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Identity And Pharmacological Classification — Deep Dive

By Editorial Desk · published 2026-06-04 · last reviewed 2026-07-09 · Guide

PPARδ agonist raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.

Reviewed 2026-07-09. 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.

Cardarine as Investigational PPARδ Agonist

Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.

Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.

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 Analytical Detection

Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.

Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.

Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.

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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.

Supporting material

== Chemical structure == COP is formed by ring-opening metathesis polymerization (ROMP) of cyclic olefin monomers such as norbornene, followed by partial or total hydrogenation. Modification of the monomer structure results in polymers with a range of glass transition temperatures, stiffness and viscosities. Commercial products include Zeon Chemical's ZEONEX® and ZEONOR® and Japan Synthetic Rubber's ARTON. An alternative process involving copolymerization with ethylene is used to make cyclic olefin copolymers (COC). These two types of cyclic olefin polymers were historically referred to as COC but are now recognized as distinct classes of polymers formed from different polymerization processes. Commercial products include Mitsui Chemical's APEL™ and TOPAS Advanced polymers' TOPAS® COC. Though they share many of the same physical properties, cyclic olefin polymer (COP) formed by ROMP offers greater transparency and mechanical stability and its surface is more amenable to plasma treatment for optimizing cell growth.

=== House of Representatives === In 1968, Mizell was elected to represent the 5th District in the 91st United States Congress. He defeated Democratic nominee Smith Bagley, an R.J. Reynolds Tobacco Company official, 84,905 (52.4 percent) to 77,112 (47.6 percent). The previous 5th District representative, Democrat Nick Galifianakis, was moved to the 4th District for the 1968 elections. A supporter of Richard Nixon, Mizell ran on a platform vehemently opposed to federal spending and Communism. In his first term, he spoke in favor of trade legislation. "I believe no nation in the world need fear the Trade Bill of 1970," he said, praising it for its benefits to foreign nations and American workers alike.

=== Diver's telephone === The communications equipment is relatively straightforward and may be of the two-wire or four-wire type. Two wire systems use the same wires for surface to diver and diver to surface messages, whereas four wire systems allow the diver's messages and the surface operator's messages to use separate wire pairs. In a two wire system the standard arrangement for diver communications is to have the diver's side normally on, so that the surface team can hear anything from the diver at all times except when the surface is sending a message. In a four-wire system the diver's side is always on, even when the surface operator is talking. This is considered an important safety feature, as the surface team can monitor the diver's breathing sounds, which can give early warning of problems developing, and confirms that the diver is alive. Heliox divers may need a decoder system (unscrambler) which reduces the frequency of the sound to make it more intelligible.

Field desorption (FD) is a method of ion formation used in mass spectrometry (MS) in which a high-potential electric field is applied to an emitter with a sharp surface, such as a razor blade, or more commonly, a filament from which tiny "whiskers" have formed. This results in a high electric field which can result in ionization of gaseous molecules of the analyte. Mass spectra produced by FD have little or no fragmentation because FD is a soft ionization method. They are dominated by molecular radical cations M+. and less often, protonated molecules

=== Nodular scabies === In 5-10% of cases, alongside the burrows, rash, and possible pustules, scabies creates raised, hard, and itchy oblong nodules on the skin, 1-4cm across. They may appear purple, dark brown, or pale in patients with darker skin tones, they are pink or red on paler skin tones. These nodules are likely a result of a localized hypersensitivity of the immune system to mites, their waste, or both. Because of this, nodular scabies may be more likely in people with chronic infections, failed treatments, or people becoming re-infected, as the immune system has had time to become sensitized. These nodules are more common on scrotal skin, vulva skin, thighs, buttocks and around the underarms. As with more common presentations of scabies, it is especially present near where skin regularly touches other skin. Once the nodules develop, it can take months for them to heal, even after successful treatment. Some details about the disease are still being researched but it is known to be more common in children and may be more common in males.

Sources: en.wikipedia.org

Supporting material

represents the turnover rate, or the number of reactions catalyzed by an enzyme over the enzyme amount. k c a t {\displaystyle k_{cat}} over k m {\displaystyle k_{m}} is known as the specificity constant, which gives a measure of the affinity of a substrate to some particular enzyme. Also known as the efficiency of an enzyme, this relationship reveals an enzyme's preference for a particular substrate. The higher the specificity constant of an enzyme corresponds to a high preference for that substrate.

