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Identity And Pharmacological Classification — Reference Sheet

By Editorial Desk · published 2026-06-10 · last reviewed 2026-07-15 · Topic

A practical reference on Cardarine: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

Reviewed 2026-07-15. 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.

Background and Regulatory Status

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.

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.

Regulation and Detection

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.

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.

Related pages on this site

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.

Reference notes

The quality of gamma-camera PET imaging is lower, and the scans take longer to acquire. Alternative methods of medical imaging include single-photon emission computed tomography (SPECT), computed tomography (CT), magnetic resonance imaging (MRI) and functional magnetic resonance imaging (fMRI), and ultrasound. SPECT is an imaging technique similar to PET that uses radioligands to detect molecules in the body.

=== Tertiary lymphoid organs === Tertiary lymphoid organs (TLOs) are abnormal lymph node-like structures that form in peripheral tissues at sites of chronic inflammation, such as chronic infection, transplanted organs undergoing graft rejection, some cancers, and autoimmune and autoimmune-related diseases. TLOs are often characterized by CD20+ B cell zone, which is surrounded by CD3+ T cell zone, similar to the lymph follicles in secondary lymphoid organs (SLOs) and are regulated differently from the normal process whereby lymphoid tissues are formed during ontogeny, being dependent on cytokines and hematopoietic cells, but still drain interstitial fluid and transport lymphocytes in response to the same chemical messengers and gradients. Mature TLOs often have an active germinal center, surrounded by a network of follicular dendritic cells (FDCs). Although the specific composition of TLOs may vary, within the T cell compartment, the dominant subset of T cells is CD4+ T follicular helper (TFH) cells, but certain number of CD8+ cytotoxic T cells, CD4+ T helper 1 (TH1) cells, and regulatory T cells (Tregs) can also be found within the T cell zone. The B cell zone contains two main areas. The mantle is located at the periphery and composed of naive immunoglobulin D (IgD)+ B cells surrounding the germinal centre. The latter is defined by the presence of proliferating Ki67+CD23+ B cells and a CD21+ FDC network, as observed in SLOs. TLOs typically contain far fewer lymphocytes, and assume an immune role only when challenged with antigens that result in inflammation.

Dystrophinopathy refers to a spectrum of diseases due to mutations in the DMD gene, which encodes for the dystrophin protein found in muscle. The severe end of the spectrum includes Duchenne muscular dystrophy (DMD), Becker muscular dystrophy (BMD), and DMD-associated dilated cardiomyopathy. The mild end of the spectrum includes asymptomatic increases in serum creatine kinase and muscle cramps with myoglobinuria. Because dystrophin is located on the X chromosome, dystrophinopathy mainly affects males, whereas females range from being carriers, to having delayed-onset and mild disease, to having severe DMD.

The paper for holding the tobacco blend may vary in porosity to allow ventilation of the burning embers or contain materials that control the burning rate of the cigarette and stability of the produced ash. The papers used in tipping the cigarette (forming the mouthpiece) and surrounding the filter stabilize the mouthpiece from saliva and moderate the burning of the cigarette, as well as the delivery of smoke with the presence of one or two rows of small laser-drilled air holes.

This is a nice example as affinity purification is used to purify the initial GST-fusion protein, to remove the undesirable anti-GST antibodies from the serum and to purify the target antibody. Monoclonal antibodies can also be selected to bind proteins with great specificity, where protein is released under fairly gentle conditions. This can become of use for further research in the future. A simplified strategy is often employed to purify antibodies generated against peptide antigens. When the peptide antigens are produced synthetically, a terminal cysteine residue is added at either the N- or C-terminus of the peptide. This cysteine residue contains a sulfhydryl functional group which allows the peptide to be easily conjugated to a carrier protein (e.g. Keyhole limpet hemocyanin (KLH)). The same cysteine-containing peptide is also immobilized onto an agarose resin through the cysteine residue and is then used to purify the antibody. Most monoclonal antibodies have been purified using affinity chromatography based on immunoglobulin-specific Protein A or Protein G, derived from bacteria. Immunoaffinity chromatography with monoclonal antibodies immobilized on monolithic column has been successfully used to capture extracellular vesicles (e.g., exosomes and exomeres) from human blood plasma by targeting tetraspanins and integrins found on the surface of the EVs. Immunoaffinity chromatography is also the basis for immunochromatographic test (ICT) strips, which provide a rapid means of diagnosis in patient care.

Sources: en.wikipedia.org

Notes from published material

=== DNA binding === α-Helices have particular significance in DNA binding motifs, including helix-turn-helix motifs, leucine zipper motifs and zinc finger motifs. This is because of the convenient structural fact that the diameter of an α-helix is about 12 Å (1.2 nm) including an average set of sidechains, about the same as the width of the major groove in B-form DNA, and also because coiled-coil (or leucine zipper) dimers of helices can readily position a pair of interaction surfaces to contact the sort of symmetrical repeat common in double-helical DNA. An example of both aspects is the transcription factor Max (see image at left), which uses a helical coiled coil to dimerize, positioning another pair of helices for interaction in two successive turns of the DNA major groove.

