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Identity And Pharmacological Classification — Reference Sheet

By Editorial Desk · published 2025-07-04 · last reviewed 2025-08-04 · News

Everything below concerns Nuclear receptor. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Updated 2025-08-04. Numbers and descriptions here follow the published literature rather than marketing material.

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.

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.

Regulatory Status and Detection Context

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.

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 Laboratory Detection

Published human data are sparse and mostly come from early-phase trials. Those studies examined short-term changes in lipids, glucose, and exercise capacity, but they were not large enough to establish efficacy or long-term safety. Some animal experiments reported increased running endurance, yet such findings do not prove a performance benefit in people. Anti-doping laboratories detect GW501516 and its metabolites in urine or blood using liquid chromatography-tandem mass spectrometry. Detection windows depend on dose, sample type, and individual metabolism. The method is sensitive enough to identify trace residues in tested samples.

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.

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Mechanism and Research Context

GW501516 acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in transcription of genes related to lipid handling and energy use. Activation of PPARδ can shift skeletal muscle toward greater fatty acid oxidation in animal models, which is one reason it drew interest for metabolic disease and exercise research. The exact downstream effects depend on tissue, species, dose, and duration. Human data are sparse, so many proposed benefits remain hypotheses rather than established clinical outcomes.

Laboratory studies have examined GW501516 in cell cultures and rodents for conditions such as dyslipidemia, insulin resistance, and obesity. Some trials in humans were initiated, but development was discontinued after preclinical findings raised concerns about cancer in certain models. Those findings do not prove that the compound causes cancer in people, but they contributed to regulatory caution. Later reviews often describe the evidence as preliminary and insufficient for assessing long-term safety.

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 is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.

Identity and Regulatory Status

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.

Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.

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.

Notes from published material

== External links == The MEROPS online database for peptidases and their inhibitors: I04.023 alpha-2+Antiplasmin at the U.S. National Library of Medicine Medical Subject Headings (MeSH) SERPINF2+protein,+human at the U.S. National Library of Medicine Medical Subject Headings (MeSH) Human SERPINF2 genome location and SERPINF2 gene details page in the UCSC Genome Browser.

== Sources == "Leslie Stephen Ettre," Obituary, Hartford Courant, June 4, 2010. C. W. Gerhke, Chromatography: A Century of Discovery 1900–2000 : The Bridge to the Sciences/Technology Journal of Chromatography Library Vol. 64 (Elsevier, 2001), pp. 178 – 179. "Happy Birthday Professor Leslie S. Ettre," Chromatographia, (2007) 66 (5–6), 301.

=== Doubling time === The doubling time is the amount of time it would take for a breeder reactor to produce enough new fissile material to replace the original fuel and additionally produce an equivalent amount of fuel for another nuclear reactor. This was considered an important measure of breeder performance in early years, when uranium was thought to be scarce. However, since uranium is more abundant than thought in the early days of nuclear reactor development, and given the amount of plutonium available in spent reactor fuel, doubling time has become a less important metric in modern breeder-reactor design.

Evidence shows that all dinosaurs had erect legs similar to that of birds and many mammals, as opposed to the sprawling leg stance of cold-blooded tetrapods. Some were herbivorous, others carnivorous. Evidence suggests that all dinosaurs were egg-laying, and that nest-building was a trait shared by many dinosaurs, both avian and non-avian. While dinosaurs were ancestrally bipedal, many extinct groups included quadrupedal species, and some were able to shift between these stances. Elaborate display structures such as horns or crests are common to all dinosaur groups, and some extinct groups developed skeletal modifications such as bony armor and spines. While the dinosaurs' modern-day surviving avian lineage (birds) are generally small due to the constraints of flight, many non-avian dinosaurs were large-bodied—the largest sauropod dinosaurs are estimated to have reached lengths of 39.7 meters (130 feet) and heights of 18 m (59 ft) and were the largest land animals of all time. The first dinosaur fossils were recognized in the early 19th century, with the name "dinosaur" (meaning "terrible lizard") being coined by Sir Richard Owen in 1842 to refer to these "great fossil lizards". Since then, mounted fossil dinosaur skeletons have been major attractions at museums worldwide, and dinosaurs have become an enduring part of popular culture. The large sizes of some dinosaurs, as well as their seemingly monstrous and fantastic nature, have ensured their regular appearance in best-selling books and films, such as the Jurassic Park franchise.

