Incretin & metabolic research compounds
Cardarine (GW501516)
Also known as GW501516 · GW-501516 · endurobol
A synthetic PPARδ agonist developed for dyslipidaemia and nicknamed an "exercise mimetic" — a doping compound that never became a medicine.
In 60 seconds
Reached phase 2 for dyslipidaemia; development did not proceed. Preclinical studies link PPARδ activation by GW501516 to tumour-promoting effects, including facilitating tumour immune escape; a 2017 commentary judged it an unsuccessful exercise mimetic.
- Development profile of GW-501516 as a PPARδ agonist in phase 2 for dyslipidaemia.
- A commentary arguing GW501516 failed as an exercise mimetic.
- In preclinical models, GW501516 promoted tumour immune escape by inhibiting phagocytosis via the CD47/SIRPα checkpoint.
Mechanism
Activating the nuclear receptor PPARδ shifts muscle metabolism toward fatty-acid oxidation and endurance-type gene expression in animals, the source of the "exercise in a pill" label.
Research status
Reached phase 2 for dyslipidaemia; development did not proceed. Prohibited in sport.
Key studies
Development profile of GW-501516 as a PPARδ agonist in phase 2 for dyslipidaemia.
GW-501516 GlaxoSmithKline/Ligand — Curr Opin Investig Drugs, 2006 · PMID 16625823
A commentary arguing GW501516 failed as an exercise mimetic.
PPARδ Modulation by GW501516: An Unsuccessful Exercise Mimetic — Clin Pharmacol Ther, 2017 · PMID 28124448
In preclinical models, GW501516 promoted tumour immune escape by inhibiting phagocytosis via the CD47/SIRPα checkpoint.
GW501516 facilitated tumor immune escape by inhibiting phagocytosis — Eur J Pharmacol, 2025 · PMID 39993702
Compared selective PPAR agonists, including a PPARδ agonist, with pan-PPAR agonism in steatohepatitis models.
Differential effects of selective- and pan-PPAR agonists on experimental steatohepatitis and hepatic macrophages — J Hepatol, 2020 · PMID 32360434
Safety signals in the literature
Preclinical studies link PPARδ activation by GW501516 to tumour-promoting effects, including facilitating tumour immune escape; a 2017 commentary judged it an unsuccessful exercise mimetic.
Legal status (South Africa)
Approved incretin medicines are prescription-only (scheduled) in South Africa and available only through a prescriber; research-grade material is not a medicine and is not for human use.
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Questions
What is Cardarine (GW501516)?
A synthetic PPARδ agonist developed for dyslipidaemia and nicknamed an "exercise mimetic" — a doping compound that never became a medicine. Activating the nuclear receptor PPARδ shifts muscle metabolism toward fatty-acid oxidation and endurance-type gene expression in animals, the source of the "exercise in a pill" label.
What is the research status of Cardarine (GW501516)?
Reached phase 2 for dyslipidaemia; development did not proceed. Prohibited in sport.
What safety signals are reported for Cardarine (GW501516)?
Preclinical studies link PPARδ activation by GW501516 to tumour-promoting effects, including facilitating tumour immune escape; a 2017 commentary judged it an unsuccessful exercise mimetic.
Does Living Water Labs stock Cardarine (GW501516)?
Not at present. Cardarine (GW501516) is profiled here for reference, with citations to the published literature. You can ask to be notified if we add it. Approved incretin medicines are prescription-only (scheduled) in South Africa and available only through a prescriber; research-grade material is not a medicine and is not for human use.
More in Incretin & metabolic
Research reference only. This page summarises published literature; it is not medical advice and contains no guidance on human use. Products supplied by Living Water Labs are for laboratory research only.
