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Background And Regulatory Status — Quick Reference

By Editorial Desk · published 2025-07-14 · last reviewed 2025-07-29 · Faq

research chemical comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.

Updated 2025-07-29. Numbers and descriptions here follow the published literature rather than marketing material.

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.

Cardarine as Investigational PPARδ Agonist

The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.

Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.

Cardarine at a glance

PropertyValueNotes
IUPAC name{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acidSystematic name for GW501516
CAS Registry Number317318-70-0Unique identifier for the parent compound
Molecular formulaC21H18F3NO3S2Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur
Molecular weight453.5 g/molApproximate value for the neutral form
AppearanceWhite to off-white powderTypical description for purified laboratory material

Mechanism and Laboratory Detection

Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.

GW501516 binds and activates PPARδ, a nuclear receptor that influences transcription of genes involved in fatty acid oxidation and energy use. Activation shifts some metabolic pathways in preclinical models, which is why the compound has been studied for lipid disorders and exercise-related endpoints. The exact downstream effects in humans are incompletely mapped. PPARδ is expressed in many tissues, including skeletal muscle, liver, and adipose tissue, so broad activation may have varied consequences. Researchers continue to examine how selective or partial activation might alter the balance between benefits and risks.

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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.

Reference notes

syncytium Also symplasm; pl. syncytia. A multinucleate cell, i.e. a cell containing more than one nucleus or, in the broadest sense, more than one nuclear genome (a meaning which is equated with polyploidy). Syncytia may form as a result of cell fusion between uninucleate cells, migration of a nucleus from one cell to another, or multiple nuclear divisions without accompanying cytokinesis (forming a coenocyte). The term may also refer to cells which are interconnected by specialized membranes with gap junctions as in some neuromuscular cell types.

== Variants == There is no consensus on some terms describing carbon nanotubes in the scientific literature: both "-wall" and "-walled" are being used in combination with "single", "double", "triple", or "multi", and the letter C is often omitted in the abbreviation, for example, multi-walled carbon nanotube (MWNT). The International Standards Organization typically uses "single-walled carbon nanotube (SWCNT)" or "multi-walled carbon nanotube (MWCNT)" in its documents.

Russia claimed to have taken the village of Shumy, ten kilometers east of Toretsk. Seven people were killed and 36 others were injured in a Russian attack in Vilniansk, Zaporizhzhia Oblast. Three people were killed in separate attacks in Donetsk and Kherson Oblasts. Russian officials claimed that five people, including two children, were killed in a Ukrainian drone strike in Gorodishche, Kursk Oblast.

=== Media preparation and washing units === The washing unit provides cleaning services for laboratory glassware and plasticware. It handles laundering of work clothing and decontamination of genetically modified organism (GMO) waste and hazardous laboratory waste. The media preparation unit prepares cultivation media and solutions for tissue culture. It produces bacteriological media and agar plates.

Sources: en.wikipedia.org

Reference notes

=== Early career === In 1966, Jim and Tammy Faye Bakker began working at Pat Robertson's Christian Broadcasting Network (CBN) in Portsmouth, Virginia, which had an audience in the low thousands at the time. The Bakkers contributed to the network's growth, hosting a children's variety show called Come On Over that employed comic routines with puppets. Due to the success of Come On Over, Robertson made Bakker the host of a new prime-time talk show, The 700 Club, which gradually became CBN's flagship program. The Bakkers left CBN in 1973 and, soon after, joined with Paul and Jan Crouch to help co-found the Trinity Broadcasting Network (TBN) in California. However, this partnership lasted only eight months until a falling-out between Jim Bakker and Paul Crouch caused the Bakkers to eventually leave the new network.

=== Mechanism === Younes and Loveland define fission as, "...a collective motion of the protons and neutrons that make up the nucleus, and as such it is distinguishable from other phenomena that break up the nucleus. Nuclear fission is an extreme example of large-amplitude collective motion that results in the division of a parent nucleus into two or more fragment nuclei. The fission process can occur spontaneously, or it can be induced by an incident particle." The energy from a fission reaction is produced by its fission products, though a large majority of it, about 85 percent, is found in fragment kinetic energy, while about 6 percent each comes from initial neutrons and gamma rays and those emitted after beta decay, plus about 3 percent from neutrinos as the product of such decay.