(Newton's second law of motion in the non-relativistic case, i.e. valid only at ion velocity much lower than the speed of light). Here F is the force applied to the ion, m is the mass of the ion, a is the acceleration, Q is the ion charge, E is the electric field, and v × B is the vector cross product of the ion velocity and the magnetic field Equating the above expressions for the force applied to the ion yields:

Sources: en.wikipedia.org

Further detail

In the Druze Faith, Jesus is considered and revered as one of the seven spokesmen or prophets (natiq), defined as messengers or intermediaries between God and mankind, along with Adam, Noah, Abraham, Moses, Muhammad and Muhammad ibn Isma'il, each of them sent in a different period of history to preach the message of God. The Druze venerate Jesus "the son of Joseph and Mary" and his four disciples, who wrote the Gospels. According to the Druze manuscripts Jesus is the Greatest Imam and the incarnation of Ultimate Reason (ʿAql) on earth and the first cosmic principle (Ḥadd), and regards Jesus and Hamza ibn Ali as the incarnations of one of the five great celestial powers, who form part of their system. Druze doctrines include the beliefs that Jesus was born of a virgin named Mary, performed miracles, and died by crucifixion. Druze doctrines include that Hamza ibn Ali took Jesus down from the cross and allowed him to return to his family, to prepare men for the preaching of his religion. In the Druze tradition, Jesus is known under three titles: the True Messiah (al-Masiḥ al-Haqq), the Messiah of all Nations (Masiḥ al-Umam), and the Messiah of Sinners. This is due, respectively, to the belief that Jesus delivered the true Gospel message, the belief that he was the Saviour of all nations, and the belief that he offers forgiveness. The Druze shrine of "Sayyidna al-Masih" (Our Lord Jesus), one of the most important religious sites for the Druze, is located on a high mountain peak in the Al-Bajjah area of As-Suwayda Governorate.

In early 2012, prices for cattle futures contracts on the Chicago Mercantile Exchange fell as result of the controversy. Cargill started using a label stating "Contains Finely Textured Beef" from 2014. Production of finely textured beef increased modestly, as beef prices rose by 27% over two years in 2014 and "retailers [sought] cheaper trimmings to include in hamburger meat and processors find new products to put it in". Senior management of Cargill claimed almost full recovery as sales tripled. BPI regained 40 customers that are mostly processors and patty-makers who distribute to retailers and the USDA since March 2012. It does not label its product.

Diphenhydramine is a first-generation antihistamine used to treat several conditions including allergic symptoms and itchiness, the common cold, insomnia, motion sickness, and extrapyramidal symptoms. Diphenhydramine also has local anesthetic properties, and has been used as such in people allergic to common local anesthetics such as lidocaine.

== Origin == Larazotide acetate is a synthetic peptide based on a Vibrio cholerae enterotoxin called zonula occludens toxin that decreases intestinal permeability. An investigation was carried out to discover which specific part of this toxin was responsible for this activity. Several mutants were constructed, and tested for their biological activity and their ability to bind to intestinal epithelial cells in culture. The responsible region was located near the carboxyl terminus of the toxin protein. This region coincided with a peptide product generated by Vibrio cholerae. The eight amino acid sequence in this region was shared with zonulin, an endogenous protein involved in tight junction modulation. This sequence was later designated larazotide acetate.

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.

Is cardarine approved for any medical use?

No. Cardarine has not received approval for human therapeutic use in major jurisdictions. It remains an investigational compound.

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