Nuclear receptor raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.
This page was last updated on 2025-09-16 and is reviewed periodically as new material appears.
Cardarine is a common name for GW501516, a synthetic compound first described in the 1990s as a selective agonist of the peroxisome proliferator-activated receptor delta. It was studied in preclinical models for metabolic and cardiovascular conditions, but it has not been approved as a medicine in the United States, Europe, or other major jurisdictions. Retail products labeled as cardarine are generally research chemicals or supplements, not pharmaceutical formulations. Because human safety and efficacy data remain limited, regulatory agencies treat it as an unapproved substance rather than a therapeutic product.
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.
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.
| Property | Value | Notes |
|---|---|---|
| IUPAC name | {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid | Systematic name for GW501516 |
| CAS Registry Number | 317318-70-0 | Unique identifier for the parent compound |
| Molecular formula | C21H18F3NO3S2 | Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur |
| Molecular weight | 453.5 g/mol | Approximate value for the neutral form |
| Appearance | White to off-white powder | Typical description for purified laboratory material |
Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.
GW501516 binds and activates PPARδ, a nuclear receptor that influences transcription of genes involved in fatty acid oxidation and energy use. Activation shifts some metabolic pathways in preclinical models, which is why the compound has been studied for lipid disorders and exercise-related endpoints. The exact downstream effects in humans are incompletely mapped. PPARδ is expressed in many tissues, including skeletal muscle, liver, and adipose tissue, so broad activation may have varied consequences. Researchers continue to examine how selective or partial activation might alter the balance between benefits and risks.
Published human data are sparse and mostly come from early-phase trials. Those studies examined short-term changes in lipids, glucose, and exercise capacity, but they were not large enough to establish efficacy or long-term safety. Some animal experiments reported increased running endurance, yet such findings do not prove a performance benefit in people. Anti-doping laboratories detect GW501516 and its metabolites in urine or blood using liquid chromatography-tandem mass spectrometry. Detection windows depend on dose, sample type, and individual metabolism. The method is sensitive enough to identify trace residues in tested samples.
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.
==== Sample preparation ==== In both conventional and in-situ dating, a thin section of the rock of interest is prepared. First, a thin layer of rock is cut by a diamond saw and ground to become optically flat. Then, it is mounted on a slide made of glass or resin, and ground smooth using abrasive grit. The final sample is usually only 30 μm thick.
Live fish: When live fish are transported they need oxygen, and the carbon dioxide and ammonia that result from respiration must not be allowed to build up. Most fish transported live are placed in water supersaturated with oxygen (though catfish can breathe air directly through their gills and body skin, and the climbing perch has special air-breathing organs). The fish are often "conditioned" (starved) before they are transported to reduce their metabolism and increase packing density, and the water can be cooled to further reduce metabolism. Live crustaceans can be packed in wet sawdust to keep the air humid. By air: Over five percent of the global fish production is transported by air. Air transport needs special care in preparation and handling and careful scheduling. Airline transport hubs often require cargo transfers under their own tight schedules. This can influence when the product is delivered, and consequently the condition it is in when it is delivered. The air shipment of leaking seafood packages causes corrosion damage to aircraft, and each year, in the US, requires millions of dollars to repair the damage. Most airlines prefer fish that is packed in dry ice or gel, and not packed in ice. By land or sea: "The most challenging aspect of fish transportation by sea or by road is the maintenance of the cold chain, for fresh, chilled and frozen products and the optimisation of the packing and stowage density. Maintaining the cold chain requires the use of insulated containers or transport vehicles and adequate quantities of coolants or mechanical refrigeration.
Further, during the first year of the COVID-19 pandemic, overdose disparities widened between Black persons and White persons. For example, in 2020, overdose rates among Black men 65 years or older (52.6 per 100 000) were nearly 7 times those of White men of the same age (7.7 per 100 000). During times of economic distress such as the COVID-19 pandemic or the 2008 recession, harmful rates of drug use has been seen to increase in populations experiencing joblessness and disadvantaged populations; moreover, Carpenter et al. found evidence that economic downturns lead to increases in the intensity of prescription pain reliever use as well as increases in clinically significant substance use disorders involving opioids. In addition, the COVID-19 pandemic has marked the start of health care policies that, should they be adopted permanently, could not only lessen the effects of the pandemic on overdoses, but also make overall treatment of opioid use disorder more effective by eliminating obstacles to previously proven therapies for these disorders. Other studies have looked at treatments for OUD during the COVID-19 pandemic. For example, one JAMA Internal Medicine research letter from December 2020 found that since the COVID-19 national emergency declaration, "the number of individuals filling buprenorphine prescriptions has plateaued but has not decreased; however, filled prescriptions for all medications collectively have decreased considerably."
