A practical reference on Cardarine: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
Reviewed 2025-07-15. Anything still debated is marked as such rather than presented as settled.
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.
Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.
GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.
| 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 |
Anti-doping laboratories identify GW501516 and related metabolites using liquid chromatography coupled with tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be analyzed. The method targets the parent compound and phase I and phase II metabolites, which extend the detection window. Because the substance is prohibited at all times, athletes can be tested outside competition. Detection limits and windows depend on the assay, sample type, and individual metabolism.
Cardarine is frequently described as a fat-burning or endurance-enhancing supplement, but these claims exceed the available evidence. The compound is not a hormone, steroid, or selective androgen receptor modulator. Research articles discuss it as a tool compound for studying PPARδ biology, while anti-doping literature focuses on its abuse and detection. Quality of unapproved products is uncertain, and independent analyses have found impurities or incorrect labeling. Open questions include whether human cancer risk resembles that seen in rodents and how often non-athletes use the substance.
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.
Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.
Anti-doping laboratories identify GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the usual matrix, and detection can occur after the parent compound has cleared from blood. The exact detection window depends on dose, formulation, individual metabolism, and assay sensitivity. Because the compound is prohibited at all times, athletes are subject to testing in and out of competition. Analytical methods continue to improve as new metabolites and designer analogs are characterized.
=== Drug development === ITC can provide insights into drug development by charactering the affinity, selectivity, ligand-induced conformational changes, and drug partitioning into membranes. Binding affinity carries a huge importance in medicinal chemistry, as drugs need to bind to the protein effectively within a desired range. An exothermic binding process with a favorable enthalpy is considered a desirable characteristic for specific protein binders, as it indicates strong potential for optimization and high selectivity. However, determining enthalpy changes and optimization of thermodynamic parameters are hugely difficult when designing drugs. ITC troubleshoots this issue easily by deducing the binding affinity, enthalpic/entropic contributions and its binding stoichiometry.
== ANA subtypes == ANAs are found in many disorders, as well as some healthy individuals. These disorders include: systemic lupus erythematosus (SLE), rheumatoid arthritis, Sjögren syndrome, scleroderma, polymyositis, dermatomyositis, primary biliary cirrhosis, drug induced lupus, autoimmune hepatitis, multiple sclerosis, discoid lupus, thyroid disease, antiphospholipid syndrome, juvenile idiopathic arthritis, psoriatic arthritis, juvenile dermatomyositis, idiopathic thrombocytopaenic purpura, infection and cancer. These antibodies can be subdivided according to their specificity, and each subset has different propensities for specific disorders.
The liver synthesizes and stores around 100g of glycogen via glycogenesis, the formation of glycogen from glucose. When needed, the liver releases glucose into the blood by performing glycogenolysis, the breakdown of glycogen into glucose. The liver is also responsible for gluconeogenesis, which is the synthesis of glucose from certain amino acids, lactate, or glycerol. Adipose and liver cells produce glycerol by breakdown of fat, which the liver uses for gluconeogenesis. Liver also does glyconeogenesis which is synthesis of glycogen from lactic acid.
mass number (A) Also atomic mass number or nucleon number. The total number of protons and neutrons (together known as nucleons) within the nucleus of an atom. It determines the atomic mass of the atom. Mass number varies between different isotopes of the same chemical element, and is often included either after the element's name (as in carbon-12) or as a superscript to the left of the element's symbol (as in 12C) to identify a specific isotope.
During the colonial period, slavery became legal in all the Thirteen colonies, and by 1770 it provided the main labor force in the large-scale, agriculture-dependent economies of the Southern Colonies from Maryland to Georgia. The practice began to be significantly questioned during the American Revolution, and spurred by an active abolitionist movement that had reemerged in the 1830s, states in the North enacted laws to prohibit slavery within their boundaries. At the same time, support for slavery had strengthened in Southern states, with widespread use of inventions such as the cotton gin (1793) having made slavery immensely profitable for Southern elites. The United States annexed the Republic of Texas in 1845, and the 1846 Oregon Treaty led to U.S. control of the present-day American Northwest. Dispute with Mexico over Texas led to the Mexican–American War (1846–1848). After the victory of the U.S., Mexico recognized U.S. sovereignty over Texas, New Mexico, and California in the 1848 Mexican Cession; the cession's lands also included the future states of Nevada, Colorado and Utah. The California gold rush of 1848–1849 spurred a huge migration of white settlers to the Pacific coast, leading to even more confrontations with Native populations. One of the most violent, the California genocide of thousands of Native inhabitants, lasted into the mid-1870s. Additional western territories and states were created.
