A practical reference on PPARδ agonist: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
Reviewed 2026-06-08. Anything still debated is marked as such rather than presented as settled.
Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.
Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.
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.
| Property | Value | Notes |
|---|---|---|
| Chemical class | Synthetic PPARδ agonist | Not a steroid or a selective androgen receptor modulator. |
| Common synonyms | Cardarine, GW501516, GW-501516, endurobol | Names vary by supplier and literature source. |
| Appearance | White to off-white powder | Consistent with many small-molecule research chemicals. |
| Solubility | Low in water; soluble in DMSO and ethanol | Often prepared in organic solvent for laboratory work. |
| Primary target | PPARδ (NR1C2) | Nuclear receptor involved in lipid and energy metabolism. |
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.
Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.
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.
=== 4 February === Ukrainian officials claimed to have done another prisoner swap with Russia, saying that 116 Ukrainian POWs have been returned, including Ukrainian soldiers and guerrillas from occupied territories. Also returned were the bodies of the two deceased British aid workers killed near Soledar, namely Chris Parry, aged 28, and Andrew Bagshaw, aged 47. Russian officials claimed some 63 soldiers were returned. The deal was in part organised by the United Arab Emirates.
Hematocrit measurements had previously been described in the literature, but Wintrobe's method differed in that it used a large tube that could be mass-produced to precise specifications, with a built-in scale. The fraction of red blood cells in the tube was measured after centrifugation to determine the hematocrit. The invention of a reproducible method for determining hematocrit values allowed Wintrobe to define the red blood cell indices.
== Biosynthesis and metabolism == Flavonoid biosynthesis in plants uses a phenylpropanoid metabolic pathway in which the amino acid phenylalanine is converted to 4-coumaroyl-CoA. This is combined with malonyl-CoA to yield a group of compounds called chalcones, which contain two phenyl rings. In the case of naringenin, the precursor is naringenin chalcone produced by the enzyme chalcone synthase. This can cyclise spontaneously but would provide racemic material. The enzyme chalcone isomerase constrains the reaction to give only the (S) isomer of the flavanone.
== See also == Substituted tryptamine List of investigational hallucinogens and entactogens List of investigational anxiolytics List of investigational antidepressants SPL028 (D2-DMT; α,α-dideutero-DMT) Deuterated 5-MeO-DMT α,α-Dideuterotryptamine
Sources: en.wikipedia.org
biotin) or clickable handles (azides or alkynes) enable enrichment of labeled enzymes prior to identification by liquid chromatography-tandem mass spectrometry (LC-MS/MS). After covalent labeling in cells or lysates, enzyme-probe adducts are captured using streptavidin or other affinity matrices, washed to remove unlabeled proteins, and digested for MS-based peptide identification. This strategy provides high sensitivity and depth of coverage, which facilitates the discovery of novel enzyme targets, detection of low-abundance enzymes and analysis of complex enzyme families. To compare enzyme activity across biological conditions, ABPP can be integrated with quantitative proteomic technologies to measure relative enzyme activity across samples. Techniques such as SILAC (Stable Isotope Labeling by Amino acids in Cell culture) incorporate heavy or light isotope-encoded amino acids into cellular proteins, facilitating direct MS-based comparison of probe-labeled peptides from different samples. TMT (Tandem mass tagging) which uses isobaric mass tags allows labeled peptides from multiple samples to be multiplexed and quantified simultaneously. These strategies have been widely applied to assess selectivity of covalent inhibitors and genome-wide changes in enzymatic activity. isoTOP-ABPP (Isotope Tagging of Optimized Probes for Activity-Based Protein Profiling) is a specialized workflow that was developed to address some of the limitations of conventional ABPP, including poor specificity, limited sensitivity, and the absence of selective chemical ligands for many human enzymes.