==== Biotextile meshes ==== In the new paradigm of tissue engineering, professionals are trying to develop new textiles so that the body can form new tissue around these devices so it's not relying solely on synthetic foreign implanted material. Graduate student Jessica Gluck has demonstrated that viable and functioning liver cells can be grown on textile scaffolds.
Sources: en.wikipedia.org
Cannabis has been used in traditional medicine over centuries. Today, cannabis is subjected to medical research mostly concentrating on the cannabinoids THC and CBD. The cannabis varieties used for the production of the hemp juice such as cannabis sativa are high in CBD content. Hemp juice can also be added into crèmes and gels, and used as an eczema treatment.
==== 2019 ==== The lifespan of Caenorhabditis elegans (free-living nematodes) was increased by 5–6 times (by 400–500%) using simultaneous impact in IIS and TOR pathways. This is equivalent to how a human would live 400–500 years. The study was done by the MDI Biological Laboratory in collaboration with the Buck Institute for Research on Aging and Nanjing University. Scientists at the Mayo Clinic report the first successful use of senolytics, a new class of drug with potential anti-aging benefits, to remove senescent cells from human patients with a kidney disease. By combining doses of lithium, trametinib and rapamycin into a single treatment, researchers extend the lifespan of fruit flies (Drosophila) by 48%. Researchers at Harvard Medical School identify a link between neural activity and human longevity. Neural excitation is linked to shorter life, while suppression of overactivity appears to extend lifespan. Scientists at the Riken Center for Integrative Medical Sciences and Keio University use single-cell RNA analysis to find that supercentenarians have an excess of cytotoxic CD4 T-cells, a type of immune cell. This phenomenon was first demonstrated in mice
Ovalbumin is a storage protein in egg white (albumen). It is a serpin. Lactalbumin, or whey protein, is a protein fraction of milk. It is mainly Beta-lactoglobulin, although serum albumin also comprises a small part of it. Some plant seeds, including hemp, encode "2S albumins". These are named for their egg-like coagulation property.
=== Insulin access and innovation === In response to rising insulin costs and research showing that many people with diabetes are skipping or rationing their insulin, Breakthrough T1D has advocated for insurance companies to provide better health coverage for those living with type 1 diabetes, including making out-of-pocket costs for insulin and other vital diabetes tools more predictable and reasonable. The aim of this advocacy is to ensure people have the freedom to choose treatment strategies that are appropriate for them, and to cover artificial pancreas/automated insulin delivery systems. In response to escalating insulin affordability issues, Breakthrough T1D partnered with nonprofit drug maker Civica to manufacture insulin that will cost $30 a vial, regardless of a patient's insurance provider. Civica insulin is expected to be available to the public in 2025. Breakthrough T1D also advocates for passage of the INSULIN Act, which caps cost-sharing under private health insurance for a month's supply of selected insulin products at $35 or 25% of a plan's negotiated price (after any price concessions), whichever is less, beginning in 2025.
=== Classification === MSUD has five clinical phenotypes that are very distinct from one another. The most common and severe is the classical type with low residual activity from 0–2% of normal. Milder types include intermediate and intermittent with higher residual activities from 3–30% of the normal. Most unique is the thiamine-responsive type, where patients respond to high doses of thiamine administered, although this method is controversial. Lastly, the E-3 deficient type is correlated to combined enzyme deficiencies in pyruvate dehydrogenase, BCKD complexes, and alpha-ketoglutarate dehydrogenase, since E3 is common within mitochondrial alpha-ketoacid dehydrogenase complexes. NBS (newborn screening) detects most individuals with intermediate MSUD, but those who were not screened as newborns can be later diagnosed with MSUD. In these individuals, plasma BCAA concentrations are similar to those who have classic MSUD. However, they have better Lucine tolerance, and during acute metabolic decompensation episodes, they do not require intensive nutritional support. Severe metabolic intoxication with significant encephalopathy and leucinosis can occur if subjected to serious catabolic stress.
Sources: en.wikipedia.org
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.
It is prohibited by the World Anti-Doping Agency as a hormone and metabolic modulator. Athletes who test positive for GW501516 can face sanctions, including suspensions and loss of results.
Cardarine is a common or trade-style name, while GW501516 is the research code for the same chemical entity. Some sources also use Endurobol or GSK-516. The names refer to the same compound, not distinct drugs.
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.