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Identity And Pharmacological Classification — Research Overview

By Editorial Desk · published 2025-09-04 · last reviewed 2025-10-11 · Guide

The short version of GW501516 fits in a sentence. The long version — which is the one that helps — is below.

Reviewed 2025-10-11. Anything still debated is marked as such rather than presented as settled.

Identity and Pharmacological Classification

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 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.

Detection, Stability, and Quality

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.

Stability of GW501516 depends on form, temperature, light exposure, and moisture. Solid reference material is typically stored frozen or refrigerated in a desiccator and protected from light. Solutions in organic solvents such as dimethyl sulfoxide are often kept frozen in aliquots to reduce freeze-thaw cycling. Aqueous solubility is low, so aqueous stock solutions can be difficult to prepare without cosolvents. Degradation may appear as changes in chromatographic purity or mass spectral signal. Stability studies are needed to establish shelf life for any specific preparation.

Cardarine at a glance

PropertyValueNotes
Chemical classPPARδ agonistNot an anabolic steroid.
Common synonymsGW501516, GW-1516Cardarine is an informal name.
AppearanceWhite to off-white powderTypical for research-grade solid.
Solubility classPoorly soluble in water; soluble in some organic solventsSuch as DMSO or ethanol in laboratory settings.
Typical storage temperatureCool, dry, protected from lightSpecific conditions vary by supplier and form.

Background and Regulatory Status

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.

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.

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Mechanism and Safety Research

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.

Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.

Regulation and Detection

Cardarine has no approved therapeutic indication and is not marketed as a medicine. The World Anti-Doping Agency lists GW501516 as a prohibited substance at all times, covering both in-competition and out-of-competition periods. National laws vary: some countries treat it as an unapproved drug subject to import controls, while others have specific restrictions on sale for human consumption. It is often sold as a research chemical, a label that does not imply safety or legality. Enforcement actions have targeted online vendors and shipments.

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.

Identity and Regulatory Status

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.

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.

Notes from published material

=== OpenTag === DASH7 Mode 2 developers benefit from the open-source firmware library called OpenTag, which provides developers with a "C"-based environment in which to develop DASH7 applications quickly. So in addition to DASH7 (ISO 18000-7) being an open source, ISO standard, OpenTag is an open-source stack that is quite unlike other wireless sensor networking (e.g. ZigBee) and active RFID (e.g. proprietary) options elsewhere in the marketplace today. Even though OpenTag is an open-source project, people may not be able to use it free of charge. As of August 2015, there is no evidence to suggest that OpenTag bears a royalty, although current versions of OpenTag license Archived 2013-12-31 at the Wayback Machine do include a provision permitting RAND licensing.

The collapse of birthrates among blacks and (non-white) Hispanics, down 50%, was largely responsible for this development. However, their birthrates remained, on average, twice as high as those of their white counterparts. The birth rates of teenage Asians and Pacific Islanders were even lower, about half that of whites. In a 2014 paper, economists Melissa S. Kearney and Phillip B. Levine howed that popular TV programs depicting the reality of teenage parenthood, such as MTV's 16 and Pregnant and its Teen Mom sequels, have played a significant role in the reduction of teenage childbearing. Researchers from the Guttmacher Institute showed that the fall in teenage birthrates is likely not due to terminated pregnancies. The number of abortions remained the same or decreased in all U.S. states except for Vermont. This contradicts the historically negative correlation between birthrates and abortions. Modern youths also have better access to contraception than did their predecessors when they were at the same age. A CDC analysis found that the rates of teens using a long-acting and reversible method of contraception, such as an intrauterine device (IUD), jumped from 0.4% in 2005 to 7.1% in 2013. The teen birthrate continues to fall in the late 2010s, down to 17.4 births per 1000 in 2018. In 2022, it fell to 13.5, the lowest on record.

