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Identity And Regulatory Status — Worked Examples

By Editorial Desk · published 2025-07-29 · last reviewed 2025-09-03 · Wiki

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

This page was last updated on 2025-09-03 and is reviewed periodically as new material appears.

Identity and Regulatory Status

Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.

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.

Regulation and Analytical Detection

Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.

Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.

Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516; GW-1516; endurobolGW501516 is the research code
Drug classPPARδ agonistNot a selective androgen receptor modulator
Molecular formulaC21H18F3NO3S2Established chemical formula
Molar mass453.5 g/molCalculated from the formula
Regulatory statusProhibited in sport; not approved as medicineStatus varies by country

Identity and Pharmacological Mechanism

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 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.

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Mechanism and Detection Methods

Handling and quality assessment of cardarine reference material follow general laboratory practices for poorly characterized compounds. It typically appears as a white to off-white powder and is sparingly soluble in water but soluble in organic solvents such as dimethyl sulfoxide and ethanol. Storage recommendations usually specify a cool, dry, dark place, with long-term storage at low temperature and desiccation. Purity may be checked by high-performance liquid chromatography with ultraviolet detection, while identity is confirmed by mass spectrometry and nuclear magnetic resonance. No pharmacopeial monograph exists, so reported purity and stability depend on the supplier’s methods.

GW501516 acts as a selective agonist at PPARδ, a nuclear receptor that regulates transcription of genes involved in lipid handling and energy metabolism. Activation of PPARδ in preclinical models increases fatty acid oxidation, mitochondrial biogenesis, and exercise endurance in rodents. These effects have made the compound a subject of metabolic research and also a target for sport anti-doping rules. In humans, however, controlled studies are limited, and whether similar endurance or metabolic changes occur at tolerated exposures remains an open question. The receptor’s broad tissue distribution also means downstream effects may vary by organ and condition.

Detection of GW501516 in biological samples generally relies on liquid chromatography coupled with tandem mass spectrometry. Urine is a common matrix in anti-doping analysis, while blood or plasma may be used in research settings. Sample preparation can involve enzymatic hydrolysis, protein precipitation, or solid-phase extraction before instrumental analysis. Because the compound undergoes metabolism, assays may target the parent molecule, one or more metabolites, or both. Detection windows are not fixed; they depend on factors such as dose, route, individual metabolism, and assay sensitivity. Reference standards are required for accurate identification and quantification.

Detection, Regulation, and Quality Context

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.

Cardarine can be detected in biological samples and product materials using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The method separates compounds by chromatography and identifies them by mass-to-charge transitions, allowing low-level detection in urine or blood. Sample preparation often involves enzymatic hydrolysis, solid-phase extraction, or protein precipitation. Certified reference materials and isotope-labeled internal standards improve quantification. Detection windows depend on metabolism, matrix, and assay sensitivity, so no single universal window applies.

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.

Notes from published material

Organoselenium chemistry is the science exploring the properties and reactivity of organoselenium compounds, chemical compounds containing carbon-to-selenium chemical bonds. Selenium belongs with oxygen and sulfur to the group 16 elements or chalcogens, and similarities in chemistry are to be expected. Organoselenium compounds are found at trace levels in ambient waters, soils and sediments. Selenium can exist with oxidation state −2, +2, +4, +6. Se(II) is the dominant form in organoselenium chemistry. Down the group 16 column, the bond strength becomes increasingly weaker (234 kJ/mol for the C−Se bond and 272 kJ/mol for the C−S bond) and the bond lengths longer (C−Se 198 pm, C−S 181 pm and C−O 141 pm). Consistent with the inertness of large-n s orbitals, dicoordinate selenium compounds have a bond angle of nearly 90°. Selenium compounds are more nucleophilic than the corresponding sulfur compounds and also more acidic. The pKa values of XH2 are 16 for oxygen, 7 for sulfur and 3.8 for selenium. In contrast to sulfoxides, the corresponding selenoxides are unstable in the presence of β-protons and this property is utilized in many organic reactions of selenium, notably in selenoxide oxidations and in selenoxide eliminations. The first organoselenium compound to be isolated was diethyl selenide in 1836.

