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Identity And Pharmacological Classification — Complete Guide

By Editorial Desk · published 2025-11-30 · last reviewed 2026-01-03 · Topic

This is a working overview of Nuclear receptor, written for readers who want more than a one-paragraph summary but less than a textbook.

This page was last updated on 2026-01-03 and is reviewed periodically as new material appears.

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.

Identity and Regulatory Status

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.

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.

Background and Research Context

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.

In laboratory settings, cardarine is studied as a tool compound for probing PPARδ biology. Published experiments often use cell cultures, rodent models, or isolated tissues. Some investigations focus on metabolic effects, while others assess potential risks such as carcinogenicity observed in long-term animal studies. Because human trials are sparse, most knowledge comes from preclinical work and adverse event reports. Scientific literature frequently notes the gap between animal findings and human outcomes. The compound is not a dietary supplement and is not intended for human consumption.

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Cardarine Identity and Mechanism

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.

Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.

Background from the literature

Liquid–liquid extraction (also called 'solvent extraction' or 'partitioning') is a common method for extracting a substance from one liquid into another liquid at a different 'phase' (such as "slurry"). This method, which implements a countercurrent mechanism, is used in nuclear reprocessing, ore processing, the production of fine organic compounds, the processing of perfumes, the production of vegetable oils and biodiesel, and other industries. Gold can be separated from a cyanide solution with the Merrill–Crowe process using Counter Current Decantation (CCD). In some mines, nickel and cobalt are treated with CCD, after the original ore was treated with concentrated sulfuric acid and steam in titanium covered autoclaves, producing nickel cobalt slurry. The nickel and cobalt in the slurry are removed from it almost completely using a CCD system exchanging the cobalt and nickel with flash steam heated water.

Sioux Nation of Indians and was involved in the Black Hills Land Claim John Lowenthal (1947), lawyer and documentary filmmaker known for his defense of Alger Hiss Norman Dorsen (1950), professor at the New York University School of Law and former president of the American Civil Liberties Union Robert O. Harris (1951), labor lawyer and chairman of the National Mediation Board Norman Marcus (1953), New York City Planning Commission general counsel and zoning expert Richard H. Stern (1953), attorney and law professor David Braun (1954), music industry lawyer, former president of PolyGram Records Alvin Hellerstein (1954), US federal judge Isaac Shapiro (1954), head of international practice at Skadden, Arps, Slate, Meagher & Flom, former president of Japan Society Clarence Benjamin Jones (1956), attorney and advisor to Martin Luther King Jr. Jerome H. Kern (1957), founder of Wachtell, Lipton, Rosen & Katz, former CEO of Playboy and Colorado Symphony Bernard Nussbaum (1958), White House counsel under Bill Clinton Ezra G. Levin (1959), lawyer, co-chair of international law firm Kramer Levin Naftalis & Frankel David G. Trager (1959), judge on the United States District Court for the Eastern District of New York Robert Abrams (1960), Bronx borough president and New York state attorney general Frank Tuerkheimer (1960), Watergate prosecutor and former U.S. attorney for the Western District of Wisconsin José A. Cabranes (1961), judge of the U.S. Court of Appeals; first Puerto Rican to sit in a U.S. District Court; current trustee of Columbia University Michael B.

== Further reading == Bachner, Paul (2021). In further pursuit of excellence: the college of American pathologists 1946-2020 (PDF) (1st ed.). Northfield: College of American Pathologists. ISBN 978-1-941096-61-1.

Sources: en.wikipedia.org

Reference notes

The André E. Lalonde Accelerator Mass Spectrometry Laboratory is an accelerator mass spectrometry research facility at the University of Ottawa in Canada. It is currently the only facility of its type in Canada. It is named after former University of Ottawa Faculty of Science dean André E. Lalonde, who died in 2012.

== Chromosome and gene abnormalities == Most cases of MFS have tumor cells that contain complex chromosome and/or gene abnormalities including ring chromosomes (i.e. chromosome whose ends are fused together to form a ring), double minutes (i.e. small fragments of extrachromosomal DNA), chromosomes with deletions of part of their genetic material, and chromosome translocations (i.e. abnormal switches in genetic material between different chromosomes). There were no apparent differences in these abnormalities between lower grade and higher grade tumors but their numbers were higher and more prevalent in recurrent tumors. These forms of chromosome/gene cytogenetic alterations are commonly found in various tumor types regardless of their grade or severity. Tumor cell mutations or deletions in the NF1 gene occur ~10% of MFS cases while mutations in the CDKN2A/CDKN2B and amplifications in the CDK6, CCND1, and MDM2 genes occur in rare MFS cases. While the cells in many tumor types express specific chromosome/gene abnormalities that help in determining their diagnoses, the cited chromosome and gene abnormalities discovered in TBS tumor cells have not yet been found specific enough to be of help in diagnosing MFS. The chromosome/gene abnormalities have not yet been defined in the epithelioid variant of MFS.

The U.S. Department of Energy (DOE) has published a list of yearly technical system targets for on-board hydrogen storage for light-duty fuel cell vehicles which guide researchers in the field (5.5 wt %/40 g L−1 by 2017; 7.5 wt %/70 g L−1 ultimate). Materials with high porosity and high surface area such as MOFs have been designed and synthesized in an effort to meet these targets. These adsorptive materials generally work via physical adsorption rather than chemisorption due to the large HOMO–LUMO gap and low HOMO energy level of molecular hydrogen. A benchmark material to this end is MOF-177 which was found to store hydrogen at 7.5 wt % with a volumetric capacity of 32 g L−1 at 77 K and 70 bar. MOF-177 consists of [Zn4O]6+ clusters interconnected by 1,3,5-benzenetribenzoate organic linkers and has a measured BET surface area of 4630 m2 g−1. Another exemplary material is PCN-61 which exhibits a hydrogen uptake of 6.24 wt % and 42.5 g L−1 at 35 bar and 77 K and 2.25 wt % at atmospheric pressure. PCN-61 consists of [Cu2]4+ paddle-wheel units connected through 5,5′,5′′-benzene-1,3,5-triyltris(1-ethynyl-2-isophthalate) organic linkers and has a measured BET surface area of 3000 m2 g−1. Despite these promising MOF examples, the classes of synthetic porous materials with the highest performance for practical hydrogen storage are activated carbon and covalent organic frameworks (COFs).

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.

Is cardarine a SARM?

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.

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