A practical reference on PPARδ agonist: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
Reviewed 2026-06-10. Anything still debated is marked as such rather than presented as settled.
At the molecular level, GW501516 binds and activates PPARδ, a nuclear receptor that regulates transcription. Activation shifts expression of genes involved in fatty acid oxidation, energy expenditure, and lipid transport in skeletal muscle and liver. Animal studies report increased endurance and altered lipid profiles after exposure. Human data are limited to small trials and do not establish long-term safety or efficacy. PPARδ also has roles in cell proliferation, so the relationship between activation and cancer risk remains an open question.
Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.
Quality assessment for cardarine samples usually combines identity, purity, and impurity testing. Nuclear magnetic resonance spectroscopy and mass spectrometry can confirm molecular structure, while high-performance liquid chromatography estimates purity. Certificates of analysis from testing laboratories may list these results, but they do not establish safety or legality. In the absence of approved manufacturing, products sold online may contain the wrong compound, variable amounts, or unlisted contaminants. Independent verification is therefore central to analytical work and to interpreting any reported biological activity.
Laboratory detection of GW501516 commonly uses liquid chromatography coupled with tandem mass spectrometry. The method can identify the parent compound or its metabolites in urine and blood after sample cleanup. Protein precipitation, solid-phase extraction, or enzymatic hydrolysis may precede analysis, depending on the matrix. Reference standards are required for accurate quantification and confirmation. Because the compound is not approved, testing often occurs in anti-doping, forensic, or research settings rather than routine clinical care. Results are reported with limits of detection and quantification.
| Property | Value | Notes |
|---|---|---|
| Common name | Cardarine | Also called GW501516 and endurobol. |
| Chemical formula | C21H18F3NO3S2 | Molecular weight about 453.5 g/mol. |
| Appearance | White to off-white solid | Form depends on synthesis and purity. |
| Solubility | Soluble in DMSO and ethanol | Low solubility in water. |
| Typical storage | -20 °C, desiccated, protected from light | Common for research chemicals. |
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.
Safety concerns emerged from long-term animal studies. In rodents given the compound for extended periods, researchers found an increased incidence of certain cancers, including liver and bladder tumors. These findings contributed to the discontinuation of clinical development. Whether similar risks apply to short-term or low-level exposure in humans is not established, and controlled human safety data are limited. The relevance of high-dose rodent carcinogenicity findings to human use remains a subject of debate.
Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.
Laboratory studies indicate that GW501516 activates PPARδ, a nuclear receptor involved in fatty acid oxidation and energy metabolism. In rodent experiments, treated animals often showed increased endurance and reduced fat mass. These effects were observed under controlled conditions and do not establish safe or effective use in humans. The exact dose-response relationship in humans remains poorly characterized. Species differences in metabolism can affect how results translate across animals and people.
A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.
Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.
Lithium is a teratogen, which can cause birth defects in a small number of newborns. Case reports and several retrospective studies have demonstrated possible increases in the rate of a congenital heart defects (CHDs) including Ebstein's anomaly if taken during the first trimester of pregnancy. The risk is dose-dependent: in the 2017 AMX registry study, the relative risk of "any malformations" is 1.11 in those taking no more than 600 mg of lithium carbonate daily, 1.60 in those taking 601–900 mg daily, and 3.22 in those taking more than 900 mg daily. The first two numbers do not indicate a statistically significant association. In a 2018 meta-analysis, there was a statistically significant 62% increase (95% CI: 12%–133%) in congenital malformations in general, but not for cardiac malformations specifically. Exposure during any part of the pregnancy is associated with a slight but statistically significant increase in the risks of preterm birth and of a larger-than-usual baby at birth. Lithium is effective for preventing relapse during and after pregnancy. As the risks of stopping Lithium can be significant, patients are sometimes recommended to stay on this medicine while pregnant. Careful weighing of the risks and benefits should be made in consultation with a psychiatric physician. The relatively low teratogenic risk of lithium allows such a choice. The decision should be made before the start of pregnancy, as there is no reason for stopping lithium once the pregnancy has started.
HT-2157 (former development code SNAP-37889) is a drug which acts as a selective non-peptide antagonist for the receptor GAL-3, which is usually activated by the neuropeptide galanin. Blocking this receptor with HT-2157 produced increased serotonin release, as well as producing antidepressant and anxiolytic effects in animal studies, and it was also being researched for treatment of cognitive dysfunction. All human clinical trials were terminated due to safety concerns however, and new GAL-3 antagonists are now being sought instead.
=== Myopathies with cores === 'Core myopathies' such as multicore myopathy and central core disease are characterized by sharply-demarcated areas devoid of oxidative enzymes NADH, SDH, and COX, in muscle fibres.