=== Phase 1 === ABL-301 (SAR-446159) – bispecific antibody against α-synuclein [72] ALS-205 (PMX-205) – complement C5a receptor antagonist [73] ALX-001 (BMS-984923) – metabotropic glutamate mGlu5 receptor silent allosteric modulator [74] ARV-102 – leucine-rich repeat kinase 2 (LRRK2) inhibitor [75] ATH-399A (DWP-307399; HL-192) – nuclear receptor subfamily 4 group A member 2 (NR4A2) agonist [76] CT-2500 – undefined mechanism of action [77] FB-418 – Bcr-Abl tyrosine kinase inhibitor and leucine-rich repeat kinase 2 (LRRK2) inhibitor [78] GT-02287 – β-glucocerebrosidase (GCase) activator and/or chaperone [79] HL-400 – NLR family pyrin domain containing 3 (NLRP3) inhibitor [80] HNC-364 (rasagiline prodrug) – monoamine oxidase B (MAO-B) inhibitor [81] Human amniotic epithelial cell therapy - Shanghai iCELL Biotechnology (hAECs; hAESCs) – cell replacement [82] JNJ-0376 – undefined mechanism of action [83] JX-2105 – undefined mechanism of action [84] Lu AF28996 (Lu AF-28996) – dopamine D1 and D2 receptor agonist [85] LY-3962681 – RNA interference and α-synuclein expression modulator [86] MEDI-1341 (TAK-341) – monoclonal antibody against α-synuclein [87] NEU-723 – leucine-rich repeat kinase 2 (LRRK2) inhibitor [88] NN-9001 – undefined mechanism of action [89] PK-081 – α-synuclein degrader [90] Selnoflast (NLRP3i; RG-6418; RO-7486967; Somalix) – NLR family pyrin domain containing 3 (NLRP3) inhibitor inhibitor [91] TRN-501 – undefined mechanism of action [92] VQ-101 – glucosylceramidase stimulant [93] WID-2301 – undefined mechanism of action [94] WIT-2001 – undefined mechanism of action [95]

== Mechanism of action == An average dairy cow begins her lactation with a moderate daily level of milk production. This daily output increases until, at about 70 days into the lactation, production peaks. From that time until the cow is dry, production slowly decreases. This increase and decrease in production is partially caused by the count of milk-producing cells in the udder. Cell counts begin at a moderate number, increase during the first part of the lactation, then decrease as the lactation proceeds. Once lost, these cells generally do not regrow until the next lactation. Administration of rBST or BST prior to peak production, in cows that are well-fed, slows the rate at which the number of mammary cells decreases, and increases the amount of nutrients directed away from fat and toward the mammary cells, leading to an extension of peak milk production. The effects are mediated by the insulin-like growth factor (IGF) system, which is upregulated in response to BST or rBST administration in well-fed cows.

Although limited in their authority, these assemblies represented a move in the direction of representative government at the national level, and by 1880 assemblies also had been formed in villages and towns. In 1880 delegates from twenty-four prefectures held a national convention to establish the Kokkai Kisei Dōmei. Although the government was not opposed to parliamentary rule, confronted with the drive for "people's rights", it continued to try to control the political situation. New laws in 1875 prohibited press criticism of the government or discussion of national laws. The Public Assembly Law (1880) severely limited public gatherings by disallowing attendance by civil servants and requiring police permission for all meetings. Within the ruling circle, however, and despite the conservative approach of the leadership, Okuma continued as a lone advocate of British-style government, a government with political parties and a cabinet organized by the majority party, answerable to the national assembly. He called for elections to be held by 1882 and for a national assembly to be convened by 1883; in doing so, he precipitated a political crisis that ended with an 1881 imperial rescript declaring the establishment of a national assembly in 1890 and dismissing Okuma. Rejecting the British model, Iwakura and other conservatives borrowed heavily from the Prussian constitutional system. One of the Meiji oligarchy, Itō Hirobumi (1841–1909), a Chōshū native long involved in government affairs, was charged with drafting Japan's constitution.

Sources: en.wikipedia.org

Frequently asked questions

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.

Why is cardarine banned in sport?

It is prohibited by the World Anti-Doping Agency as a hormone and metabolic modulator. Athletes who test positive for GW501516 can face sanctions, including suspensions and loss of results.

What is the difference between cardarine and GW501516?

Cardarine is a common or trade-style name, while GW501516 is the research code for the same chemical entity. Some sources also use Endurobol or GSK-516. The names refer to the same compound, not distinct drugs.

What is cardarine?

Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.

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