Acadesine (AICAr), 50 mg
AICAr is a cell-permeable compound whose phosphorylated metabolite activates AMP-activated protein kinase (AMPK). Incubation of rat hepatocytes with the non-phosphorylated AICAR results in accumulation of the monophosphorylated derivative within the cell. ZMP mimics both activating effects of AMP on AMPK, i.e. direct allosteric activation of phospho-transferase activity of AMPK. Unlike other methods for activating AMPK in intact cells AICAR does not perturb the cellular concentrations of ATP, ADP or AMP. Incubation of hepatocytes with AICAR activates AMPK due to increased phosphorylation, causes phosphorylation and inactivation of a known target for AMPK (3-hydroxy-3-methylglutaryl-CoA reductase), and causes almost total cessation of two of the known target pathways, i.e. fatty acid and sterol synthesis. Incubation of isolated adipocytes with AICAR antagonizes isoprenaline-induced lipolysis.
Molecular weight 258.2 g/mol. Appearance: Off-white solid. Purity: 98%, Solubility: soluble in diluted acetic acid. Formula C9H14N4O5.
Synonyms: AICAr, AICA-Riboside, Z-Riboside
PLEASE NOTE: Our reagents and chemicals are provided to academic institutes and pharmaceutical companies for in vitro research use only. This product has not been approved for any other purposes including, without limitation, diagnostic or therapeutic purposes, for use in preparation of food or pharmaceutical products nor for administration to humans. We do not supply private customers or non-research organizations with this product!
Product specific literature references:
Mullane K (1993) "Acadesine: the prototype adenosine regulating agent for reducing myocardial ischaemic injury." Cardiovasc. Res. (1):43-7
Sullivan JE, Brocklehurst KJ, Beri RK et al. (1994) "Inhibition of lipolysis and lipogenesis in isolated rat adipocytes with AICAR, a cell-permeable activator of AMP-activated protein kinase" FEBS Lett. 353(1):33-6
Nawarskas JJ. (1999) "Acadesine: a unique cardioprotective agent for myocardial ischemia." Heart Dis. (4):255-60.
Corton JM, Gillespie JG, Hawley SA, Hardie DG (1995) "5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells?" Eur J Biochem. 229(2):558-65
Muoio DM, Seefeld K, Witters LA, Coleman RA. (1999) "AMP-activated kinase reciprocally regulates triacylglycerol synthesis and fatty acid oxidation in liver and muscle: evidence that sn-glycerol-3-phosphate acyltransferase is a novel target." Biochem. J. 338 ( Pt 3): 783-91.
Salt IP, Connell JM, Gould GW (2000) "5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) inhibits insulin-stimulated glucose transport in 3T3-L1 adipocytes" Diabetes 49(10):1649-56
Buhl ES, Jessen N, Lund S et al. (2002) "Long-term AICAR administration reduces metabolic disturbances and lowers blood pressure in rats displaying features of the insulin resistance syndrome" Diabetes 51(7):2199-206
Aschenbach WG, Hirshman MF, Goodyear LJ et al. (2002) "Effect of AICAR treatment on glycogen metabolism in skeletal muscle" Diabetes 51(3):567-73
Gadalla AE, Pearson T, Frenguelli BG et al. (2004) "AICA riboside both activates AMP-activated protein kinase and competes with adenosine for the nucleoside transporter in the CA1 region of the rat hippocampus." J. Neurochem. 88(5):1272-82