In 1945, Libby moved to the University of Chicago, where he began his work on radiocarbon dating. He published a paper in 1946 in which he proposed that the carbon in living matter might include 14C as well as non-radioactive carbon. Libby and several collaborators proceeded to experiment with methane collected from sewage works in Baltimore, and after isotopically enriching their samples they were able to demonstrate that they contained 14C. By contrast, methane created from petroleum showed no radiocarbon activity because of its age. The results were summarized in a paper in Science in 1947, in which the authors commented that their results implied it would be possible to date materials containing carbon of organic origin. Libby and James Arnold proceeded to test the radiocarbon dating theory by analyzing samples with known ages. For example, two samples taken from the tombs of two Egyptian kings, Zoser and Sneferu, independently dated to 2625 BC ± 75 years, were dated by radiocarbon measurement to an average of 2800 BC ± 250 years. These results were published in Science in December 1949. Within 11 years of their announcement, more than 20 radiocarbon dating laboratories had been set up worldwide. In 1960, Libby was awarded the Nobel Prize in Chemistry for this work.

== Society and culture == As of 2018, there is a lack of compelling evidence to conclude superiority of insulin aspart over human insulin in type 2 diabetes. It is thus unclear why the shifting of people from human insulin to insulin aspart has occurred. In type 1 diabetes it appears to result in slightly better blood sugar control.

In late August 2008, Georgian president Saakashvili said that he expected threat from Abkhazia and had most of the forces stationed near Abkhazia, adding: "if we'd intended to attack, we'd have withdrawn our best-trained forces from Iraq up front." He also said that he had been told in Dubrovnik that Russia would attack Georgia in the summer of 2008. By late August, President Saakashvili said that before the war, he had warned Western leaders (among them U.S. Secretary of State Condoleezza Rice and German Chancellor Angela Merkel) about Russia's intentions to invade Georgia; however his warnings were not taken into account. The Georgian authorities were aware that the United States would not become militarily involved in the conflict with Russia. On 31 August, President Saakashvili told the CNN that he supported neutral international investigation into the causes of the war. He further said that Putin had threatened with the war in the fall of 2006 before the announcement of trade embargo against Georgia. In September 2008, former Russian president Vladimir Putin said the war began during the second half of 7 August and Russian military reached Tskhinvali in two days. Putin accused the United States of encouraging Georgian military attack. He added, "When an aggressor comes into your territory, you need to punch him in the face." Putin claimed there would be a "second blow" into the North Caucasus if Russia had not acted in Georgia.

Sources: en.wikipedia.org

Supporting material

== History == Nalbuphine was first synthesized in 1965 and was introduced for medical use in the United States in 1979. In the search for opioid analgesics with less abuse potential than pure MOR agonist opioids, a number of semisynthetic opioids were developed. These substances are referred to as mixed agonist–antagonists analgesics. Nalbuphine belongs to this group of substances. The mixed agonists-antagonists drug class exerts their analgesic actions by agonistic activity at the KOR. While all drugs in this class possess MOR antagonistic activity leading to less abuse potential, nalbuphine is the only approved drug in the mixed agonist–antagonist class listed in terms of its pharmacological actions and selectivities on opioid receptors as a MOR partial agonist or antagonist as well as a KOR agonist (Gustein et al. 2001). Nubain was approved for marketing in the United States in 1978 and remains as the only opioid analgesic of this type (marketed in the U.S.) not controlled under the Controlled Substances Act (CSA). When the Controlled Substances Act (CSA) was enacted in 1971, nalbuphine was placed in schedule II. Endo Laboratories, Inc. subsequently petitioned the DEA to exclude nalbuphine from all schedules of the CSA in 1973. After receiving a medical and scientific review and a scheduling recommendation from the Department of Health, Education and Welfare, forerunner to the Department of Health and Human Services, nalbuphine was removed from schedule II of the CSA in 1976. Presently, nalbuphine is not a controlled substance under the CSA.

=== Data modelling === Much of Aarons' work focuses on building an understanding of how the effects of drugs or toxic agents are managed in humans. In 2009 he co-authored a paper that aimed to explore an approach to the modelling of effects on people by drugs and toxic agents "based on the underlying physiology and pathology of the biological processes,...[ and to review]...the current status of pharmacodynamic and pharmacokinetic modelling, and outline a conceptual framework that may be helpful in advancing the field." A model was proposed that included the kinetics of the substance as a part of the process. To some extent, this was a challenge to the widely accepted dose/effect concept in pharmacology and toxicology at the time which assumed that the exposure/dose of a drug or a toxin is related to the effects on the patient, beneficial or toxic. The paper explained the purposes of data modelling as being to describe complex data, test hypotheses and make predictions, and noted when a drug interacts with a patient, there is a "chain of events at the molecular level, cellular level, organ/physiological system level, and whole-body level...[and ]... in principle, modelling may be performed at each of these levels." The effect on a patient could be therapeutic or possibly result in adverse outcomes. The authors concluded that including the systems biology model they discussed in the paper into conventional PKPD modelling would require further collaboration to make it robust but able to be clearly defined.

When a reactant undergoes two reactions in series, the macro-constant for the combined reaction is the product of the micro-constant for the two steps. For example, the abovementioned cysteine zwitterion can lose two protons, one from sulphur and one from nitrogen, and the overall macro-constant for losing two protons is the product of two dissociation constants

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 is cardarine?

Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.

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