Description
GW-501516 (Cardarine, Endurobol) is a PPARδ receptor agonist (Peroxisome Proliferator-Activated Receptor Delta), not a SARM. Its listing in the SARM category is historical, since the substance is often used alongside SARMs in recreational research stacks.
Per study reports Cardarine activates the PPARδ receptor, predominantly expressed in skeletal muscle, fat tissue and liver. Activation increases fatty acid oxidation and mitochondrial biogenesis. It also upregulates various genes of lipid metabolism. In the original GlaxoSmithKline research, GW-501516 was developed as an HDL-raising therapeutic - early studies showed HDL values rising dose-dependently by 30-79%.
The most spectacular data come from mouse studies on endurance performance: trained mice under GW-501516 in Narkar et al 2008 (Cell) showed nearly doubled running endurance vs placebo. The effect is based on transcriptional reprogramming of skeletal muscle toward type I fibers and increased mitochondrial density.
Development was stopped in 2007 by GSK after two-year carcinogenicity studies in mice and rats showed dose-dependent tumor formation - at substantially higher doses than used in typical recreational research practice. Safety profile in human studies remains incompletely characterized due to discontinued development.
Cardarine is on the WADA banned list. Pharmacokinetically oral with about 24-hour half-life.
You can order Cardarine as oral tablets in one bottle with 10mg or 20mg per tablet.
This information is for research and educational purposes only. No medical recommendations.
Risks & Safety
Cardarine sits in the mid range of the risk scale, with one important open point: the safety profile in humans remains incompletely characterized because of the discontinued development.
Documented in studies and the literature:
- Carcinogenicity signal: in two-year carcinogenicity studies in mice and rats, tumors appeared dose-dependently - the reason GlaxoSmithKline stopped development in 2007. The doses were substantially above typical recreational research practice, but the signal must be taken seriously.
- Incomplete human data: because of the discontinued development, a complete characterization of the safety profile in humans is missing.
- No HPG suppression: Cardarine is not a SARM. No PCT is required.
- WADA banned list: Cardarine is on the banned list for sport.
Monitoring via bloodwork is recommended. This classification does not replace medical advice. Risk and responsibility for any actual use lie entirely with the buyer.
Studies
- AMPK and PPARδ Agonists Are Exercise Mimetics - Cell 2008, Narkar et al: classic endurance study in mice, GW-501516 plus training nearly doubles running distance.
- A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport - PNAS 2001, Oliver et al: original study on HDL elevation and reverse cholesterol transport under GW-501516.
- Activation of peroxisome proliferator-activated receptor δ induces fatty acid β-oxidation in skeletal muscle and attenuates metabolic syndrome - PNAS 2003, Tanaka et al: PPARδ activation increases fatty acid β-oxidation in skeletal muscle and attenuates metabolic syndrome.
- The PPARδ agonist, GW501516, promotes fatty acid oxidation but has no direct effect on glucose utilisation or insulin sensitivity in rat L6 skeletal muscle cells - FEBS Letters 2007, Dimopoulos et al: mechanistic study on fatty acid oxidation in muscle cells.
