What it is
AICAR (5-aminoimidazole-4-carboxamide ribonucleotide) is a compound that activates AMPK, the central regulator of cellular energy metabolism. By stimulating AMPK, AICAR promotes glucose uptake and fatty-acid oxidation, leading to improved energy production and endurance. It also supports cardiovascular and metabolic health and improves insulin sensitivity in resistant states.
Mechanism of action
Cell-permeable adenosine analog phosphorylated to ZMP intracellularly, which mimics AMP and allosterically activates AMPK. AMPK activation increases glucose transport (GLUT4), fatty-acid oxidation, mitochondrial biogenesis, and inhibits anabolic pathways via mTOR suppression.
Half-life: Short in plasma β minutes.
Evidence summary
Classic 1997β2008 work in rodent muscle and liver established the AMPK-mediated metabolic effects. Narkar et al. (Cell, 2008) demonstrated exercise-mimetic gene expression. Limited but informative human trials in type 2 diabetes show acute improvements in glucose handling.
Typical dosing protocols
- Investigational β published doses range 10β60 mg/kg/day in animal models
- Human studies have used IV infusion
- Not currently available as an approved oral therapeutic
Side effects & safety
- Banned by WADA β listed as prohibited for athletes
- Possible nausea, GI upset, and uric-acid elevation
- Long-term safety not established
Cited studies
- Merrill GF, Kurth EJ, Hardie DG, Winder WW (1997). AICA riboside increases AMP-activated protein kinase, fatty acid oxidation, and glucose uptake in rat muscle. American Journal of Physiology.Read source β
- Buhl ES, Jessen N, Pold R, et al. (2002). AICAR administration causes an apparent enhancement of muscle and liver insulin action in insulin-resistant high-fat-fed rats. Diabetes.Read source β
- (2002). 5-Aminoimidazole-4-carboxamide ribonucleoside treatment improves glucose homeostasis in insulin-resistant diabetic (ob/ob) mice. Diabetologia.Read source β
- (2008). Intravenous AICAR administration reduces hepatic glucose output and inhibits whole body lipolysis in type 2 diabetic patients. Diabetologia.Read source β
- Narkar VA, Downes M, Yu RT, et al. (2008). AMPK and PPARΞ΄ agonists are exercise mimetics. Cell.Read source β
All content is for research and educational purposes. Peptides described are sold for laboratory research use only and are not intended to diagnose, treat, cure, or prevent any disease. Always consult a qualified healthcare professional before beginning any protocol.