Sources: en.wikipedia.org
==== Activity-based Profiling ==== To achieve functional degradomics, the enzymatic activity of proteases must be analyzed. Methods have been developed to distinguish the proteolytic activity of different enzymes in biological samples and separate active proteases from their inactive forms, namely zymogen precursors and those proteases bound by inhibitors. Two techniques are activity-based probes (ABPs) and Proteolytic Signature Peptides (PSPs). ABP molecules serve as probes to irreversibly bind only to active proteases and ignore their zymogen precursors and inhibited proteases. Placing a reactive group and a recognizable tag feature on the same molecule using a linker moiety gives an ABP molecule its structure. The reactive molecule, designed after protease inhibitor mechanisms, lends ABPs their specificity towards targeting active proteases. Once bound, the reactive group acts much like an irreversible inhibitor to the protease. Depending on the nature of the tag moiety, the ABP-protease complex can then be visualized or retrieved from biological samples for further studies of localization and quantification. Limitations including difficult production, specificity, stability, and toxicity hamper ABP development but these probes have proved useful in revealing protease biological activity and remain a promising avenue in degradomic technology. PSPs do not depend on targeting active proteases with tagged compounds but rather on quantitative proteomics using stable isotope labeled standard peptides.
While significant progress has been made in the sophistication of calorimeters since the review of this subject in 1989, the conclusions reached by the reviewers today are similar to those found in the 1989 review.
==== Other territories ==== Darbar grossed over ₹200 crore worldwide in the 11 days after its release. The film grossed US$400,000 on its opening day in the United States. In its opening weekend, Darbar earned $1 million (₹7.09 crore) in the US. Darbar earned approximately ₹70 crore in the overseas market in the first 11 days of its release. Darbar entered the Top Five of the worldwide box office for the weekend ending 12 January 2020, following an estimated global opening of US$21.2 million.
=== Anti-human globulin cross-matching === The AHG crossmatch is done by incubating the recipient serum/plasma with the donor's red blood cells and adding anti-human globulin. It is essentially an indirect Coomb's test. It is also called "full cross-matching", "IAT cross-matching" and "Coomb's cross-matching".
Sources: en.wikipedia.org
===== Phase I ===== During phase I metabolism, mitragynine undergoes hydrolysis of the methylester group on C16 as well as o-demethylation of both methoxy groups on positions 9 and 17. Following this step, oxidation and reduction reactions convert aldehyde intermediates into alcohols and carboxylic acids. P450 metabolic enzymes are known to facilitate the phase I metabolism of mitragynine which reportedly has an inhibitory effect on multiple P450 enzymes, raising the possibility of adverse drug interactions.
== History == The effectiveness of velmanase alfa was evaluated in participants with alpha-mannosidosis in a phase III multicenter, randomized, double-blind, placebo-controlled, parallel group study. The trial evaluated the efficacy of velmanase alfa over 52 weeks at a dose of 1 mg/kg given weekly as an intravenous infusion. A total of 25 participants were enrolled (14 males, 11 females), including 13 adult participants (age range: ≥18 to 35 years; mean: 25 years) and 12 pediatric participants (age range: ≥6 to <18 years; mean: 11 years); all participants were White. Fifteen participants (8 adult and 7 pediatric) received velmanase alfa and 10 participants (5 adult and 5 pediatric) received placebo.
== Miscellaneous nomenclature == Any non-racemic chiral substance is called scalemic. Scalemic materials can be enantiopure or enantioenriched. A chiral substance is enantiopure when only one of two possible enantiomers is present so that all molecules within a sample have the same chirality sense. Use of homochiral as a synonym is strongly discouraged. A chiral substance is enantioenriched or heterochiral when its enantiomeric ratio is greater than 50:50 but less than 100:0. Enantiomeric excess or e.e. is the difference between how much of one enantiomer is present compared to the other. For example, a sample with 40% e.e. of R contains 70% R and 30% S (70% − 30% = 40%).
=== Proposed high-capacity version === A "minimum-change" development of the Il-86, stated to have been designated Il-86V, was test-flown on 1 June 1982 and was ready for service by 27 April 1985. It was said to have 450 seats, with the underfloor vestibules fitted with seats and possible changes to main-deck seating. The version is not known to have entered passenger service but may have been used by the military.
microvillus A small, slender, tubular cytoplasmic projection, generally 0.2–4 micrometres long and 0.1 micrometres in diameter, protruding from the surface of some animal cells and supported by a central core of microfilaments. When present in large numbers, such as on epithelial cells lining the respiratory and alimentary tracts, they form a dense brush border which presumably serves to increase each cell's absorptive surface area.
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.
It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.