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Identity And Pharmacological Classification — 2026 Update

By Editorial Desk · published 2026-03-16 · last reviewed 2026-04-17 · Topic

If you have been reading about Nuclear receptor 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.

Updated 2026-04-17. Numbers and descriptions here follow the published literature rather than marketing material.

Identity and Pharmacological Classification

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.

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.

Mechanism and Safety Research

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 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 Detection

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

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.

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Detection, Regulation, and Quality Context

Regulatory treatment of cardarine differs by context and jurisdiction. In competitive sport, the World Anti-Doping Agency lists PPARδ agonists, including GW501516, as prohibited at all times. Outside sport, it lacks approval as a prescription medicine in major drug markets, and products sold for human consumption may be treated as unapproved drugs. Some countries also restrict importation or sale through general consumer protection and medicines laws. These classifications affect availability, testing, and legal risk without establishing therapeutic value.

Because cardarine is not an approved medicine, no pharmacopeial monograph defines its identity, purity, or storage requirements. Laboratories typically rely on in-house methods and reference standards when testing materials labeled as GW501516. Certificates of analysis may report purity and identity for a specific batch, but their scope varies and they do not guarantee safety or legal status. Independent verification can include high-performance liquid chromatography, mass spectrometry, nuclear magnetic resonance, and elemental analysis. The distinction between research chemical labeling and human use is significant because quality standards and oversight differ.

Background and Regulatory History

Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.

Cardarine is a common name for the investigational chemical GW501516, also written GW-1516. It was developed as a peroxisome proliferator-activated receptor delta agonist for metabolic conditions such as dyslipidemia. Early research focused on lipid handling and energy use in skeletal muscle and other tissues. The compound was never approved as a medicine. In public discussion, it is often grouped with performance-enhancing substances, although its receptor target differs from that of anabolic steroids or selective androgen receptor modulators. Regulatory and health authorities have issued warnings about its use.

GW501516 acts on PPARδ, a nuclear receptor that helps regulate fatty acid oxidation and energy homeostasis. In animal studies, activation of this receptor was associated with increased endurance and changes in lipid metabolism. Human trials examined effects on blood lipids and other metabolic markers, but the compound did not advance to approval. Rodent studies later reported tumors in multiple tissues at doses used in those experiments. Whether those findings translate to human risk remains uncertain, and the clinical relevance of the animal data is still debated.

Cardarine Identity and Mechanism

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.

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.

Further detail

== Major families == The barrier for a regular protein to become a selenoprotein is relatively high due to the requirement for a SECIS element. As a result, new selenoprotein families do not easily appear. It is also not uncommon for these families to include non-selenoprotein descendants, as (mainly terristial) selenium-poor environments provide a fitness advantage to an organism that has lower requirements of selenium. The below will focus on families found in humans.

The international drug control conventions, also known as the United Nations drug control conventions, are three related, non self-executing treaties that establish an international legal framework for drug control. They serve to maintain a classification system of controlled substances including psychoactive drugs and precursors, to ensure the regulated supply of those substances useful for medical and scientific purposes, and to prevent other uses. Ratification is near universal among UN member countries. The treaties are the Single Convention on Narcotic Drugs (1961; amended in 1972), the Convention on Psychotropic Substances (1971), and the UN Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances (1988). There are also other minor treaties addressing drugs, such as the Convention on the Rights of the Child or the UN Convention on the Law of the Sea.

== Catabolic reaction: How do CDPSs synthesize cyclodipeptides? == It was firstly thought that nonribosomal peptide synthetases (NRPSs) were the responsible ones of CDPs construction, either through specific biosynthetic pathways or with the premature liberation of dipeptidyl intermediates meanwhile the elongation process was done. On account of AlbC discovery, an enzyme with the ability to specifically create CDP using loaded ARNt as substrates, it was disclosed that there was a second route for the cyclodipeptide production. CDPSs' catalytic cycle begins with the binding of the first aa-tRNA, with its aminoacyl transferred onto a conserved serine residue to form an aminoacyl-enzyme intermediate. The second aa-tRNA interacts with this intermediate so that its aminoacyl is transferred to the aminoacyl-enzyme to form a dipeptidyl-enzyme intermediate. Finally, the dipeptidyl goes through an intramolecular cyclization leading to the final cyclodipeptide.

Sources: en.wikipedia.org

Background from the literature

The debate over AI developers training models on copyrighted material without consent is highly contentious in the UK. In 2024, the government proposed a broad text and data mining (TDM) exception allowing AI companies to use publicly available copyrighted material. This faced intense opposition from the creative sector. In March 2026, the House of Lords Communications and Digital Committee concluded that generative AI poses a "clear and present danger" to the creative industries. Trade unions campaigned against the proposals, leading the government to abandon the "opt-out" model. The government acknowledged the need to build an evidence base before reforming copyright law.

