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Identity And Pharmacological Classification — Hands-On Walkthrough

By Editorial Desk · published 2026-01-22 · last reviewed 2026-02-28 · Faq

The short version of Nuclear receptor fits in a sentence. The long version — which is the one that helps — is below.

Reviewed 2026-02-28. Anything still debated is marked as such rather than presented as settled.

Identity and Pharmacological Classification

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 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.

Identity and Pharmacological Mechanism

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.

Cardarine at a glance

PropertyValueNotes
Chemical classPPARδ agonistNot an anabolic steroid.
Common synonymsGW501516, GW-1516Cardarine is an informal name.
AppearanceWhite to off-white powderTypical for research-grade solid.
Solubility classPoorly soluble in water; soluble in some organic solventsSuch as DMSO or ethanol in laboratory settings.
Typical storage temperatureCool, dry, protected from lightSpecific conditions vary by supplier and form.

Mechanism and Laboratory Detection

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.

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.

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Detection, Stability, and Quality

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 as Investigational PPARδ Agonist

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.

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.

Background from the literature

About 95% of the depleted uranium produced until now is stored as uranium hexafluoride, or (D)UF6, in steel cylinders in open air storage yards close to enrichment plants. Each cylinder typically holds up to 12.7 tonnes (14.0 short tons) of UF6. In the U.S. 560,000 tonnes (620,000 short tons) of depleted UF6 had accumulated by 1993. In 2008, 686,500 tonnes (756,700 short tons) in 57,122 storage cylinders were located near Portsmouth, Ohio; Oak Ridge, Tennessee; and Paducah, Kentucky. The storage of (D)UF6 presents environmental, health, and safety risks because of its chemical instability. When UF6 is exposed to water vapor in the air, it reacts with the moisture to produce UO2F2 (uranyl fluoride), a solid, and HF (hydrogen fluoride), a gas, both of which are highly soluble and toxic. The uranyl fluoride solid acts to plug the leak, limiting further escape of depleted UF6. Release of the hydrogen fluoride gas to the atmosphere is also slowed by the plug formation. Like any other uranium compound, uranyl fluoride is radioactive, and precautions should be taken. Whether ingested, inhaled, or absorbed through the skin, it is corrosive and may harm internal organs, potentially resulting in death. Effects of exposure may be delayed. The U.S. government has been converting depleted UF6 to solid uranium oxides for use or disposal. Such disposal of the entire DUF6 inventory could cost anywhere from US$15 million to US$450 million.

Sulfonylureas bind to and close ATP-sensitive K+ (KATP) channels on the cell membrane of pancreatic beta cells, which depolarizes the cell by preventing potassium from exiting. This depolarization opens voltage-gated Ca2+ channels. The rise in intracellular calcium leads to increased fusion of insulin granules with the cell membrane, and therefore increased secretion of mature insulin. There is some evidence that sulfonylureas also sensitize β-cells to glucose, that they limit glucose production in the liver, that they decrease lipolysis (breakdown and release of fatty acids by adipose tissue) and decrease clearance of insulin by the liver. The KATP channel is an octameric complex of the inward-rectifier potassium ion channel Kir6.x and sulfonylurea receptor SUR which associate with a stoichiometry of 4:4. Furthermore, it has been shown that sulfonylureas interact with the nucleotide exchange factor Epac2. Mice lacking this factor exhibited a decreased glucose-lowering effect upon sulfonylurea treatment.

Hemolymph or haemolymph is a body fluid that circulates inside arthropod bodies transporting nutrients and oxygen to tissues, comparable to blood in vertebrates. It is composed of a plasma in which circulating immune cells called hemocytes are dispersed in addition to many plasma proteins (hemoproteins) and dissolved chemicals. It is the key component of the open circulatory system characteristic of arthropods such as insects, arachnids, myriapods and crustaceans. Some non-arthropod invertebrates such as molluscs and annelids also possess a similar hemolymphatic circulatory system. In insects, the largest arthropod clade, the hemolymph mainly carries nutrients but not oxygen, which is supplied to the tissues separately by direct deep ventilation through an extensive tracheal system. In other arthropods, oxygen is dissolved into the hemolymph from gills, book lungs or across the cuticle and then distributed to the body tissues via the hemocoel.

Sources: en.wikipedia.org

Reference notes

– the particles are not coated or surface modified. In July 2025, the Scientific Committee on Consumer Safety (SCCS) adopted its fourth opinion (Submission IV), concluding that nano‑hydroxyapatite is safe at concentrations up to 29.5% in toothpaste and up to 10% in mouthwash, under defined particle morphology constraints.

Roeder and Robert Tjian, for their outstanding work on eukaryotic transcription regulation 1993 James E. Rothman and Randy Schekman, for determining the components of the secretory pathway 1992 Paul Nurse and Leland H. Hartwell, for establishing the details of the control of eukaryotic cell cycle 1991 David Botstein, Raymond L. White and Ronald W. Davis, for creating the methods by which variations in the human genome can be detected and analyzed 1990 Richard Henderson and Peter Nigel Tripp Unwin, for determining the first structure of an integral membrane protein 1989 Christiane Nüsslein-Volhard and Edward B. Lewis, for pioneering studies of eukaryotic development 1988 Sidney Altman and Thomas R. Cech, for discovering RNA catalysis 1987 Shinya Inoué, for his innovations in light microscopy 1986 Harland G. Wood, for his outstanding work on enzyme function 1985 Seymour Benzer and Sydney Brenner, for founding modern eukaryotic genetics 1984 Donald D. Brown and Robert L. Letsinger, for their seminal work on development 1983 Eric R. Kandel and Daniel E. Koshland, Jr., for pioneering contributions to sensory transduction 1982 Keith R. Porter and Alexander Rich 1981 Stanley Cohen, Rita Levi-Montalcini and Gordon H. Sato 1980 Elias J. Corey, Bengt I. Samuelsson and Frank H. Westheimer 1979 Howard Green and Beatrice Mintz 1978 César Milstein 1977 Barbara McClintock 1976 Peter D. Mitchell 1975 Bruce Ames, James A. Miller and Elizabeth C. Miller 1974 Arthur B. Pardee and H. Edwin Umbarger 1973 H. Ronald Kaback and Saul Roseman 1972 Boris Ephrussi 1971 David H. Hubel and Torsten N.

Diethylaminoethyl cellulose (DEAE-C) is a positively charged resin used in ion-exchange chromatography, a type of column chromatography, for the separation and purification of proteins and nucleic acids. Gel matrix beads are derivatized with diethylaminoethanol (DEAE) and lock negatively charged proteins or nucleic acids into the matrix. The proteins are released from the resin by increasing the salt concentration of the solvent or changing the pH of the solution as to change the charge on the protein.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine also known as?

Cardarine is commonly known as GW501516 or GW-1516. These names refer to the same synthetic compound. It is not a brand-name approved medicine.

Is cardarine a steroid?

No, cardarine is not a steroid. It is classified as a PPARδ agonist. Its structure and receptor target differ from anabolic steroids.

Has cardarine been approved for human use?

No regulatory agency has approved cardarine as a medicine. It was investigated in early research but development was discontinued. It is not available as a prescription drug.

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.

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