If you have been reading about Prohibited substance and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.
Updated 2025-07-18. Numbers and descriptions here follow the published literature rather than marketing material.
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.
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.
| Property | Value | Notes |
|---|---|---|
| Common name | Cardarine | Common internet and media name. |
| Research code | GW501516 | Also written GW-1516. |
| Drug class | PPARδ agonist | Not a selective androgen receptor modulator. |
| Development status | Discontinued | Clinical development halted after rodent cancer findings. |
| Regulatory status | Prohibited in sport | Listed by WADA; not approved as medicine. |
=== Structure-activity experiments === When the 12-amino acid sequence of 'peptide 3'/CCL2 is aligned with the sequences of the other chemokines CCL3, CXCL8 and CXCL12 5 amino acids are conserved, Cys3, Asp5, Pro6, Trp10 and Gln12. In addition Val11 is also present in CCL3 and CXCL8. The corresponding 11th amino acid in CXCL12 is Ile. Ala4 in CCL2 is also present in CCL3 but the corresponding residue is Leu in CXCL8 and Ile in CXCL12. Inclusion of Leu at position 4 and Ile at position 11 (NH2-EICLDPKQKWIQ-OH) increased the inhibition potency of the peptide to 2-4μM. Removal of the first two residues from 'Peptide 3' (NH2-CADPKQKWVQ-OH) does not lower its BSCI potency. Peptide 3-Leu4, Ile11, the most potent BSCI peptide was chosen for further development. The first two amino acids were removed, and then according to the method of Jameson et al., the amino acid sequence was reversed and the amino acids replaced with D-amino acids. This combined transformation changes the orientation of the amides in the backbone but does not change the position of the amino acid sidechains. The peptide was then cyclised by adding a cysteine to the other end (HO-CLDPKQKWIQC-NH2), and oxidisation to form a disulfide bond to give NR58,3-14-3.
Le Cerveau by Gérard Oury (1968) La Beuze (2003) Disco (2008) La Fée, also presented at the Directors' Fortnight in 2011. The film by Sophie Marceau, La Disparue de Deauville, made in 2007, contains many scenes around the port of Le Havre, in the Coty shopping centre of Coty and in the streets of the central city. The film Le Havre by Aki Kaurismäki received two prizes at the 2011 Cannes Film Festival and also the Louis Delluc Prize. It was nominated three times for the 37th César Awards.
The four substrates of this enzyme are 7-methylxanthine, reduced nicotinamide adenine dinucleotide (NADH), oxygen, and a proton. Its products are xanthine, oxidised NAD+, water, and formaldehyde. The enzyme is a non-heme iron protein that is part of the pathway of caffeine degradation in Pseudomonas putida.
=== Pharmacokinetics === The percentage of ribociclib absorbed in the gut has not been determined. Highest blood plasma levels are reached after one to four hours; and after repeated dosage, steady state concentrations are reached after about eight days. Food intake has no effect on absorption rates. When in the bloodstream, about 70% of ribociclib is bound to plasma proteins. The substance is mainly metabolized by CYP3A4 and subsequently by various phase II enzymes, resulting in a large number of metabolites. Those with highest blood plasma concentrations in humans are called CCI284 (an unspecified N-hydroxylation product), LEQ803 (the N-demethylation product) and M1 (a glucuronide). All metabolites have negligible clinical activity. Ribociclib has a slight tendency to accumulate in the body. It is eliminated with an average biological half-life of 32 hours, mostly (69%) via the feces, but also (23%) via the urine. The unchanged drug accounts for 17% of the substance in the feces and 12% of the substance in the urine, the rest being metabolites.
==== Insecticides ==== RNAi is under development as an insecticide, employing multiple approaches, including genetic engineering and topical application. Cells in the midgut of some insects take up the dsRNA molecules in the process referred to as environmental RNAi. In some insects the effect is systemic as the signal spreads throughout the insect's body (referred to as systemic RNAi). Animals exposed to RNAi at doses millions of times higher than anticipated human exposure levels show no adverse effects. RNAi has varying effects in different species of Lepidoptera (butterflies and moths). Drosophila spp., Bombyx mori, Locusta spp., Spodoptera spp., Tribolium castaneum, Nilaparvata lugens, Helicoverpa armigera, and Apis mellifera are models that have been widely used to learn how RNAi works within particular taxa of insects. Musca domestica has two Ago2 genes and Glossina morsitans three, as found by Lewis et al. 2016 and Hain et al. 2010. In the case of the miRNA pathway Diuraphis noxia has two Ago1s, M. domestica two Dcr1s, Acyrthosiphon pisum two each of Ago1 and Loqs and Dcr1 and four of Pasha. While in the piRNA, G. morsitans and A. pisum have two or three Ago3s each. This has led to identification of future insecticide development targets, and the modes of action and reasons for insecticide resistance of other insecticides.
