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Identity And Pharmacological Classification — Practical Notes

By Editorial Desk · published 2025-09-24 · last reviewed 2025-10-31 · 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.

Last reviewed on 2025-10-31. Where a claim depends on a specific study, the study is described rather than over-claimed.

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.

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.

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.

Laboratory detection of GW501516 commonly uses liquid chromatography coupled with tandem mass spectrometry. The method can identify the parent compound or its metabolites in urine and blood after sample cleanup. Protein precipitation, solid-phase extraction, or enzymatic hydrolysis may precede analysis, depending on the matrix. Reference standards are required for accurate quantification and confirmation. Because the compound is not approved, testing often occurs in anti-doping, forensic, or research settings rather than routine clinical care. Results are reported with limits of detection and quantification.

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 Regulatory Status

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.

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.

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Mechanism and Safety Research

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.

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.

Supporting material

In 1972, Sweden introduced a law that made it possible to change a person's legal gender, but in order to do that, transgender individuals were required to be sterilized and were not allowed to save any sperm or eggs. Apart from this, there were no other mandatory surgeries required for legal gender change. In 1999, people who had been forcibly sterilized in Sweden were entitled to compensation. However, the sterilization requirement remained for people who changed their legal gender. In January 2013, forced sterilization was banned in Sweden. Depending on the person's health and wishes there are several different treatments and surgeries available. Today, no form of treatment is mandatory. Although to access medical and legal transitional treatment (e.g. hormone replacement therapy, and top surgery to enhance or remove breast tissue), the person will need to be diagnosed with transexualism or gender dysphoria, which requires at least one year of therapy, during which they must live for one full year as their desired gender in all professional, social, and personal matters. Gender clinics are recommended to provide male-to-female patients with wigs and breast prostheses for the endeavor. The evaluation additionally involves, if possible, meetings with family members and/or other individuals close to the patient. Patients may be denied care for any number of "psychosocial dimensions", including their choice of job or their marital status.

== Departments == Division of Basic Medical Sciences I Department of Biochemistry Department of General Biology Department of Medical Physics Division of Basic Medical Sciences II Department of Anatomy Department of General Pharmacology Department of Physiology Division of Clinical Laboratories Department of Microbiology Department of Nuclear Medicine Department of Pathology Department of Public Health Department of Radiology Division of Internal Medicine Ι Department of Internal Medicine Division of Paediatrics & Obstetrics – Gynaecology Department of Obstetrics - Gynecology Department of Paediatric Surgery Department of Paediatrics Division of Surgery Department of Anaesthesiology and Intensive Care Department of Cardiothoracic Surgery Department of Neurosurgery Department of Ophthalmology Department of Orthopaedics Department of Otorhinolaryngology Department of Surgery Department of Urology Department of Vascular Surgery

An oligopeptide (oligo-, "a few"), is a peptide consisting of two to twenty amino acids, including dipeptides, tripeptides, tetrapeptides, and other polypeptides. Some of the major classes of naturally occurring oligopeptides include aeruginosins, cyanopeptolins, microcystins, microviridins, microginins, anabaenopeptins, and cyclamides. Microcystins are best studied because of their potential toxicity impact in drinking water. A review of some oligopeptides found that the largest class are the cyanopeptolins (40.1%), followed by microcystins (13.4%).

In the context of these functional rearrangements, these tertiary or quaternary structures are usually referred to as "conformations", and transitions between them are called conformational changes. Such changes are often induced by the binding of a substrate molecule to an enzyme's active site, or the physical region of the protein that participates in chemical catalysis. In solution, protein structures vary because of thermal vibration and collisions with other molecules.

Sources: en.wikipedia.org

Supporting material

EC 7.1.1 Hydron translocation or charge separation linked to oxidoreductase reactions EC 7.1.2 Hydron translocation linked to the hydrolysis of a nucleoside triphosphate EC 7.1.3 Hydron translocation linked to the hydrolysis of diphosphate An important translocase contained in this group is ATP synthase, also known as EC 7.1.2.2.

== Dosage regimen == The dosage in patients without severe renal impairment is 50 μg/kg subcutaneously once a day either abdominal, in thigh, or hip. Most patients will be able to self-administer the drug after appropriate training. Patients with severe renal impairment should receive only 25 μg/kg daily. The first dose should be given 6 to 24 hours after completion of chemotherapy. Dosing should be continued until platelet counts reach at least 50,000 cells. Usually, one course of Neumega encompasses 10 to 21 days. The drug should be discontinued at least 2 days before starting the next chemotherapy cycle.

Another case was that of Ismil bin Kadar, who was initially sentenced to death for a 2005 robbery-murder case in Boon Lay, but eventually acquitted of the crime as the Court of Appeal found that based on the evidence, Ismil was not involved in the case and that it was solely his younger brother Muhammad bin Kadar who was responsible for the robbery and murder; Muhammad was subsequently executed in April 2015. Successful clemency applications are thought to be even rarer. Since 1965, the presidential clemency has been granted seven times to death row inmates, whose sentences were all commuted to life imprisonment (not counting the clemency pleas of the underaged offenders serving TPP). The most recent case was in August 2025, when convicted drug trafficker Tristan Tan Yi Rui was granted clemency by President Tharman Shanmugaratnam, who commuted Tan's death sentence to life imprisonment. Prior to Tan's pardon, the last presidential clemency to be granted was in April 1998, when President Ong Teng Cheong pardoned a 19-year-old death row inmate and convicted murderer Mathavakannan Kalimuthu, commuting his death sentence to life imprisonment. Previously, other than the Court of Appeal, offenders were allowed to file criminal or civil appeals to the Privy Council in London, where the judges could hear their appeals once they exhausted all avenues of appeal in Singapore. This avenue of appeal was fully abolished for all criminal and civil matters in April 1994. One case in which an appeal to the Privy Council was successful was the case of murderer Mohamed Yasin bin Hussin.

=== Male === For males, erogenous zones consist of the glans and the penis itself, along with the scrotum, the perineum, and the anus. Males may also experience sexual stimulation via the prostate, either from anal sex or massage. The prostate gland may be stimulated from inside the rectum, such as by anal sex, or by applying pressure on the base of the perineum near the anus. Men who report the sensation of prostate stimulation often give descriptions similar to females' accounts of G-spot stimulation.

The three substrates of this enzyme are 4-hydroxybenzaldehyde, oxidised nicotinamide adenine dinucleotide (NAD+), and water. Its products are 4-hydroxybenzoic acid, reduced NADH, and a proton. This enzyme belongs to the family of oxidoreductases, specifically those acting on the aldehyde or oxo group of donor with NAD+ or NADP+ as acceptor. The systematic name of this enzyme class is 3-hydroxybenzaldehyde:NAD+ oxidoreductase. This enzyme is also called p-hydroxybenzaldehyde dehydrogenase. This enzyme participates in toluene and xylene degradation in bacteria. It is also found in carrots (Daucus carota).

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.

How is cardarine measured in biological samples?

LC-MS/MS is common, often after sample cleanup. The assay targets GW501516 or its metabolites.

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