AICA ribonucleotide is a cell-permeable activator of AMP-activated protein kinase (AMPK).1 It activates AMPK in a cell-free assay when used at concentrations ranging from 1 to 500 µM. AICA ribonucleotide (100-500 µM) inhibits lipolysis and lipogenesis in primary rat adipocytes. In vivo, AICA ribonucleotide (0.5 mg/kg) increases insulin sensitivity and prevents pancreatic β-cell damage in Zucker diabetic fatty rats.2 AICA ribonucleotide (0.5 mg/kg) induces cardiac mobilization and myofibroblast differentiation of endogenous CD44+CD45- mesenchymal stem cells (MSCs), as well as decreases cardiac scar formation, in an aged mouse model of myocardial infarction induced by left anterior descending artery (LAD) occlusion.3 Formulations containing AICA ribonucleotide have been used in the treatment and prevention of cardiac ischemic injury.
1.Sullivan, J.E., Brocklehurst, K.J., Marley, A.E., et al.Inhibition of lipolysis and lipogenesis in isolated rat adipocytes with AICAR, a cell-permeable activator of AMP-activated protein kinaseFEBS Lett.353(1)33-36(1994) 2.Pold, R., Jensen, L.S., Jessen, N., et al.Long-term AICAR administration and exercise prevents diabetes in ZDF ratsDiabetes54(4)928-934(2005) 3.Cieslik, K.A., Taffet, G.E., Crawford, J.R., et al.AICAR-dependent AMPK activation improves scar formation in the aged heart in a murine model of reperfused myocardial infarctionJ. Mol. Cell. Cardiol.6326-36(2013)