=== Regier et al. (2010) === A 2010 study of nuclear genomes (Regier et al.) strongly supports Pancrustacea and strongly favour Mandibulata (Myriapoda + Pancrustacea) over Paradoxopoda (Myriapoda + Chelicerata). According to this study, Pancrustacea is divided into four lineages: Oligostraca (Ostracoda, Mystacocarida, Branchiura, Pentastomida), Vericrustacea (Malacostraca, Thecostraca, Copepoda, Branchiopoda), Xenocarida (Cephalocarida, Remipedia) and Hexapoda, with Xenocarida as a sister group to the Hexapoda (comprising "Miracrustacea"). New clades proposed by Regier et al. are:

However, there have also been pleas to take a more nuanced approach to judging the distribution skewness of the impact factor. Ludo Waltman and Vincent Antonio Traag, in their 2021 paper, ran numerous simulations and concluded that "statistical objections against the use of the IF at the level of individual articles are not convincing", and that "the IF may be a more accurate indicator of the value of an article than the number of citations of the article".

Estradiol has been studied and used by intranasal administration. It was available as a cyclodextrin-containing nasal spray under the brand name Aerodiol in some countries, although this specific product was discontinued in 2007. The product was administered once per day as one 150-μg spray in each nostril (300 μg/day total). Intranasal estradiol has pharmacokinetics similar to those of sublingual and intravenous administration of estradiol, including a sharp peak and then rapid decline in estradiol levels. Despite the relatively short duration of intranasal estradiol, it has similar effectiveness to other, longer-lasting routes of administration in terms of relief of menopausal symptoms like hot flashes.

There are no FDA-approved Health Claims or Qualified Health Claims for vitamin B6. Structure/Function Claims can be made without FDA review or approval as long as there is some credible supporting science. Examples for this vitamin are "Helps support nervous system function" and "Supports healthy homocysteine metabolism."

Sources: en.wikipedia.org

Background from the literature

Wilhelm Wien demonstrates that canal rays can be deflected using strong electric and magnetic fields. He shows that the mass-to-charge ratio of the particles have opposite polarity and is much larger compared to the electron. He also realizes that the particle mass is similar to that of the hydrogen particle. 1898 J. J. Thomson measures the mass-to-charge ratio of electrons.

Carbon dioxide is colorless. At low concentrations, the gas is odorless; however, at sufficiently high concentrations, it has a sharp, acidic odor. At standard temperature and pressure, the density of carbon dioxide is around 1.98 kg/m3, about 1.53 times that of air. Carbon dioxide has no liquid state at pressures below 0.51795(10) MPa (5.11177(99) atm). At a pressure of 1 atm (0.101325 MPa), the gas deposits directly to a solid at temperatures below 194.6855(30) K (−78.4645(30) °C) and the solid sublimes directly to a gas above this temperature. In its solid state, carbon dioxide is commonly called dry ice.

Control is a standard against which experimental observations may be evaluated. In clinical trials, one group of participants is given an experimental drug, while another group (i.e., the control group) is given either a standard treatment for the disease or a placebo. (NLM) Coordinating Committee

=== Prosecution === In his opening statement, prosecutor Brian Leveson portrayed the Wests as sadistic sex-obsessed murderers, terming the bodies discovered at Cromwell Street and Midland Road "secrets more terrible than words can express ... [The victims'] last moments on earth were as objects of the sexual depravity of this woman and her husband." He pointed out that Fred had been incarcerated when Charmaine was killed, claimed that Fred and Rose had each learned from their mistake in allowing Owens to live, and said that the gag on victim Thérèse Siegenthaler evinced a "feminine" touch‍—‌a scarf tied in a bow. Leveson promised to demonstrate Rose's controlling and sexually sadistic character, as well as her efforts to deflect suspicion about the disappearance of their victims. Prosecution witnesses included Cromwell Street lodgers, victims' relatives, Rose's mother, Daisy, and sister, Glenys, and surviving victims including Kathryn Halliday (a former lover of Fred and Rose), Owens, Anne Marie and a "Miss A" (who had been sexually assaulted at age 14 by Fred and Rose in 1977 and who described Rose as the more aggressive perpetrator of the two). Neighbours described Charmaine's 1971 disappearance while Fred was imprisoned and Rose's casual indifference to Heather's disappearance. Rose's counsel, Dick Ferguson, tried to discredit prosecution witnesses as either having financially exploited their connection to the case or being motivated by grudges.

