endurobol. |
| Chemical formula | C21H18F3NO3S2 | Molecular weight about 453.5 g/mol. |
| Appearance | White to off-white solid | Form depends on synthesis and purity. |
| Solubility | Soluble in DMSO and ethanol | Low solubility in water. |
| Typical storage | -20 °C, desiccated, protected from light | Common for research chemicals. |
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.
Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.
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.
GW501516 acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in transcription of genes related to lipid handling and energy use. Activation of PPARδ can shift skeletal muscle toward greater fatty acid oxidation in animal models, which is one reason it drew interest for metabolic disease and exercise research. The exact downstream effects depend on tissue, species, dose, and duration. Human data are sparse, so many proposed benefits remain hypotheses rather than established clinical outcomes.
Laboratory studies have examined GW501516 in cell cultures and rodents for conditions such as dyslipidemia, insulin resistance, and obesity. Some trials in humans were initiated, but development was discontinued after preclinical findings raised concerns about cancer in certain models. Those findings do not prove that the compound causes cancer in people, but they contributed to regulatory caution. Later reviews often describe the evidence as preliminary and insufficient for assessing long-term safety.
Transmembrane protein 125 is a protein that, in humans, is encoded by the TMEM125 gene. It has 4 transmembrane domains and is expressed in the lungs, thyroid, pancreas, intestines, spinal cord, and brain. Though its function is currently poorly understood by the scientific community, research indicates it may be involved in colorectal and lung cancer networks. Additionally, it was identified as a cell adhesion molecule in oligodendrocytes, suggesting it may play a role in neuron myelination. The TMEM125 gene has no aliases, except for its encoded protein’s name. Its cytogenic location is at 1p34.2 on the plus strand and it spans from bases 43,272,723 to 43,273,379. TMEM125 comprises four exons. Five TMEM125 promoters were identified by Genomatix Gene2Promoter. The primary promoter (NM_001320244) is 1881 bp in length. It consists of binding sites for fork head domain factors and zinc finger transcription factors.
=== Shingrix === Shingrix is a suspension for intramuscular injection consisting of a lyophilized recombinant varicella zoster virus glycoprotein E antigen that is reconstituted at the time of use with AS01B suspension as an immunological adjuvant. The antigen is a purified truncated form of the glycoprotein, expressed in Chinese hamster ovary cells. The AS01B adjuvant suspension is composed of 3-O-desacyl-4'-monophosphoryl lipid A (MPL) from Salmonella (Minnesota strain) and a saponin molecule (QS-21) purified from Quillaja saponaria (soap bark tree) extract, combined in a liposomal formulation consisting of dioleoyl phosphatidylcholine (DOPC) and cholesterol in phosphate-buffered saline solution.
Cytolysis occurs when a cell bursts due to an osmotic imbalance that has caused excess water to move into the cell. Cytolysis can be prevented by several different mechanisms, including the contractile vacuole that exists in some paramecia, which rapidly pump water out of the cell. Cytolysis does not occur under normal conditions in plant cells because plant cells have a strong cell wall that contains the osmotic pressure, or turgor pressure, that would otherwise cause cytolysis to occur.
Dubnium, having an atomic number of 105, is a superheavy element; like all elements with such high atomic numbers, it is very unstable. The longest-lasting known isotope of dubnium, 268Db, has a half-life of around a day. No stable isotopes have been seen, and a 2012 calculation by JINR suggested that the half-lives of all dubnium isotopes would not significantly exceed a day. Dubnium can only be obtained by artificial production. The short half-life of dubnium limits experimentation. This is exacerbated by the fact that the most stable isotopes are the hardest to synthesize. Elements with a lower atomic number have stable isotopes with a lower neutron–proton ratio than those with higher atomic number, meaning that the target and beam nuclei that could be employed to create the superheavy element have fewer neutrons than needed to form these most stable isotopes. (Different techniques based on rapid neutron capture and transfer reactions are being considered as of the 2010s, but those based on the collision of a large and small nucleus still dominate research in the area.) Only a few atoms of 268Db can be produced in each experiment, and thus the measured lifetimes vary significantly during the process. As of 2022, following additional experiments performed at the JINR's Superheavy Element Factory (which started operations in 2019), the half-life of 268Db is measured to be 16+6−4 hours. The second most stable isotope, 270Db, has been produced in even smaller quantities: three atoms in total, with lifetimes of 33.4 h, 1.3 h, and 1.6 h.