== Use and effects == In his book PiHKAL (Phenethylamines I Have Known and Loved) and other publications, Alexander Shulgin lists 3,4-DMA's dose as "a few hundred milligrams" (route unspecified) and its duration as unknown. A dose of approximately 70 mg intravenously produced insignificant to slight psychoactive effects in two individuals. Conversely, a subsequent approximate 700 mg dose intravenously in the same two people produced a definite mescaline-like state, including visual hallucinations (e.g., geometric figures and occasional structured forms), visual distortions, after-images, feelings of unreality, paranoia, marked pupil dilation, and gross body tremors. Gordon Alles reported 3,4-DMA to be inactive at doses of 10 to 120 mg orally but active at 160 mg orally, with reported effects including increased blood pressure, slight pupil dilation, lacrimation, and gastrointestinal uneasiness. He estimated that the response at this dose was equivalent to that of about 60 to 80 mg 3,4-methylenedioxyamphetamine (MDA), suggesting that 3,4-DMA's potency may be about 2- to 3-fold lower than that of MDA and may fall midway between that of MDA and mescaline. Alternatively, according to Shulgin, 3,4-DMA may have comparable potency to mescaline, with an effective dose of perhaps 300 to 400 mg orally, or may be less potent than mescaline. Richard Glennon suggested that the dose may be 400 to 700 mg orally.

=== Plant === Many plant expression vectors are based on the Ti plasmid of Agrobacterium tumefaciens. In these expression vectors, DNA to be inserted into plant is cloned into the T-DNA, a stretch of DNA flanked by a 25-bp direct repeat sequence at either end, and which can integrate into the plant genome. The T-DNA also contains the selectable marker. The Agrobacterium provides a mechanism for transformation, integration of into the plant genome, and the promoters for its vir genes may also be used for the cloned genes. Concerns over the transfer of bacterial or viral genetic material into the plant however have led to the development of vectors called intragenic vectors whereby functional equivalents of plant genome are used so that there is no transfer of genetic material from an alien species into the plant. Plant viruses may be used as vectors since the Agrobacterium method does not work for all plants. Examples of plant virus used are the tobacco mosaic virus (TMV), potato virus X, and cowpea mosaic virus. The protein may be expressed as a fusion to the coat protein of the virus and is displayed on the surface of assembled viral particles, or as an unfused protein that accumulates within the plant. Expression in plant using plant vectors is often constitutive, and a commonly used constitutive promoter in plant expression vectors is the cauliflower mosaic virus (CaMV) 35S promoter.

== Plasma proteins == Plasma contains a large variety of proteins including albumin, immunoglobulins, and clotting proteins such as fibrinogen. Albumin constitutes about 60% of the total protein in plasma and is present at concentrations between 35 and 55 mg/mL. It is the main contributor to osmotic pressure of the blood and it functions as a carrier molecule for molecules with low water solubility such as lipid-soluble hormones, enzymes, fatty acids, metal ions, and pharmaceutical compounds. Albumin is structurally stable due to its seventeen disulfide bonds and unique in that it has the highest water solubility and the lowest isoelectric point (pI) of the plasma proteins. Due to the structural integrity of albumin it remains stable under conditions where most other proteins denature.

Sources: en.wikipedia.org

Background from the literature

The periodic table, also known as the periodic table of the elements, is an ordered arrangement of the chemical elements into rows ("periods") and columns ("groups"). An icon of chemistry, the periodic table is also widely used in physics and other sciences. It is a depiction of the periodic law, which states that when the elements are arranged in order of their atomic numbers an approximate recurrence of their properties is evident. The table is divided into four roughly rectangular areas called blocks. Elements in the same group tend to show similar chemical characteristics. Vertical, horizontal and diagonal trends characterize the periodic table. Metallic character increases going down a group and from right to left across a period. Nonmetallic character increases going from the bottom left of the periodic table to the top right. The first periodic table to become generally accepted was that of the Russian chemist Dmitri Mendeleev in 1869; he formulated the periodic law as a dependence of chemical properties on atomic mass. As not all elements were then known, there were gaps in his periodic table, and Mendeleev successfully used the periodic law to predict some properties of some of the missing elements. The periodic law was recognized as a fundamental discovery in the late 19th century. It was explained early in the 20th century, with the discovery of atomic numbers and associated pioneering work in quantum mechanics, both ideas serving to illuminate the internal structure of the atom. A recognisably modern form of the table was reached in 1945 with Glenn T.

== Career == Middleton's cake-making business, now defunct, was inspired by reading that a mother's baking is a highly evocative childhood memory. He supplied baking kits so home bakers would be able to get all the ingredients in one place for adventurous creations such as "football cakes". He started baking in the family kitchen and expanded into a freight container and converted barns. Themed birthday cake baking kits were distributed by his parents' company, Party Pieces. Themed cakes were later provided for companies such as Jigsaw, 3 and Ralph Lauren. Middleton caused "shudders" at Buckingham Palace after taking part in a Hello magazine photoshoot for which he was commissioned to bake 21 cakes commemorating its 21st birthday, each iced with one of the magazine's front covers – amongst them, several members of the royal family, including Diana, Princess of Wales. The business won Smarta 100 and Haines Watts Young Entrepreneur awards. In April 2011, he registered three businesses: Nice Cakes, Nice Wine, and Nice Group London and planned to expand the Cake Kit Company. The Cake Kit Company was dissolved in 2015. In May 2020, Middleton launched Ella & Co, a mail order dog food company that offers freeze-dried, raw, organic dog food.

== Comparison == LADA differs from both type 1 and type 2 diabetes. It has a later onset and slower progression than classic type 1 diabetes and is characterized by autoimmune-mediated β-cell destruction, while also exhibiting features of type 2 diabetes due to progressive insulin deficiency over time. Genetic testing can help distinguish LADA from monogenic forms of diabetes (e.g., MODY), which lack autoimmune markers and do not share the same genetic profile.

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.

Is cardarine approved for human use?

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.

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