PPARδ agonist is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.
Updated 2025-10-19. Numbers and descriptions here follow the published literature rather than marketing material.
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.
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.
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.
| Property | Value | Notes |
|---|---|---|
| IUPAC name | {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid | Systematic name for GW501516 |
| CAS Registry Number | 317318-70-0 | Unique identifier for the parent compound |
| Molecular formula | C21H18F3NO3S2 | Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur |
| Molecular weight | 453.5 g/mol | Approximate value for the neutral form |
| Appearance | White to off-white powder | Typical description for purified laboratory material |
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.
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.
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.
In the fitness and bodybuilding literature, cardarine is frequently discussed as an endurance agent or fat-loss compound, although such claims are not supported by robust clinical evidence. Online descriptions often mix animal data, user anecdotes, and marketing language. Researchers who study PPARδ agonists distinguish between receptor activation in controlled experiments and unsupervised use of unverified products. The latter introduces unknown purity, dose, and interactions, making reported experiences difficult to interpret scientifically.
By taking command in person, Buller had allowed the overall direction of the war to drift. Because of concerns about his performance and negative reports from the field, he was replaced as Commander in Chief by Lord Roberts. Roberts assembled a new team for headquarters staff from far and wide: Lord Kitchener (Chief of Staff) from the Sudan; Frederick Russell Burnham (Chief of Scouts), the American scout, from the Klondike; George Henderson from the Staff College; Neville Bowles Chamberlain from Afghanistan; and William Nicholson (Military Secretary) from Calcutta. Like Buller, Roberts first intended to attack directly along the Cape Town–Pretoria railway but, again like Buller, was forced to relieve the beleaguered garrisons. Leaving Buller in command in Natal, Roberts massed his main force near the Orange River and along the Western Railway behind Methuen's force at the Modder River and prepared to make a wide outflanking move to relieve Kimberley. Except in Natal, the war had stagnated. Other than a single attempt to storm Ladysmith, the Boers made no attempt to capture the besieged towns. In the Cape Midlands, the Boers did not exploit the British defeat at Stormberg and were prevented from capturing the railway junction at Colesberg. In the dry summer, the grazing on the veld became parched, weakening the Boers' horses and draught oxen, and many Boer families joined their menfolk in the siege lines and laagers (encampments), fatally encumbering Cronjé's army.
Femarelle is a dietary supplement range containing DT56a, a tofu-derived soy extract, together with additional ingredients including flaxseed powder, vitamins, and minerals. DT56a has been studied for its potential activity as a selective estrogen receptor modulator (SERM), meaning that it may interact selectively with estrogen receptors in different tissues. Femarelle has been evaluated in several clinical studies investigating its possible role in supporting women during menopause, including studies on menopausal symptoms, vaginal health, bone health, and safety profile. Some studies reported encouraging findings, including improvements in menopausal symptoms and a favorable safety profile compared with traditional hormone replacement therapy, although the published trials were generally limited by relatively small sample sizes and short study durations. In 2008, an application was submitted to the European Food Safety Authority (EFSA) regarding a health claim related to bone mineral density and osteoporosis risk. EFSA concluded that the available evidence at that time was insufficient to establish a cause-and-effect relationship between Femarelle consumption and improvements in bone mineral density or reduction of osteoporosis risk in postmenopausal women.
=== Sex === Differences in male and female skeletal anatomy are used by bioarchaeologists to determine the biological sex of human skeletons. Humans are sexually dimorphic, although overlap in body shape and sexual characteristics is possible. Not all skeletons can be assigned a sex, and some may be wrongly identified. Biological males and biological females differ most in the skull and pelvis; bioarchaeologists focus on these body parts, although other body parts can be used. The female pelvis is generally broader than the male pelvis, and the angle between the two inferior pubic rami (the sub-pubic angle) is wider and more U-shaped, while the sub-pubic angle of the male is more V-shaped and less than 90 degrees. In general, the male skeleton is more robust than the female skeleton because of male's greater muscles mass. Male skeletons generally have more pronounced brow ridges, nuchal crests, and mastoid processes. Skeletal size and robustness are influenced by nutrition and activity levels. Pelvic and cranial features are considered to be more reliable indicators of biological sex. Sexing skeletons of young people who have not completed puberty is more difficult and problematic, because the body has not fully developed. Bioarchaeological sexing of skeletons is not error-proof. Recording errors and re-arranging of human remains may play a part in such misidentification.
== Metabolism == Metabolism of this compound has been assessed, revealing diclazepam has an approximate elimination half-life of 42 hours and undergoes N-demethylation to delorazepam, which can be detected in urine for 6 days following administration of the parent compound. Other metabolites detected were lorazepam and lormetazepam which were detectable in urine for 19 and 11 days, respectively, indicating hydroxylation by cytochrome P450 enzymes occurring concurrently with N-demethylation.
Sources: en.wikipedia.org
== Other uses == Seed Science and Technology, a journal about seed science published by the International Seed Testing Association SST (typeface) Swiss Solvency Test, a framework for the regulation of the insurance industry in Switzerland Serious Sam: Tormental, a video game by Gungrounds Sales and Services Tax, a type of tax in Malaysia
== Applications == The covalent binding of the isopeptag to its binding partner can be used to permanently link proteins together in the complex environment of a bacterial cell, to target proteins of interest for cellular imaging, and to develop new protein structures.