== Role of the clinical data manager in a clinical trial == Job profile acceptable in CDM: clinical researcher, clinical research associate, clinical research coordinator etc. The clinical data manager plays a key role in the setup and conduct of a clinical trial. The data collected during a clinical trial form the basis of subsequent safety and efficacy analysis which in turn drive decision making on product development in the pharmaceutical industry. The clinical data manager is involved in early discussions about data collection options and then oversees development of data collection tools based on the clinical trial protocol. Once subject enrollment begins, the data manager ensures that data are collected, validated, complete, and consistent. The clinical data manager liaises with other data providers (e.g. a central laboratory processing blood samples collected) and ensures that such data are transmitted securely and are consistent with other data collected in the clinical trial. At the completion of the clinical trial, the clinical data manager ensures that all data expected to be captured have been accounted for and that all data management activities are complete. At this stage, the data are declared final (terminology varies, but common descriptions are "Database Lock", “Data Lock” and "Database Freeze"), and the clinical data manager transfers data for statistical analysis.

In protein design, the target structure (or structures) of the protein are known. However, a rational protein design approach must model some flexibility on the target structure in order to increase the number of sequences that can be designed for that structure and to minimize the chance of a sequence folding to a different structure. For example, in a protein redesign of one small amino acid (such as alanine) in the tightly packed core of a protein, very few mutants would be predicted by a rational design approach to fold to the target structure, if the surrounding side-chains are not allowed to be repacked. Thus, an essential parameter of any design process is the amount of flexibility allowed for both the side-chains and the backbone. In the simplest models, the protein backbone is kept rigid while some of the protein side-chains are allowed to change conformations. However, side-chains can have many degrees of freedom in their bond lengths, bond angles, and χ dihedral angles. To simplify this space, protein design methods use rotamer libraries that assume ideal values for bond lengths and bond angles, while restricting χ dihedral angles to a few frequently observed low-energy conformations termed rotamers. Rotamer libraries are derived from the statistical analysis of many protein structures. Backbone-independent rotamer libraries describe all rotamers. Backbone-dependent rotamer libraries, in contrast, describe the rotamers as how likely they are to appear depending on the protein backbone arrangement around the side chain.

From the mid-1960s onward, Ramachandran continued studying crystallography, including the conformation of peptides including types of β-turns, conformation of prolyl residues, cis-peptide units, occurrence and need for non-planarity of the peptides, NMR coupling constants and peptides containing L and D residues, among other tops. He was awarded the prestigious Jawarharlal Nehru Fellowship in 1968 for research on Protein and Polypeptide Conformation; he was one of its first recipients. Ramachandran can be credited for bringing together into the one field of molecular biophysics the then disparate fields of X-ray crystallography, peptide synthesis, NMR and other optical studies, and physico-chemical experimentation. In 1970, he founded the Molecular Biophysics Unit at the Indian Institute of Science which was later known as the Centre of Advanced Study in Biophysics. Ramachandran and A.V. Lakshminarayanan developed convolution-backprojection algorithms which greatly improved the quality and practicality of results obtainable by x-ray tomography. Compared to previously used methods, their algorithms considerably reduced computer processing time for image reconstruction, as well as providing more numerically accurate images. As a result, commercial manufacturers of x-ray tomographic scanners started building systems capable of reconstructing high resolution images that were almost photographically perfect. In 1971, they published their research in PNAS. In 1981, Ramachandran became a founding member of the World Cultural Council.

Sources: en.wikipedia.org

Further detail

Membranoproliferative GN (MPGN), also known as mesangiocapillary glomerulonephritis, is characterised by an increase in the number of cells in the glomerulus, and alterations in the glomerular basement membrane. These forms present with the nephritic syndrome, hypocomplementemia, and have a poor prognosis. Three subtypes have been proposed:

243Am(15N,xn)258−xNo (x=4) This reaction was studied in 1966 at the FLNR. The team were able to detect 250Fm using chemical techniques and determined an associated half-life significantly higher than the reported 3 s by Berkeley for the supposed parent 254No. Further work later the same year measured 8.1 MeV alpha particles with a half-life of 30–40 s.

== Reproduction and development == Eggs are laid in an ootheca which the female carries out the end of her abdomen for varying lengths of time. When ready she either deposits it on the ground, or attaches it to an object. The hardened ootheca helps protect the developing eggs. Optimal temperature range and patterns effect the hatch rate. Research has found that the best hatch rates occur when temperature alternates between 5°C and 30°C (the ootheca were left at the lower temperature for seven days, then left at the higher temperature for the remainder of development), the development time averages 44 days. Less effective temperature combinations may result in longer development times, alternating 10°C and 25°C, averages 61 days. E. sinensis is considered to have a flexible life cycle, as length can vary from 1 to 3 years, depending on latitude the population is from. Females can survive up to 30 months, while males lifespan is much shorter. The variable lifespans correlates to varying number of instars, 7 to 9, or 9 to 11. Males generally develop faster than females. The species takes longer to develop at lower temperatures.