1993/1947) Learning for Work (Miscellaneous Provisions) Order 1993 (S.I. 1993/1949) Act of Adjournal (Consolidation Amendment) (Courses for Drink-drive Offenders) 1993 (S.I. 1993/1955) Act of Sederunt (Sheriff Court Ordinary Cause Rules) 1993 (S.I. 1993/1956) Double Taxation Relief (Taxes on Income) (General) (Manufactured Overseas Dividends) Regulations 1993 (S.I. 1993/1957) Dartford–Thurrock Crossing (Amendment) Regulations 1993 (S.I. 1993/1961) Harwich Haven Harbour Revision Order 1993 (S.I. 1993/1962) A4 Trunk Road (Great West Road, Hounslow) (Prescribed Routes) Order 1993 (S.I. 1993/1963) London South Circular Trunk Road (A205) (Westhorne Avenue, Lewisham) (Prohibition of Use of Gaps in Central Reserve) Order 1993 (S.I. 1993/1964) Civil Aviation (Route Charges for Navigation Services) Regulations 1993 (S.I. 1993/1965) Importation of Bovine Semen (Amendment) Regulations 1993 (S.I. 1993/1966) Animals and Animal Products (Import and Export) (Amendment) Regulations 1993 (S.I. 1993/1967) Criminal Justice Act 1993 (Commencement No. 1) Order 1993 (S.I. 1993/1968) Education (Teachers) (Amendment) Regulations 1993 (S.I. 1993/1969) Clyde Port Authority (Dissolution) Order 1993 (S.I. 1993/1970) Education Act 1993 (Commencement No. 1 and Transitional Provisions) Order 1993 (S.I. 1993/1975) Education (London Oratory School) (Exemption from Pay and Conditions Orders) Order 1993 (S.I. 1993/1976) Further Education (Attribution of Surpluses and Deficits) (The Ridge College) Regulations 1993 (S.I.
== Side effects == Although melarsoprol cures about 96% of people with late stage disease, its toxicity limits its use. About 1–5% of people die during treatment. As a toxic organic compound of arsenic, melarsoprol is a dangerous treatment that is typically only administered by injection under the supervision of a licensed physician. Notable side effects are similar to arsenic poisoning. Among clinicians, it is colloquially referred to as "arsenic in antifreeze". Severe and life-threatening adverse reactions are associated with melarsoprol. It is known to cause a range of side effects including convulsions, fever, loss of consciousness, rashes, bloody stools, nausea and vomiting. In approximately 5–10% of cases, it causes encephalopathy. Of those, about 50% die due to encephalopathy-related adverse reactions. Additional potentially serious side effects of melarsoprol include damage to the heart, presence of albumin in the urine that could be associated with kidney damage, and an increase in blood pressure.
Sources: en.wikipedia.org
Double-stranded RNA (dsRNA) is RNA with two complementary strands, similar to the DNA found in all cells, but with the replacement of thymine by uracil and the adding of one oxygen atom. dsRNA forms the genetic material of some viruses (double-stranded RNA viruses). Double-stranded RNA, such as viral RNA or siRNA, can trigger RNA interference in eukaryotes, as well as interferon response in vertebrates. In eukaryotes, double-stranded RNA (dsRNA) plays a role in the activation of the innate immune system against viral infections.
== Function == CHS catalysis serves as the initial step for flavonoid biosynthesis. Flavonoids are important plant secondary metabolites that serve various functions in higher plants. These include pigmentation, UV protection, fertility, antifungal defense and the recruitment of nitrogen-fixing bacteria. CHS is believed to act as a central hub for the enzymes involved in the flavonoid pathway. Studies have shown that these enzymes interact via protein-protein interactions. Through FLIM FRET, it was shown that CHS interacts with chalcone isomerase (CHI), a consecutive step enzyme, as well as other non-consecutive step enzymes flavanone 3-hydroxylase (F3H), dihydroflavonol 4-reductase (DFR), and flavonol synthase I. Naringenin-chalcone synthase uses malonyl-CoA and 4-coumaroyl-CoA to produce CoA, naringenin chalcone, and CO2.
==== Colorimetric detection ==== The colorimetric detection method depends on incubation of the Western blot with a substrate that reacts with the reporter enzyme (such as peroxidase) that is bound to the secondary antibody. This converts the soluble dye into an insoluble form of a different colour that precipitates next to the enzyme and thereby stains the membrane. Development of the blot is then stopped by washing away the soluble dye. Protein levels are evaluated through densitometry (how intense the stain is) or spectrophotometry.
=== Energy === Formic acid can be used directly in formic acid fuel cells or indirectly in hydrogen fuel cells. Electrolytic conversion of electrical energy to chemical fuel has been proposed as a large-scale source of formate by various groups. The formate could be used as feed to modified E. coli bacteria for producing biomass. Natural methylotroph microbes can feed on formic acid or formate Formic acid has been considered as a means of hydrogen storage. The co-product of this decomposition, carbon dioxide, can be rehydrogenated back to formic acid in a second step. Formic acid contains 53 g/L hydrogen at room temperature and atmospheric pressure, which is three and a half times as much as compressed hydrogen gas can attain at 350 bar pressure (14.7 g/L). Pure formic acid is a liquid with a flash point of 69 °C, much higher than that of gasoline (−40 °C) or ethanol (13 °C). It is possible to use formic acid as an intermediary to produce isobutanol from CO2 using microbes.
where {ML} is the activity of the chemical species ML etc. K⊖ is dimensionless since activity is dimensionless. Activities of the products are placed in the numerator; activities of the reactants are placed in the denominator. See activity coefficient for a derivation of this expression. Since activity is the product of concentration and activity coefficient (γ) the definition could also be written as
Sources: en.wikipedia.org
Cardarine is a common name for the investigational compound GW501516. It acts as a PPARδ agonist and is not approved for human use. It is prohibited in sport.
It activates PPARδ, a nuclear receptor that influences gene expression related to lipid and energy metabolism. Animal studies show changes in endurance and lipid levels. Human effects and risks are not well established.
No, cardarine is not a steroid. It belongs to a different chemical class, the PPARδ agonists. It is also not a selective androgen receptor modulator.
LC-MS/MS is common, often after sample cleanup. The assay targets GW501516 or its metabolites.