Oxandrolone has been used illicitly by bodybuilders and athletes for its muscle-building effects as a doping agent in sports. Cases of doping with oxandrolone by professional athletes have been reported. Because it is more anabolic than androgenic, women and those seeking less intense steroid regimens used it particularly often. In the past many valued oxandrolone's supposed low hepatotoxicity relative to most other orally active AASs.

This approach enabled Swedish physicist Sven Nilsson et al., as well as other groups, to make the first detailed calculations of the stability of nuclei within the island. With the emergence of this model, Strutinsky, Nilsson, and other groups argued for the existence of the doubly magic nuclide 298114Fl (Z = 114, N = 184), rather than 310Ubh (Z = 126, N = 184) which was predicted to be doubly magic as early as 1957. Subsequently, estimates of the proton magic number have ranged from 114 to 126, and there is still no consensus.

Sources: en.wikipedia.org

Reference notes

Two major principalities survived east of the Weser after the Napoleonic Wars: the Kingdom of Hanover and the Duchy of Brunswick (after 1866 Hanover became a Prussian province; after 1919 Brunswick became a free state). Historically a close tie existed between the royal house of Hanover (Electorate of Hanover) and the United Kingdom of Great Britain and Ireland as a result of their personal union in the 18th century (the personal union was dissolved when Victoria became the Queen of the United Kingdom in 1837 because Hanover did not allow female rulers). West of the River Hunte a "de-Westphalianising process" began in 1815. After the Congress of Vienna the territories of the later administrative regions (Regierungsbezirke) of Osnabrück and Aurich transferred to the Kingdom of Hanover. The Grand Duchy of Oldenburg and the Principality of Schaumburg-Lippe retained state autonomy. Nevertheless, the entire Weser-Ems region (including the city of Bremen) were grouped in 1920 into a Lower Saxon Constituency Association (Wahlkreisverband IX (Niedersachsen)). This indicates that at that time the western administrations of the Prussian Province of Hanover and the state of Oldenburg were perceived as being "Lower Saxon". The forerunners of today's state of Lower Saxony were lands that were geographically and, to some extent, institutionally interrelated from very early on.

An update to Two Point Hospital (2020) on Steam added a patient suffering from a Headcrab attack, while the Steam release of Super Meat Boy featured a playable Headcrab. The Headcrab has received multiple pieces of merchandise, including a 1/4 scale Headcrab Zombie and a plush.

Pitolisant is an inverse agonist (antagonist) of the histamine H3 autoreceptor. As such, pitolisant is an antihistamine medication that also belongs to the class of CNS stimulants. Pitolisant is also considered a medication of eugeroic class, which means that it promotes wakefulness and alertness. Pitolisant is the first wakefulness-promoting agent that acts by blocking the H3 autoreceptor. Pitolisant has been shown to be effective and well-tolerated for the treatment of narcolepsy with or without cataplexy. Pitolisant is the only non-controlled anti-narcoleptic drug in the United States. It has shown minimal abuse risk in studies. Blocking the histamine H3 autoreceptor increases the activity of histamine neurons in the brain. The H3 autoreceptors regulate histaminergic activity in the central nervous system (and to a lesser extent, the peripheral nervous system) by inhibiting histamine biosynthesis and release upon binding to endogenous histamine. By preventing the binding of endogenous histamine at the H3, as well as producing a response opposite to that of endogenous histamine at the receptor (inverse agonism), pitolisant enhances histaminergic activity in the brain.

== Later life == Dayhoff's Atlas became a template for many indispensable tools in large portions of DNA or protein-related biomedical research. In spite of this significant contribution, Dayhoff was marginalized by the community of sequencers. The contract to manage GenBank (a technology directly related to her research), awarded in 1983 by the NIH, went to Walter Goad at the Los Alamos National Laboratory. The reason for this attitude was unknown, with theories ranging from sexism to a clash of values with the experimental science community. Despite the success of Dayhoff's Atlas, experimental scientists and researchers considered their sequence information very valuable and were often reluctant to submit it to such a publicly available database. During the last few years of her life, she focused on obtaining stable, adequate, long-term funding to support the maintenance and further development of her Protein Information Resource. She envisioned an online system of computer programs and databases, accessible by scientists all over the world, for identifying protein from sequence or amino acid composition data, for making predictions based on sequences, and for browsing the known information. Less than a week before she died, she submitted a proposal to the Division of Research Resources at NIH for a Protein Identification Resource. After her death, her colleagues worked to make her vision a reality, and the protein database was fully operational by the middle of 1984.

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 the main molecular target of cardarine?

It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.

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