If you have been reading about LC-MS/MS 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 2025-08-10. Numbers and descriptions here follow the published literature rather than marketing material.
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.
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.
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.
| Property | Value | Notes |
|---|---|---|
| Solubility | Soluble in dimethyl sulfoxide and some organic solvents; practically insoluble in water | Solvent choice affects laboratory handling |
| Typical storage | -20 °C, desiccated, protected from light | Common condition for research samples |
| Analytical method | Liquid chromatography–tandem mass spectrometry (LC-MS/MS) | Used for identification and quantification in biological or product samples |
| Common synonyms | GW501516, GW-501516, GSK-516, Endurobol | Names found in research and anti-doping literature |
| Regulatory status | Unapproved therapeutic; prohibited in competitive sport | Status can vary by country and context |
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.
Analytical laboratories typically identify cardarine and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is a common matrix in anti-doping testing, while blood and tissue may be used in research settings. Detection windows depend on the assay, the sample matrix, and the compound's metabolism. Because cardarine is extensively metabolized, laboratories often target specific metabolites to improve sensitivity and confirmation. Reference standards are required for reliable quantification. Method validation includes checks for selectivity, linearity, and carryover.
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.
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.
=== Mechanism of action === Phencyclidine is a noncompetitive NMDA receptor antagonist that blocks the activity of the NMDA receptor to cause anaesthesia and analgesia without causing cardiorespiratory depression. NMDA is an excitatory receptor in the brain, when activated normally the receptor acts as an ion channel and there is an influx of positive ions through the channel to cause nerve cell depolarisation. Phencyclidine inhibits the NMDA receptor by binding to the specific PCP binding site located within the ion channel. The PCP binding site is near the magnesium blocking site, which may explain the similar inhibitory effects. Binding at the PCP site is mediated by two non-covalent interactions within the receptor: hydrogen bonding and hydrophobic interaction. Binding is also controlled by the gating mechanism of the ion channel. Because the PCP site is located within the ion channel, a coagonist such as glycine must bind and open the channel for PCP to enter, bind to the PCP site, and block the channel.
=== Economics === In the UK, trastuzumab emtansine was not recommended for use by the National Health Service by advisory body NICE, reportedly because an acceptable pricing agreement could not be reached with Roche. Originally it cost £5,900 a month. and NICE estimated it cost £166,000 per QALY (well over the usual maximum). It has been funded by the English NHS Cancer Drugs Fund but in January 2015 it was proposed to remove it from the approved list. After a secret discount was agreed by Roche the Cancer Drugs Fund will continue to fund it. In June 2017, the NHS Confederation and NHS Chief Executive Simon Stevens announced that the NHS would be offering trastuzumab emtansine to a limited number of women after striking a deal with Roche on the price.
== Antagonists == Becampanel CNQX Dasolampanel DNQX Fanapanel (MPQX) Kaitocephalin Kynurenic acid – endogenous ligand L-theanine NBQX 3,5-Dibromo-L-phenylalanine, a naturally occurring halogenated derivative of L-phenylalanine Perampanel Selurampanel Tezampanel Zonampanel
== See also == Oxides, e.g., Al2O3, CaO, Fe2O3, MgO, MnO, P2O5, K2O, SiO2 Carbonates: Na2CO3 (soda ash), K2CO3 (potash) Bicarbonates, e.g., NaHCO3 (baking soda) Sulfates: sulfate ash, according to Ph. Eur. Inductively coupled plasma emission spectrometry Atomic absorption spectroscopy
Sources: en.wikipedia.org
=== Diabetes mellitus === Today, the term "diabetes" most commonly refers to diabetes mellitus. Diabetes mellitus is itself an umbrella term for a number of different diseases involving problems processing sugars that have been consumed (glucose metabolism). Historically, this is the "diabetes" which has been associated with sugary urine (glycosuria).
== In nature == Numerous biomolecules exhibit the ability to dissolve certain metal cations. Thus, proteins, polysaccharides, and polynucleic acids are excellent polydentate ligands for many metal ions. Organic compounds such as the amino acids glutamic acid and histidine, organic diacids such as malate, and polypeptides such as phytochelatin are also typical chelators. In addition to these adventitious chelators, several biomolecules are specifically produced to bind certain metals (see next section). Virtually all metalloenzymes feature metals that are chelated, usually to peptides or cofactors and prosthetic groups. Such chelating agents include the porphyrin rings in hemoglobin and chlorophyll. Many microbial species produce water-soluble pigments that serve as chelating agents, termed siderophores. For example, species of Pseudomonas are known to secrete pyochelin and pyoverdine that bind iron. Enterobactin, produced by E. coli, is the strongest chelating agent known. The marine mussels use metal chelation, especially Fe3+ chelation with the Dopa residues in mussel foot protein-1 to improve the strength of the threads that they use to secure themselves to surfaces. In earth science, chemical weathering is attributed to organic chelating agents (e.g., peptides and sugars) that extract metal ions from minerals and rocks. Most metal complexes in the environment and in nature are bound in some form of chelate ring (e.g., with a humic acid or a protein).
=== Animal welfare citations by the United States Department of Agriculture === In June 2011, a report showed that improper housing conditions led to frostbite on the tails of many monkeys. In February 2012, the company was cited after a monkey died after being entangled by an enrichment device. In March 2012, the company was cited for housing a monkey in isolation for almost eight months.
Sources: en.wikipedia.org
It binds and activates PPARδ, a nuclear receptor that influences gene expression related to fatty acid metabolism and energy balance. This mechanism has been studied mainly in animals and cell models, not established as a safe human therapy.
No. It is not an anabolic-androgenic steroid; it is a synthetic PPARδ agonist. Because it is banned in sport, it is sometimes grouped with doping agents even though its chemical class differs from steroids.
Human data are limited and development was discontinued, so major effects and long-term risks are not well characterized. Some early studies examined metabolic markers, but they do not provide a basis for unsupervised use.
Anti-doping and clinical laboratories commonly use liquid chromatography-tandem mass spectrometry. The method can identify GW501516 and its metabolites in urine or blood. Detection depends on sample timing and the amount present.