Sources: en.wikipedia.org
=== Receptors === Innate immune system senses intact peptidoglycan and peptidoglycan fragments using numerous PRRs (pattern recognition receptors) that are secreted, expressed intracellularly or expressed on the cell surface.
== Further reading == Robertson, G. L. (2013). Food Packaging: Principles & Practice. CRC Press. ISBN 978-1-4398-6241-4 Yam, K. L., Encyclopedia of Packaging Technology, John Wiley & Sons, 2009, ISBN 978-0-470-08704-6 Harwell, Edward M., Packaging and Displaying Meats in Self-Service Meat Markets, United States Department of Agriculture. June 1953
=== Therapeutic reactivation and gene therapy === While increasing p53 levels might appear beneficial for treating cancer, sustained p53 activation can cause premature aging. A more promising approach involves restoring normal, endogenous p53 function. In some tumor types, this leads to regression via apoptosis or normalization of cell growth. The first commercial gene therapy, Gendicine, was approved in China in 2003 for head and neck squamous cell carcinoma. It delivers a functional copy of the TP53 gene using a modified adenovirus. The small-molecule inhibitor MI-63 can bind to MDM2, blocking its interaction with p53 and reactivating p53 in cancers where its function is suppressed. A p53 reactivator rezatapopt is in clinical trials in patients whose tumors show the common Y220C mutation of p53, and restores anti-cancer effectiveness to the mutated protein.
Sources: en.wikipedia.org
=== 21 March === Explosions were reported to have occurred at the city of Dzhankoi, Crimea. The local Russian administrator, Ihor Ivin, said that a 33-year-old man was taken to hospital due to shrapnel from a downed drone. The power grid was damaged and several buildings caught fire. The Ukrainian Defence Ministry said the explosions "...destroyed Russian Kalibr-KN cruise missiles as they were being transported by rail". The ministry added that the missiles were supposedly destined for submarine launch by the Russian Black Sea fleet, but Ukraine did not explicitly claim responsibility for the explosions. Japanese Prime Minister Fumio Kishida met with President Zelenskyy in Kyiv. In an effort to speed up delivery, the US government said it would supply Ukraine with older M1A1 Abrams tanks that have been upgraded so that they offer a "very similar capability to the M1A2" rather than the newer M1A2 tanks. In addition, the UK government also said it would supply Ukraine with depleted uranium shells.
After hypoglycemia in a person is identified, rapid treatment is necessary and can be life-saving. The main goal of treatment is to raise blood glucose back to normal levels, which is done through various ways of administering glucose, depending on the severity of the hypoglycemia, what is on-hand to treat, and who is administering the treatment. A general rule used by the American Diabetes Association is the "15-15 Rule," which suggests consuming or administering 15 grams of a carbohydrate, followed by a 15-minute wait and re-measurement of blood glucose level to assess if blood glucose has returned to normal levels.
=== Effects on physiological development === In general, androgens such as testosterone promote protein synthesis and thus growth of tissues with androgen receptors. Testosterone can be described as having anabolic and androgenic (virilising) effects, though these categorical descriptions are somewhat arbitrary, as there is a great deal of mutual overlap between them. The relative potency of these effects can depend on various factors and is a topic of ongoing research. Testosterone can either directly exert effects on target tissues or be metabolized by 5α-reductase into dihydrotestosterone (DHT) or aromatized to estradiol (E2). Both testosterone and DHT bind to an androgen receptor; however, DHT has a stronger binding affinity than testosterone and may have more androgenic effect in certain tissues at lower levels.
Sources: en.wikipedia.org
Cardarine is a common name for the investigational compound GW501516. It acts as a PPARδ agonist and is not approved for human use. It is prohibited in sport.
It activates PPARδ, a nuclear receptor that influences gene expression related to lipid and energy metabolism. Animal studies show changes in endurance and lipid levels. Human effects and risks are not well established.
No, cardarine is not a steroid. It belongs to a different chemical class, the PPARδ agonists. It is also not a selective androgen receptor modulator.
Yes, WADA prohibits cardarine as a PPARδ agonist. It appears on the prohibited list and can be detected in urine or blood. Athletes using it risk sanctions.