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Identity And Pharmacological Classification — Evidence Review

By Editorial Desk · published 2026-05-28 · last reviewed 2026-07-02 · Faq

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

This page was last updated on 2026-07-02 and is reviewed periodically as new material appears.

Identity and Pharmacological Classification

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 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.

Preclinical Findings and Safety Signals

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.

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.

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.

Mechanism and Detection

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

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.

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Detection and Regulatory Landscape

Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.

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.

Background and Regulatory History

Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.

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.

Identity and Regulatory Status

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.

Notes from published material

Present data show that (R)-phenylpiracetam increases motivation, i.e., the work load, which animals are willing to perform to obtain more rewarding food. At the same time consumption of freely available normal food does not increase. Generally this indicates that (R)-phenylpiracetam increase motivation [...] The effect of (R)-phenylpiracetam is much stronger than that of methylphenidate and amphetamine.

Antimicrobial peptide resistance and lipid A acylation protein PagP is a family of several bacterial antimicrobial peptide resistance and lipid A acylation (PagP) proteins. The bacterial outer membrane enzyme PagP transfers a palmitate chain from a phospholipid to lipid A. In a number of pathogenic Gram-negative bacteria, PagP confers resistance to certain cationic antimicrobial peptides produced during the host innate immune response.

== Applications == FTIR can be used in all applications where a dispersive spectrometer was used in the past (see external links). In addition, the improved sensitivity and speed have opened up new areas of application. Spectra can be measured in situations where very little energy reaches the detector. Fourier transform infrared spectroscopy is used in geology, chemistry, materials, botany and biology research fields.

Sources: en.wikipedia.org

Background from the literature

==== Military ==== The war exposed shortages in the US' weapons stockpiles, calling into question years of defense investment after the September 11 attacks. After less than five months of the war, US was already running out of ammunition against a middle-tier adversary. This could limit US ability to deter other adversaries, including Russia and China. Former secretary of defense Leon Panetta described this as a "dangerous moment". The US has no longer the capacity to deter a future conflict in the South China Sea and elsewhere. The United States consumed more than half of its Patriot missiles used to intercept Iranian missiles and drones. The stockpiles limitation has reportedly turned into a key determinant for continuation or expansion of the conflict. As of 5 August 2026, the US had reportedly used roughly 80% of its THAAD missiles in the war. The United States burned through "virtually all" of its PrSM and ATACMS munitions, and "a little less than half" of its global Tomahawk supply, according to a Reuters report on 4 August. On 6 August, Trump and Hegseth clashed at Camp David over "extreme missile shortages", according to Washington Post. Trump claimed he felt misled, while Hegseth put the blame on his deputy, Stephen Feinberg. Trump denied the aforementioned report, and threatened long prison sentences for anyone leaking information about military supplies. As of 14 August, the US had reportedly lost around 25% of their Reaper drones in the war.

== Definition == In animal studies, maximum span is often taken to be the mean life span of the most long-lived 10% of a given cohort. By another definition, however, maximum life span corresponds to the age at which the oldest known member of a species or experimental group has died. Calculation of the maximum life span in the latter sense depends upon the initial sample size. Maximum life span contrasts with mean life span (average life span, life expectancy), and longevity. Mean life span varies with susceptibility to disease, accident, suicide and homicide, whereas maximum life span is determined by "rate of aging". Longevity refers only to the characteristics of the especially long lived members of a population, such as infirmities as they age or compression of morbidity, and not the specific life span of an individual.

== Use in astronomy == While the total number of "catalytic" nuclei are conserved in the cycle, in stellar evolution the relative proportions of the nuclei are altered. When the cycle is run to equilibrium, the ratio of the carbon-12/carbon-13 nuclei is driven to 3.5, and nitrogen-14 becomes the most numerous nucleus, regardless of initial composition. During a star's evolution, convective mixing episodes moves material, within which the CNO cycle has operated, from the star's interior to the surface, altering the observed composition of the star. Red giant stars are observed to have lower carbon-12/carbon-13 and carbon-12/nitrogen-14 ratios than do main sequence stars, which is considered to be convincing evidence for the operation of the CNO cycle.

