MECHANISM OF ACTION
Cardarine (GW501516) is a PPAR-δ (peroxisome proliferator-activated receptor delta) agonist that activates genes involved in fatty acid oxidation, mitochondrial biogenesis, and glucose uptake. Originally developed by GlaxoSmithKline and Ligand Pharmaceuticals for metabolic syndrome. Phase I/II clinical trials demonstrated remarkable endurance enhancement and HDL elevation at doses of 2.5–10 mg daily. PPAR-δ activation shifts skeletal muscle fuel preference toward fatty acid oxidation, improving endurance capacity and metabolic flexibility. Research continues to examine PPAR-δ pharmacology for applications in metabolic disease, lipid metabolism, and exercise biology.
RESEARCH APPLICATIONS
- Endurance and aerobic capacity research
- Fatty acid oxidation and body composition
- HDL elevation and dyslipidaemia models
- PPAR-δ receptor pharmacology
- Metabolic syndrome research
RESEARCH HIGHLIGHTS
PPAR-δ Endurance Enhancement
2004Transgenic mice expressing constitutively active PPAR-δ ran twice as far as wild-type controls - the "marathon mouse" model that first identified GW501516 as an endurance target.
Ref: Wang et al., PLOS Biol
Phase II: HDL +79%, LDL -7%
2007Phase II metabolic syndrome trial: GW501516 produced dramatic HDL increases and HDL particle size improvement vs. placebo at 8 weeks at doses of 2.5–10 mg daily.
Ref: Sprecher et al., Arterioscler Thromb Vasc Biol
RESEARCH PROTOCOL NOTES
Chemical Identity
Storage & Stability
Small molecule, oral formulation. Store at room temperature away from moisture and light. Stable for 12–24 months if sealed.
Regulatory Status
Clinical development discontinued by GSK. Not approved by any regulatory authority. WADA prohibited under S4 (Hormone and Metabolic Modulators). SAHPRA: unscheduled research compound.