MECHANISM OF ACTION
Cardarine is a small molecule (not a peptide) that activates a switch called PPAR-delta, found in muscle cells. This switch controls which fuel source the muscles prefer to burn. When activated, muscles shift strongly towards burning fat rather than sugar, making more fat available as energy and improving stamina. It also triggers the growth of more mitochondria (the energy-producing parts of cells) and raises HDL cholesterol (the "good" kind). Originally developed by GlaxoSmithKline for metabolic syndrome, it reached Phase II clinical trials where it showed remarkable endurance and cholesterol benefits at very low doses. Clinical development was halted for reasons unrelated to its mechanism, but the research data is publicly available and remains of interest to scientists studying metabolism and exercise physiology.
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
2004Preclinical gene-expression models expressing constitutively active PPAR-δ ran twice as far as 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.