Sources: en.wikipedia.org

Further detail

== Early years and education == Muñoz, was born in Lima, Peru. In 1996, she attended the National University of San Marcos (UNMSM), where she earned her pharmaceutical degree. While studying, she developed an interest in the field of nutrition. She earned a master's degree in biochemistry and nutrition, and earned a PhD in Pharmacy and Biochemistry from the National University of San Marcos (UNMSM) in 2006.

Aerodynamic theory does not predict that bumblebees should not be able to fly; the physics of insect flight is quite well understood. The misconception appears to come from a calculation based on a fixed-wing aircraft mentioned in a 1934 book, and was further popularized in the 2007 film Bee Movie. While certainly critical to the pollination of many plant species, European honey bees are not essential to human food production, despite claims that without their pollination, humanity would starve or die out "within four years". In fact, the most essential staple food crops on the planet, like wheat, maize, rice, soybeans and sorghum, are wind-pollinated or self-pollinating, and only slightly over 10% of the total human diet of plant crops is dependent upon insect pollination. Most bees do not die if they use their sting. This happens for only a small minority of species, including the honey bee, when they sting mammals. They survive when they sting other insects. Cockroaches would not be the only organisms capable of surviving in an environment contaminated with nuclear fallout. While cockroaches have a much higher radiation resistance than vertebrates, they are not immune to radiation poisoning, nor are they exceptionally radiation-resistant compared to other insects or smaller living beings. For comparison, parasitic wasps, tardigrades, and bacteria such as Deinococcus radiodurans have much higher radiation resistance compared to cockroaches.

=== Fertility aid === One of the most damaged areas of the body following chemotherapy is typically the uterus. Following uterine damage due to cancer treatment, follicle damage makes it difficult for individuals to get pregnant even if viable ova are present. With bone marrow stem cell transplants, chemotherapy patients have been able to increase their fertility as follicle damage is repaired. As follicles are necessary for ovum attachment to the endometrium, it is important for these areas to be repaired in order to increase fertility. For individuals who have sustained egg and follicle damage, IVF has been found to be more effective following bone marrow stem cell transplantation. One human clinical case has shown improvements of uterine lining thickness and overall endometrium repair following bone marrow stem cell transplantation. This repair allowed for the patient to successfully become pregnant and carry to term. Additional repairs following bone marrow stem cell transplant to the endometrium include increased vascularity and iron levels, with egg implantation clustering around areas with high blood flow.

==== Metals as catalytic sites ==== The metals in the MOF structure often act as Lewis acids. The metals in MOFs often coordinate to labile solvent molecules or counter ions which can be removed after activation of the framework. The Lewis acidic nature of such unsaturated metal centers can activate the coordinated organic substrates for subsequent organic transformations. The use of unsaturated metal centers was demonstrated in the cyanosilylation of aldehydes and imines by Makoto Fujita and coworkers in 2004. They reported MOF of composition {[Cd(4,4′-bpy)2(H2O)2] • (NO3)2 • 4H2O} which was obtained by treating linear bridging ligand 4,4′-bipyridine (bpy) with Cd(NO3)2. The Cd(II) centers in this MOF possess a distorted octahedral geometry having four pyridines in the equatorial positions, and two water molecules in the axial positions to form a two-dimensional infinite network. On activation, two water molecules were removed leaving the metal centers unsaturated and Lewis acidic. The Lewis acidic character of metal center was tested on cyanosilylation reactions of imine where the imine gets attached to the Lewis-acidic metal centre resulting in higher electrophilicity of imines. For the cyanosilylation of imines, most of the reactions were complete within 1 h affording aminonitriles in quantitative yield. Kaskel and coworkers carried out similar cyanosilylation reactions with coordinatively unsaturated metals in three-dimensional (3D) MOFs as heterogeneous catalysts.

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.

What did animal studies show?

Rodent studies reported increased endurance and fat oxidation after GW501516 exposure. Long-term studies also found higher rates of some tumors, which led to halted development.

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