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Identity And Pharmacological Mechanism — Reference Sheet

By Editorial Desk · published 2025-10-14 · last reviewed 2025-11-04 · Wiki

The short version of GW501516 fits in a sentence. The long version — which is the one that helps — is below.

Reviewed 2025-11-04. Anything still debated is marked as such rather than presented as settled.

Identity and Pharmacological Mechanism

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 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.

Background and Regulatory Status

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.

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 at a glance

PropertyValueNotes
Chemical classSynthetic PPARδ agonistNot a steroid or a selective androgen receptor modulator.
Common synonymsCardarine, GW501516, GW-501516, endurobolNames vary by supplier and literature source.
AppearanceWhite to off-white powderConsistent with many small-molecule research chemicals.
SolubilityLow in water; soluble in DMSO and ethanolOften prepared in organic solvent for laboratory work.
Primary targetPPARδ (NR1C2)Nuclear receptor involved in lipid and energy metabolism.

Regulatory Status and Detection Context

Analytical laboratories typically identify cardarine and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is a common matrix in anti-doping testing, while blood and tissue may be used in research settings. Detection windows depend on the assay, the sample matrix, and the compound's metabolism. Because cardarine is extensively metabolized, laboratories often target specific metabolites to improve sensitivity and confirmation. Reference standards are required for reliable quantification. Method validation includes checks for selectivity, linearity, and carryover.

A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.

Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.

Related pages on this site

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.

Further detail

=== 6 December === The Governor of Kursk Oblast in Russia, Roman Starovoyt, claimed that a Ukrainian drone attack destroyed an oil tank near an airbase. No reports of casualties and the fire was under control. There was no comment from Ukraine on these claims.

The expected results for external quality assessment samples are not disclosed to the laboratory. External quality assessment programs have been widely adopted in North America and western Europe, and laboratories are often required to participate in these programs to maintain accreditation. Logistical issues may make it difficult for laboratories in under-resourced areas to implement external quality assessment schemes.

== External links == Royal Society of Chemistry, Historical Group, short biography of Curtius University of Kiel history of the inorganic department Heidelberg University German Alpen Association, Kiel section

Sources: en.wikipedia.org

Supporting material

Merck & Co. adapted the 1936 laboratory-scale synthesis, allowing them to manufacture thiamine in Rahway in 1937. However, an alternative route using the intermediate Grewe diamine (5-(aminomethyl)-2-methyl-4-pyrimidinamine), first published in 1937, was investigated by Hoffman La Roche and competitive manufacturing processes followed. Efficient routes to the diamine have continued to be of interest. In the European Economic Area, thiamine is registered under REACH regulation and between 100 and 1,000 tonnes per annum are manufactured or imported there.

[(CH3)3SiO]2SO2 + 3 HF + SbF5 → [H3SO4]+[SbF6]− + 2 (CH3)3SiF The above reaction is thermodynamically favored due to the high bond enthalpy of the Si–F bond in the side product. Protonation using simply fluoroantimonic acid, however, has met with failure, as pure sulfuric acid undergoes self-ionization to give [H3O]+ ions:

=== Opposition to the Award === Basuto chiefs—including Lerotholi—welcomed the Award, and 3,000 heads of cattle were paid almost immediately as a gesture of goodwill. On 9 May 1881, Thomas Charles Scanlen replaced Sprigg as prime minister, while Basutophile Jacobus Wilhelmus Sauer was appointed as the new Secretary for Native Affairs. Scanlen encountered challenges in fully enforcing the Award, such as the erosion of the colonial administration's prestige. Masopha demanded to be granted almost arbitrary power, refusing to pay his share of the hut tax and forbidding the return of the local magistrate. Joseph Orpen, who replaced Griffith, was seen as too sympathetic to the former rebels. His handling of cattle and land compensation led to the alienation of Basuto loyalists and the departure of nearly all pre-war magistrates from Basutoland. In January 1882, Letsie I assembled an army in order to enforce the Award on Masopha, yet the expedition was cancelled as it was judged that Masopha retained considerable popular support. The Colonial Office refused to allow the Cape to abandon Basutoland and cancel the Award. Robinson then set 15 March as the new deadline for the enforcement of the Award, threatening to confiscate land from the chiefs failing to abide to it and to redistribute Quthing District to white volunteers who fought in the war. Following pleas by Letsie I and Orpen, Robinson cancelled the Award on 15 March and pledged not to confiscate land. This was followed by the repeal of the Peace Preservation Act on 6 April.

silent mutation A type of neutral mutation which does not have an observable effect on the organism's phenotype. Though the term "silent mutation" is often used interchangeably with synonymous mutation, synonymous mutations are not always silent, nor vice versa. Missense mutations which result in a different amino acid but one with similar functionality (e.g. leucine instead of isoleucine) are also often classified as silent, since such mutations usually do not significantly affect protein function.

Sources: en.wikipedia.org

Frequently asked questions

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.

How does cardarine interact with the body?

It binds to and activates PPARδ, a nuclear receptor that regulates genes related to fatty acid oxidation and energy use. This activation alters transcription in tissues such as skeletal muscle and liver. The full range of downstream effects in humans is not fully established.

Is cardarine found naturally?

No, cardarine is not known to occur naturally in plants, animals, or humans. It is a synthetic molecule produced for laboratory research. Products labeled as cardarine should therefore be treated as manufactured chemicals with variable purity.

Is cardarine approved for human use?

No. Major drug regulators have not approved GW501516 for treating any medical condition. Products sold as cardarine are typically unapproved research chemicals or supplements, so their contents and safety are not assured.

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