Sources: en.wikipedia.org
=== Parkinson's disease === α-Synuclein is a protein that is associated with Parkinson's disease. In humans, this protein is encoded by the SNCA gene. α-Synuclein is involved in recycling synaptic vesicles that carry neurotransmitters and naturally occurs in an unfolded form. Elevated levels of α-Synuclein are found in patients with Parkinson's disease. There is a correlation between the concentration of unphosphorylated α-Synuclein present in the patient and the severity of Parkinson's disease. Specifically, phosphorylation of Ser129 in α-Synuclein has an impact on severity. Healthy patients have higher levels of unphosphorylated α-Synuclein than patients with Parkinson's disease. The measurement of change in the ratio of concentrations of phosphorylated α-Synuclein to unphosphorylated α-Synuclein within a patient could be a marker of the disease progression. Antibodies that target α-Synuclein at phosphorylated Ser129 are used to study the molecular aspects of synucleinopathies. Phosphorylation of Ser129 is associated with the aggregation of the protein and further damage to the nervous system. The aggregation of phosphorylated α-Synuclein can be enhanced if a presynaptic scaffold protein, Sept4, is present in insufficient quantities. Direct interaction of α-Synuclein with Sept4 inhibits the phosphorylation of Ser129. However, phosphorylation of Ser129 can be observed without synuclein aggregation in conditions of overexpression.
=== Social services === On November 15, 2018, the government announced it was eliminating three watchdog legislative offices, including the child and youth advocate. One of the biggest cuts, announced in the 2019 budget, was the $1 billion cut—over four years—to the Ministry of Community and Social Services. In February 2019, the government had announced changes to the Ontario Autism Program, which had over 20,000 children on a waiting list. Under Minister MacLeod and Fee, changes were made in "how children qualified, based on age and family income". During the revamping of the Program, support for children already receiving service, was clawed back which meant that families had to pay most of the bills for "very expensive behavioural therapies." This "outraged those in the autism community". The protests included a "huge rally at Queen's Park that could be heard inside the legislature and inundated Tory MPPs and Social Services Minister Lisa MacLeod with complaints." In response, the Ford government "scrambled to pour more money into the program and in early May [2019] announced consultations that would help shape further reforms to the system, moving toward one based on need." The Hamilton Spectator said that of all the "policy snafus", the funding of services for families of children with autism, was the one that bothered Ford the most.
=== Wound healing macrophages === Interleukin 4, secreted by granulocytes after tissue damage or by adaptive immune cells within a Th2 response, causes macrophages to secrete minimal amounts of pro-inflammatory cytokines and to have lower activity against intracellular pathogens. They also promote extracellular matrix synthesis via production of ornithine, via arginase; this is used as a precursor for extracellular matrix components. The overall result is a macrophage population that promotes wound healing. The specific roles macrophages play in the Th2 response are still under investigation.
== Northern Hemisphere == In the Northern Hemisphere, there are two towns in Sakha, Russia that compete for the title of "Pole of Cold". These are Verkhoyansk (located at 67°33′N 133°23′E, altitude 127 metres (417 ft)) and Oymyakon (located at 63°15′N 143°9′E, altitude 745 metres (2,444 ft)). However, the World Meteorological Organization has recognized in 2020 a temperature of −69.6 °C (−93.3 °F), measured near the topographic summit of the Greenland Ice Sheet on 22 December 1991, as the lowest in the Northern Hemisphere. The record was measured at an automatic weather station and was uncovered after nearly 30 years. In December 1868 and then in February 1869 Ivan Khudyakov made the discovery of the Northern Pole of Cold by measuring a record temperature of −63.2 °C (−81.8 °F) in Verkhoyansk. Later, on January 15, 1885, a temperature of −67.8 °C (−90.0 °F) was registered there by Sergey Kovalik. This measurement was published in the Annals of the General Physical Observatory in 1892; by mistake it was written as −69.8 °C (−93.6 °F), which was later corrected. One can still find this incorrect value in some literature. The coldest reliably measured temperature in Verkhoyansk was −67.8 °C (−90.0 °F) on February 5 and 7 of 1892. On February 6, 1933, a temperature of −67.7 °C (−89.9 °F) was recorded at Oymyakon's weather station. At the time, this was the coldest reliably measured temperature for the Northern Hemisphere. The weather station is in a valley between Oymyakon and Tomtor.
Sources: en.wikipedia.org
No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.
Preclinical rodent studies reported cancers, including liver and bladder tumors, at tested doses. The human relevance of those findings is uncertain, but development was discontinued. No approved human product resulted.
No. It remains an investigational compound without approved therapeutic labeling. Sports regulators prohibit its use, and health agencies have warned against consuming it.
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.