==== CIA assessment ==== At the latest, the successful start of Sputnik 2 with the satellite weighing more than 500 kg proved that the USSR had achieved a leading advantage in rocket technology. The CIA, initially astonished, estimated the launch weight of the rocket at 500 metric tons, requiring an initial thrust exceeding 1,000 tons, and assumed the use of a three-stage rocket. In a classified report, the agency described the event as a "stupendous scientific achievement" and concluded that the USSR had likely perfected an intercontinental ballistic missile (ICBM) capable of accurately targeting any location. In reality, the launch weight of the Soviet rocket was 267 metric tons with an initial thrust of 410 tons with one and a half stages. The CIA's misjudgement was caused by extrapolating the parameters of the US Atlas rocket developed at the same time (launch weight 82 tons, initial thrust 135 tons, maximum payload of 70 kg for low Earth orbit). In part, the favourable data of the Soviet launcher was based on concepts proposed by the German rocket scientists headed by Helmut Gröttrup on Gorodomlya Island, such as, among other things, the rigorous weight saving, the control of the residual fuel quantities and a reduced thrust to weight relation of 1.4 instead of usual factor 2. The CIA had heard about such details already in January 1954 when it interrogated Göttrup after his return from the USSR but did not take him seriously.
Pakistan, a federal parliamentary republic, consists of four provinces: Punjab, Khyber Pakhtunkhwa, Sindh, and Balochistan, along with three territories: Islamabad Capital Territory, Gilgit-Baltistan, and Azad Kashmir. The Government of Pakistan governs the western parts of the Kashmir Region, organised into separate political entities, Azad Kashmir and Gilgit-Baltistan. In 2009, the constitutional assignment (the Gilgit–Baltistan Empowerment and Self-Governance Order) granted Gilgit-Baltistan semi-provincial status, providing it with self-government. The local government system consists of districts, tehsils, and union councils, with an elected body at each tier.
Sources: en.wikipedia.org
The oxygen transmission rate of a gas through packaging is defined as the amount of oxygen permeating per unit of permeable area and per unit of time in a packaging system considering standardized test conditions (23 °C and 1 atm. partial pressure difference). It is an effective tool to estimate the barrier properties of a certain material. The determination of the OTR is usually carried out by means of a steady-state and isostatic method, reported by the ASTM D 3985 or ASTM F 1307, containing respectively standardized protocols for the measurements of the OTR of several kinds of packaging. The typical instrumentation consists in a permeation cell composed by two distinct chambers, separated by the tested material; one of the chambers is then filled with a carrier gas (e.g., nitrogen), while the other one with oxygen, hence creating the necessary driving force to let the oxygen permeate across the barrier's material.
Growth of many unfavorable wild yeasts is generally slowed at lower cellar temperatures, so many winemakers who wish to inhibit the activities of these yeasts before the more favorable Saccharomyces yeast kick in, will often chill their must, such as the practice of "cold soaking" the must during a pre-fermentation maceration at temperatures between 4–15 °C (39–59 °F). Though some species, such as Brettanomyces, will not be inhibited and may even thrive during an extended period of cold soaking.
Gorlice–Tarnów Offensive — The Central Powers attacked Lemberg, the Galician capital and sent the Russians into a headlong retreat. Second Battle of Artois — French forces under command of General Victor d'Urbal launched renewed artillery bombardments and infantry assaults against the German line on the Western Front south of German-held Souchez, France. Battle of Hébuterne — The battle concluded with the French holding on to their line, but at a cost of over 10,000 casualties. The Germans lost around 4,000 including 651 prisoners. Charge of Rokitna — A cavalry squadron of 70 men led by Rittmeister Zbigniew Dunin-Wasowicz with the 2nd Polish Brigade charged Imperial Russian Army positions at the village of Rokytne in the Austrian-Hungarian province of Bukovina (now part of Ukraine). The charge broke through three lines of Russian trenches, but resulted in 40 casualties among the squadron including the commanding officer. The Austro-Hungarian infantry failed to capitalize on the break. Greece held legislative elections under the Old Style calendar, with Eleftherios Venizelos and his Liberal Party winning by a landslide, gaining 187 of the 316 seats in the Greek Parliament. Legislative elections were held in Portugal, with the Democratic Party winning 106 of the 163 seats in the House of Representatives and 45 of the 69 seats in the Senate. General elections were held in San Marino to elect the fourth Grand and General Council.
Sources: en.wikipedia.org
Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.
It binds to and activates PPARδ, a nuclear receptor that regulates genes related to fatty acid oxidation and energy use. This activation alters transcription in tissues such as skeletal muscle and liver. The full range of downstream effects in humans is not fully established.
No, cardarine is not known to occur naturally in plants, animals, or humans. It is a synthetic molecule produced for laboratory research. Products labeled as cardarine should therefore be treated as manufactured chemicals with variable purity.
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.