=== Discussed health risks === Like other foods, the consumption of edible insects could present health risks stemming from biological, toxicological, and allergenic hazards. Biological hazards include bacteria, viruses, protozoa, fungi and mycotoxins; toxological risks are poisons, pesticides, heavy metals and antinutrients; allergenic hazards relate to arginine kinase, tropomyosin and α-Amylase. Additionally, recent studies have indicated that proteins from yellow mealworm (Tenebrio molitor) may act as allergens, potentially triggering immunoglobulin E (IgE)-mediated allergic reactions and cross-reactivity, especially in individuals already sensitized to crustaceans or other arthropods. Chitin, a component of insect exoskeletons and other body parts, induces cytokine production in the digestive systems of humans and other mammals. Enzymes break the chitin down into smaller fragments, which trigger an immune response that results in inflammatory and allergic reactions. The human immune response to chitin is thought to be related to the abundance of dust mites as a cause of airway inflammatory disease and parasites as a cause of numerous diseases. In general, insects harvested from the wild pose a greater risk than farmed insects, and insects consumed raw pose a greater risk than insects that are cooked before consumption. Feed substrate and growing conditions are the main factors influencing the microbiological and chemical hazards of farmed insects.

Sources: en.wikipedia.org

Further detail

autozygote A cell or organism that is homozygous for a locus at which the two homologous alleles are identical by descent, both having been derived from a single gene in a common ancestor. Contrast allozygote.

In 1976, economist Rudolf Meidner established a study committee that came up with a proposal called the Meidner Plan which entailed the transferring of the excess profits into investment funds controlled by the workers in said efficient firms, with the goal that firms would create further employment and pay workers higher wages in return rather than unduly increasing the wealth of company owners and managers. Capitalists immediately denounced the proposal as socialism and launched an unprecedented opposition and smear campaign against it, threatening to terminate the class compromise established in the 1938 Saltsjöbaden Agreement.

Independently from Ibn al-Nafis, Michael Servetus rediscovered the pulmonary circulation, but this discovery did not reach the public because it was written down for the first time in the "Manuscript of Paris" in 1546, and later published in the theological work for which he paid with his life in 1553. Later this was described by Renaldus Columbus and Andrea Cesalpino. Herman Boerhaave is sometimes referred to as a "father of physiology" due to his exemplary teaching in Leiden and textbook 'Institutiones medicae' (1708). Pierre Fauchard has been called "the father of modern dentistry".

The known active constituent of Salvia divinorum is a trans-neoclerodane diterpenoid known as salvinorin A (chemical formula C23H28O8). This compound is present in the dried plant at about 0.18%. Salvinorin A is not an alkaloid (meaning it does not contain a basic nitrogen), unlike most known opioid receptor ligands. Salvinorin A is the first documented diterpene hallucinogen. Similar to many psychoactive herbs, Salvia divinorum synthesizes and excretes its active constituent (salvinorin A) via trichomes, of the peltate-glandular morphology, located just beneath the cuticle (subcuticular) layer.

Adoptive T cell therapy is a form of passive immunization by the transfusion of T-cells. They are found in blood and tissue and typically activate when they find foreign pathogens. Activation occurs when the T-cell's surface receptors encounter cells that display parts of foreign proteins (either on their surface or intracellularly). These can be either infected cells or other antigen-presenting cells (APCs). The latter are found in normal tissue and in tumor tissue, where they are known as tumor-infiltrating lymphocytes (TILs). They are activated by the presence of APCs such as dendritic cells that present tumor antigens. Although these cells can attack tumors, the tumor microenvironment is highly immunosuppressive, interfering with immune-mediated tumour death. Multiple ways of producing tumour-destroying T-cells have been developed. Most commonly, T-cells specific to a tumor antigen can be removed from a tumor sample (TILs) or filtered from blood. The T-cells can optionally be modified in various ways, cultured and infused into patients. T cells can be modified via genetic engineering, producing CAR-T cell or TCR T cells or by exposing the T cells to tumor antigens in a non-immunosuppressive environment, that they recognize as foreign and learn to attack. Another approach is transfer of haploidentical γδ T cells or natural killer cells from a healthy donor. The major advantage of this approach is that these cells do not cause graft-versus-host disease. The disadvantage is that transferred cells frequently have impaired function.

Sources: en.wikipedia.org

Frequently asked questions

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.

Is cardarine approved for human use?

No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.

Why was its development discontinued?

Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.

Is cardarine legal to buy?

Legal status varies by country, but cardarine is not approved as a medicine in major jurisdictions. It is often sold as a research chemical, a category that may not be lawful for human use. Buyers should check local laws and product labels carefully.

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