If you have been reading about Metabolite and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.
Updated 2026-02-23. Numbers and descriptions here follow the published literature rather than marketing material.
Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.
Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.
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.
| Property | Value | Notes |
|---|---|---|
| Regulatory status | Prohibited in sport | Listed by WADA as a metabolic modulator. |
| Approved medical use | None in major jurisdictions | Not a registered drug. |
| Common test matrix | Urine | Most anti-doping samples use urine. |
| Typical detection method | LC-MS/MS | Detects parent compound and metabolites. |
| Reference standard storage | -20 °C, desiccated | Typical for analytical standards. |
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 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.
==== Glutamatergic, neurotrophic, and neuroplastic modulation ==== Research suggests that tianeptine produces its antidepressant effects through indirect alteration and inhibition of glutamate receptor activity (i.e., AMPA receptors and NMDA receptors) and release of BDNFTooltip brain-derived neurotrophic factor, in turn affecting neural plasticity. Some researchers hypothesize that tianeptine has a protective effect against stress induced neuronal remodeling. There is also action on the NMDA and AMPA receptors. In animal models, tianeptine inhibits the pathological stress-induced changes in glutamatergic neurotransmission in the amygdala and hippocampus. It may also facilitate signal transduction at the CA3 commissural associational synapse by altering the phosphorylation state of glutamate receptors. With the discovery of the rapid and novel antidepressant effects of drugs such as ketamine, many believe the efficacy of antidepressants is related to promotion of synaptic plasticity. This may be achieved by regulating the excitatory amino acid systems that are responsible for changes in the strength of synaptic connections as well as enhancing BDNF expression, although these findings are based largely on preclinical studies.
In 2010, due to a rise in foreign competition, Ajinomoto began restructuring to focus on several of its products while divesting others. The company divested its Calpis beverage unit in Japan in 2012, the Ajinomoto Sweetener Company (France) in October 2015, and Amoy Food (China) in November 2018. Ajinomoto decided to focus on its food and biomedical divisions, and acquired the contract manufacturing organization Althea Technologies (US) in 2013, the frozen food company Windsor Quality Holdings, Inc. (US) in November 2014, and the frozen food company Lavelli・Terrell・Smile (France) in November 2017. In April 2016, Ajinomoto merged its pharmaceutical division with Eisai, launching EA Pharma in Japan. In October 2017, Ajinomoto introduced a "Global Brand Logo" for use throughout the Ajinomoto group. In December 2017, Ajinomoto announced it had begun construction to expand its Kawasaki Plant, along with the construction of a new R&D building. In October 2018, Ajinomoto Althea (US) and OmniChem (Belgium) merged to form Ajinomoto Bio-Pharma Services, but in April 2025, all of Althea shares were transferred to Packaging Coordinators Inc. In April 2020, the Ajinomoto Group Nutrient Profiling System for Product, which has been developed as a method to scientifically estimate the nutritive value of products such as powdered soup and frozen foods, was introduced globally to about 500 kinds of group products in seven countries. In August, Ajinomoto announced its participation in the international environment initiative RE100 for renewable energy.
Silver nitrate is an inorganic compound with chemical formula AgNO3. It is a colorless solid that is a precursor to many other silver compounds. Silver nitrate is highly soluble in water but is poorly soluble in most organic solvents, except acetonitrile (111.8 g/100 g, 25 °C). Silver nitrate is the least expensive salt of silver; it offers several other advantages as well. It is non-hygroscopic (in contrast to silver fluoroborate and silver perchlorate). In addition, it is relatively stable to light, and it dissolves in numerous solvents, including water. The nitrate can be easily replaced by other ligands.
== Early life and education == Goldstein grew up on Staten Island and received his B.S. degree from Wagner College in 1959 and his M.S. and Ph.D. degrees from Rutgers University, the latter in 1964. He served on the faculty of the Albert Einstein College of Medicine from 1964 to 1972, and as director of the Division of Biochemistry at the University of Texas Medical Branch in Galveston from 1972 through 1978 before accepting the chairmanship of the Department of Biochemistry and Molecular Biology at the George Washington University School of Medicine & Health Sciences, a position he held for 31 years.
The targeting of journalists has prompted national and international condemnation. International watchdogs have urged Mexican authorities to end impunity for attacks on journalists. About 74 percent of the journalists killed since 1992 in Mexico have been reporters for print newspapers, followed in number by Internet media and radio at about 11 percent each. Television journalism accounts for 4 percent of the deaths.
Sources: en.wikipedia.org
Tetramethylurea (TMU) is the organic compound with the formula (Me2N)2CO. It is a substituted urea. This colorless liquid is used as an aprotic-polar solvent, especially for aromatic compounds and is used e. g. for Grignard reagents. TMU has a mild aromatic odor and, unlike other compounds of urea, is a colorless liquid.
=== Pharmacokinetics === Bromazepam is reported to be metabolized by a hepatic enzyme belonging to the cytochrome P450 family of enzymes. In 2003, a team led by Oda Manami at Oita Medical University reported that CYP3A4, a member of the Cytochrome P450 family, was not the responsible enzyme since itraconazole, a known inhibitor of CYP3A4, did not affect its metabolism. In 1995, J. van Harten at the Solvay Pharmaceutical Department of Clinical Pharmacology in Weesp reported that fluvoxamine, which is a potent inhibitor of CYP1A2, a less potent CYP3A4 inhibitor, and a negligible inhibitor of CYP2D6, does inhibit its metabolism. The major metabolite of bromazepam is hydroxybromazepam, which is an active agent too and has a half-life approximately equal to that of bromazepam.
== Medical uses == It is used to treat pulmonary arterial hypertension (PAH), pulmonary fibrosis, as well as atherosclerosis. In pediatric practice, prostacyclin is commonly used to mantain patency of the ductus arteriosus. Prostacyclins are given to people with class III or class IV PAH.
In biochemistry, the most prevalent, internationally accepted system of nomenclature for fatty acids is defined by the International Union of Pure and Applied Chemistry (IUPAC). Herein, the ω-x system (also known as the omega x or n-x system) establishes that fatty acids can be identified through the following formation: C:Dω–x where C is the total number of carbons, D is the number of double bonds, and ω–x indicates the position of the first double bond, counting from the –CH3 end of the fatty acid. The ω–x system curbs ambiguity regarding SFAs and MUFAs, as it specifically denotes both the carbon and unsaturation numbers, as well as the location of the double bond (i.e., for MUFAs). Equally, ω–x nomenclature is widely used for PUFAs, particularly for those wherein two consecutive double bonds are consistently separated by a methylene group (–CH2–). However, several PUFAs contain double bonds that are not always interrupted by a methylene group, and thus the ω–x system fails to establish the specific position of all double bonds about PUFA chains. As such, these atypical PUFAs are generically referred to as "non-methylene interrupted" (NMI) fatty acids, and are commonly found in lipids from marine invertebrates.
Sources: en.wikipedia.org
Legal status varies by country, but cardarine is not approved as a medicine in major jurisdictions. It is often sold as a research chemical, a category that may not be lawful for human use. Buyers should check local laws and product labels carefully.
Anti-doping laboratories use LC-MS/MS to detect GW501516 and its metabolites, usually in urine. The method can identify the parent compound at low concentrations. Detection windows vary with dose and individual factors.
No, cardarine has no approved medical uses in major jurisdictions. Early research explored metabolic conditions, but those programs were discontinued. It is not a registered treatment for any disease.
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.