Meanwhile, the regulatory approach favored by Liu would help maintain points of contact between Han and indigenous people, and, according to Wang Zhuo, would make them "more accustomed to Hanization." Liu did not personally reiterate those statements, although this was an argument presented by his faction and criticized by their opponents. In the end, Liu's side prevailed, and wula would not be fully abolished until the establishment of communist rule decades later. Liu did abolish several minor corvée duties, including the provision of firewood, fodder, tea, and miscellaneous services such as sweeping, but these were distinct from the transport corvée. Liu defended the wula system's continued existence in a 1939 conference: "if the people think the corvée is an oppressive policy, then they are wrong." Liu's 1990 biography mentions this as emblematic of the limits of warlord-driven reform compared to the wula's complete abolition under Mao in 1959.

Sources: en.wikipedia.org

Supporting material

== Mechanism of action == Precise mechanism of antidepressant activity of SSRIs remains somewhat uncertain, but a number of biochemical functions associated with SSRI treatment have been established. SSRIs primarily inhibit SERT in the brain and have negligible effects on DAT and NET. The SSRIs also have less affinity for α1, α2, H1 and muscarinic receptors, which might explain the differences of adverse events between TCAs and SSRIs. Although SSRIs arrive rapidly to the brain after administration and the effects on 5-HT re-uptake can be measured instantly, it takes about 2–4 weeks to get therapeutic effects. The SSRIs have very high and selective affinity for SERT and after administration they inhibit SERT immediately. SERT inhibition is implicated in the antidepressant activity of SSRIs. 70-80% inhibition of SERT is usually necessary to induce antidepressant effects and higher dosage does not induce greater antidepressant effects for average patients. Higher dosage does, however, increase the incidence and severity of adverse events associated with excessive 5-HT re-uptake inhibition.

Transporter competition: Many GalNAc-conjugated siRNA drugs (e.g., inclisiran, givosiran, lumasiran) are taken up by hepatocytes via the asialoglycoprotein receptor (ASGPR). Co-administration of agents that saturate or alter this receptor pathway may affect hepatic delivery of the siRNA payload. Carrier protein binding: Some oligonucleotide drugs bind serum albumin or lipoproteins. Competition with highly protein-bound small molecules could alter free-drug concentrations. Indirect CYP modulation: siRNA drugs that silence transcription factors controlling CYP gene expression (e.g., silencing of PCSK9 influences LXR/SREBP pathways) may indirectly alter CYP expression in co-treated patients. On-target miRNA network perturbation: Because endogenous microRNA (miRNA) regulates the expression of drug-metabolizing enzymes and transporters, therapeutic oligonucleotides that modulate miRNA activity can produce secondary DDIs via altered enzyme expression rather than direct enzyme binding.

=== Birds === Birds' unique circulatory lungs also promote efficient use of oxygen at low partial pressures of O2. These two adaptations reinforce each other and account for birds' remarkable high-altitude performance. This was specifically found in hummingbirds that inhabit the Andes. Hummingbirds already expend a lot of energy and thus have high oxygen demands and yet Andean hummingbirds have been found to thrive in high altitudes. Non-synonymous mutations in the hemoglobin gene of multiple species living at high elevations (Oreotrochilus, A. castelnaudii, C. violifer, P. gigas, and A. viridicuada) have caused the protein to have less of an affinity for inositol hexaphosphate (IHP), a molecule found in birds that has a similar role as 2,3-BPG in humans; this results in the ability to bind oxygen in lower partial pressures.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine also known as?

Cardarine is commonly known as GW501516 or GW-1516. These names refer to the same synthetic compound. It is not a brand-name approved medicine.

Is cardarine a steroid?

No, cardarine is not a steroid. It is classified as a PPARδ agonist. Its structure and receptor target differ from anabolic steroids.

Has cardarine been approved for human use?

No regulatory agency has approved cardarine as a medicine. It was investigated in early research but development was discontinued. It is not available as a prescription drug.

How is cardarine measured in biological samples?

LC-MS/MS is common, often after sample cleanup. The assay targets GW501516 or its metabolites.

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