GW501516 is a synthetic PPARδ agonist (EC50 ~1 nM). PPARδ is a nuclear receptor expressed abundantly in skeletal muscle, adipose tissue, and heart. Activation shifts skeletal muscle metabolism from glucose oxidation to fatty acid oxidation (fibre-type switching, increased CPT1 expression, UCP3 upregulation). Simultaneously upregulates ABCA1 (reverse cholesterol transport) raising HDL. Termed “exercise in a pill” in media due to endurance effects in rodent models.
C57BL/6 mice on high-fat diet: GW501516 significantly reduced adiposity, improved glucose tolerance, and increased fatty acid oxidation markers. Skeletal muscle CPT1, PDK4, and UCP3 mRNA increased dose-dependently. Fibre-type shift from type IIb to oxidative type IIa fibres.
Endurance / Exercise Mimetic Research
Narkar et al. 2008 (Cell): GW501516 + AICAR in sedentary mice increased running endurance 77% vs vehicle — “exercise in a pill” study. PPARδ activation upregulates genes for fatty acid metabolism and mitochondrial biogenesis. Widely cited endurance research model.
PPARδ activation suppresses NF-κB signalling and reduces pro-inflammatory cytokines in macrophage and endothelial models. Potential interest in inflammatory disease and metabolic syndrome research.
Key Research Data
Study / Source
Key Findings
Narkar et al. 2008 Cell
“Exercise in a pill”: PPARδ agonism in sedentary mice increased running endurance 77%, fibre-type switching confirmed
Cardarine (GW501516) is a synthetic PPARδ (Peroxisome Proliferator-Activated Receptor delta) agonist. Not a SARM — activates a different nuclear receptor pathway. Shifts skeletal muscle metabolism from glucose to fatty acid oxidation, increases HDL, and in rodent models dramatically increases endurance. Used in metabolic, endurance, and lipid research.
Is Cardarine a SARM?
No — Cardarine (GW501516) is commonly grouped with SARMs in research communities but operates via a completely different mechanism. SARMs (like LGD-4033 and RAD-140) bind the androgen receptor. Cardarine binds PPARδ, a nuclear receptor involved in fatty acid metabolism and energy expenditure. Different receptor, different pathway, different tissue effects.
What did the “exercise in a pill” study show?
Narkar et al. 2008 (Cell) showed that GW501516 combined with AICAR (AMPK activator) in sedentary mice increased running endurance by 77% vs vehicle. PPARδ activation upregulated genes for fatty acid oxidation and fibre-type switching. Widely cited as proof-of-concept for metabolic reprogramming via PPARδ.
Does QSC ship Cardarine to the USA?
Yes. QSC Cardarine is available with domestic USA shipping and ships to EU, UK, Canada, and Australia. All batches carry Janoshik third-party COA confirming ≥99% HPLC purity and MS identity verification.