== Chemistry == The separation of the stereoisomers is one of the easier in organic chemistry and is described in the original patent. It involves "treatment of racemic methadone base with d-(+)-tartaric acid in an acetone/water mixture [which] precipitates almost solely the dextro-methadone levo-tartrate, and the more potent Levomethadone can easily be retrieved from the mother liquor in a high state of optical purity." There is now an asymmetric synthesis available to prepare both levomethadone (R-(−)-methadone) and dextromethadone (S-(+)-methadone).
=== Leukocyte adhesion deficiency and the "multistep paradigm" === Working with physicians seeing patients with recurring, life-threatening bacterial infections, Springer found their leukocytes lacked LFA-1 (αLβ2), Mac-1 (αMβ2), and αXβ2. Anderson and Springer named the disease leukocyte adhesion deficiency (LAD) in a review article, and it was shown to be caused by mutations in the β2 subunit common to the leukocyte integrins. Patients have abnormally high levels of neutrophils in their circulation, which cannot emigrate out of the bloodstream to fight infection. This demonstrated that β2 integrins were important in leukocyte interactions with vascular endothelial cells and stimulated Springer to set up work in the lab on endothelial cells and flow chambers. In related work on LFA-1 ligands, ICAM-1 and ICAM-2 were shown to be inducible and constitutively expressed, respectively, on endothelium. It had long been known from intravital microscopy that leukocyte emigration involved leukocyte rolling on endothelium followed by firm adhesion and subsequent transendothelial migration. Using white blood cells infused in flow chambers and purified adhesion molecules on the chamber walls under physiological shear rates found in vivo, Springer and postdoctoral fellow Mike Lawrence reconstituted three sequential interactions required for leukocyte emigration. Flow chamber walls were coated with P-selectin, ICAM-1, or both. Infused neutrophils were found to readily attach and then roll on P-selectin, but could not attach to ICAM-1 in flow.
== Other media == A Borderlands film was released by Gearbox and Lionsgate in 2024, with Eli Roth as director. The film received negative reviews from critics and poor reception from fans. In April 2020, Gearbox announced it was developing a television series based on its Brothers in Arms series.
Sources: en.wikipedia.org
Synthetic biology generally falls under existing regulations for GMOs and biotechnology in general, and any regulations that exist for downstream commercial products, although there are generally no regulations in any jurisdiction that are specific to synthetic biology.
== Controversy on acidity == Recent research has challenged these proposed ranges, finding that healthy human skin naturally tends to return to acidity levels below 5.0 when left untouched by skincare products or water for extended periods. An ideal pH value of 4.7 has been identified, with some individuals showing levels as low as 4.3. Subjects with a skin pH below 5.0 exhibited significantly less scaling, higher hydration levels, and better skin flora presence compared to those with higher pH levels, suggesting better overall skin condition. The acidic surface pH is crucial for the growth conditions of resident skin microbiota, which play a vital role in maintaining skin health. Human skin and its microbiota have a mutually beneficial symbiotic relationship, with the skin providing an optimal environment for resident microbiota while the microbiota help reinforce the skin's immunity by preventing colonization by harmful pathogens and contributing to skin acidification. Skin care products that lower skin pH to 4.0–4.5 help maintain resident microbiota on the skin, whereas alkaline personal care products promote their dispersal.
== Safety == In 2023, the European Food Safety Authority reassessed the safety of erythritol and lowered the recommended daily intake limit to 0.5 grams per kg body weight, which equates to 35 g for an average adult (70 kg). The lower limit was set to "safeguard against its laxative effect and to mitigate against long-term effects, such as electrolyte imbalance arising from prolonged exposure to erythritol-induced diarrhea." Previously, in 2015, scientists assessed doses for erythritol where symptoms of mild gastrointestinal upset occurred, such as nausea, excess flatus, abdominal bloating or pain, and stool frequency. At a content of 1.6% in beverages, it was not considered to have a laxative effect. The upper limit of tolerance was 0.78 and 0.71 g/kg body weight in adults and children respectively. In the United States, erythritol is among several sugar alcohols that are generally recognized as safe (GRAS) for food manufacturing.
=== Infant deficiency === Comparative studies carried out in lactating mothers indicate a mean value of vitamin D content in the breast milk of 45 IU/liter. This vitamin D content is too low to meet the vitamin D requirement of 400 IU/day recommended by several government organizations ("...as breast milk is not a meaningful source of vitamin D."). The same government organizations recommend that lactating women consume 600 IU/day, but this is insufficient to raise breast milk content to deliver recommended intake. There is evidence that breast milk content can be increased, but because the transfer of the vitamin from the lactating mother's serum to milk is inefficient, this requires that she consume a dietary supplement above the government-set safe upper limit of 4,000 IU/day. Given the shortfall, there are recommendations that breast-fed infants be fed a vitamin D dietary supplement of 400 IU/day during the first year of life. If not breastfeeding, infant formulas are designed to deliver 400 IU/day for an infant consuming a liter of formula per day – a normal volume for a full-term infant after the first month.
Sources: en.wikipedia.org
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.
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.
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.
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.