GW501516 comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.
Last reviewed on 2025-09-23. Where a claim depends on a specific study, the study is described rather than over-claimed.
Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.
Cardarine is a common name for GW501516, an investigational compound developed in the 1990s for metabolic conditions. It acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in lipid and energy metabolism. The compound is frequently mislabeled as a selective androgen receptor modulator, or SARM, but its molecular target is different. GW501516 reached early clinical testing before development was discontinued. It has no approved therapeutic use in any country. The name cardarine is not a formal international nonproprietary name.
Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.
Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.
Anti-doping laboratories identify GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the usual matrix, and detection can occur after the parent compound has cleared from blood. The exact detection window depends on dose, formulation, individual metabolism, and assay sensitivity. Because the compound is prohibited at all times, athletes are subject to testing in and out of competition. Analytical methods continue to improve as new metabolites and designer analogs are characterized.
| Property | Value | Notes |
|---|---|---|
| Common synonyms | GW501516; GW-1516; endurobol | GW501516 is the research code |
| Drug class | PPARδ agonist | Not a selective androgen receptor modulator |
| Molecular formula | C21H18F3NO3S2 | Established chemical formula |
| Molar mass | 453.5 g/mol | Calculated from the formula |
| Regulatory status | Prohibited in sport; not approved as medicine | Status varies by country |
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 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.
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.
== Clinical significance == Guanine nucleotide synthesis is essential for maintaining normal cell function and growth, and is also important for the maintenance of cell proliferation and immune responses. IMPDH expression is found to be upregulated in some tumor tissues and cell lines. B and T lymphocytes display a dependence on IMPDH for normal activation and function, and demonstrate upregulated IMPDH expression. Therefore, IMPDH has been addressed as a drug target for immunosuppressive and cancer chemotherapy. Mycophenolate is an immunosuppressant that is used to prevent transplant rejection and acts through inhibition of IMPDH. Mycophenolate mofetil has been shown to inhibit completely both vaccinia and monkeypox viruses. Mutations in the Bateman domain of IMPDH1 are associated with the RP10 form of autosomal dominant retinitis pigmentosa and dominant Leber's congenital amaurosis.
=== Cell Selection & Expansion === IBA has developed an affinity chromatography system for non-magnetic isolation of peripheral blood mononuclear cells, T cells, B cells and other cells of interest. This technology is known as Fab-TACS (Traceless Affinity Cell Selection) and is based on Strep-tagged Fab fragments, which reversibly capture and release the target cells. This delivers label-free, non-activated cells suitable for immunologic or cell biological assays. The technology can be used with manual gravity flow columns as well as with the automated cell selection device FABian. Isolated and purified cells are being deployed for basic research as well as diagnostic applications. The Streptamers for cell expansion enable the controlled stimulation of T cells. They consist of non-magnetic soluble protein complexes generated by multimerization of αCD3- and αCD28 Fab-Streps with a Strep-Tactin multimer. The reversible reagents can be easily removed from the cells by the addition of biotin. This allows to regulate the extent of stimulation precisely and to study functional and label-free activated T cells.
This system is used in many unrelated animals: ants, bees, and wasps, termites, naked mole-rat, Damaraland mole-rat, Synalpheus regalis shrimp, certain beetles, some gall thrips and some aphids. Oxygenate blood came about in unrelated animals groups: vertebrates use iron (hemoglobin) and crustaceans and many mollusks use copper (hemocyanin). Biomineralization the secrete protective shells or carapaces made out of organically made hard materials like mineral carbonates and organic chitins came about in unrelated species all at the same time during the cambrian Explosion in: mollusks, brachiopods, arthropods, bryozoans, echinoderms, tube worms. Reef builders, a number of unrelated species of sea life build rocky like reefs: some types of bacteria make stromatolites, various sponges build skeletons of calcium carbonate, like: archaeocyath sponges, and stromatoporoid sponges, corals, some anthozoan cnidarians, bryozoans, calcareous algae and some bivalves (rudist bivalves). Magnetite for orientation, magnetically charged particles of magnetite for directional sensing have been found in unrelated species of salmon, rainbow trout, some butterflies and birds. Hydrothermal vent adaptations like the use of bacteria housed in body flesh or in special organs, to the point they no longer have mouth parts, have been found in unrelated hydrothermal vent species of mollusks and tube worms (like the giant tube worm). Lichens are partnerships of fungi and algae. Each "species" of lichen is make of different fungi and algae species, thus each has to come about independently.
== History == 4-HO-NiPT was first described in the scientific literature, as a metabolite of 4-AcO-DiPT, in 2022. Subsequently, its synthesis was described in 2023 and its pharmacology was reported in 2024. The drug was reported as a possible novel designer drug online in 2022.
Sources: en.wikipedia.org
Benefits to this method include that the person who is suspected of drug use does not need to be confronted or aware of testing. Only a very small amount of material is needed to obtain results, and can be used to test powder, pills, capsules, crystals, or organic material. There is also the ability to detect illicit material when mixed with other non-illicit materials. The tests are used for general screening purposes, offering a generic result for the presence of a wide range of drugs, including heroin, cocaine, methamphetamine, amphetamine, ecstasy/MDMA, methadone, ketamine, PCP, PMA, DMT, MDPV, and may detect rapidly evolving synthetic designer drugs. Separate tests for cannabis are also available. There are five primary color-test reagents used for general screening purposes. The Marquis reagent turns into a variety of colors when in the presence of different substances. Dille-Koppanyi reagent uses two chemical solutions which turns a violet-blue color in the presence of barbiturates. Duquenois-Levine reagent is a series of chemical solutions that turn to the color of purple when the vegetation of marijuana is added. Van Urk reagent turns blue-purple when in the presence of LSD. Scott test's chemical solution shows up as a faint blue for cocaine base. In recent years, the use of presumptive test kits in the criminal justice system has come under great scrutiny due to the lack to forensic studies, questioned reliability, rendering of false positives with legal substances, and wrongful arrests.
Edrophonium, formerly sold under the brand name Tensilon among others, is a readily reversible acetylcholinesterase inhibitor. It prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
=== Moondust: Knuckles Tech Demos === Moondust: Knuckles Tech Demos is a tech demo created for the Valve Index controllers which is set in the Portal universe. The game was released on Steam on June 21, 2018, however it is unlisted.
Sources: en.wikipedia.org
No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.
No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.
Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.
It binds to and activates PPAR delta, a nuclear receptor that controls expression of genes related to fatty acid oxidation. This mechanism can alter energy metabolism in animal models. It is not a direct stimulant or fat-burning enzyme.