Purity: > 98%
AICAR(cas 2627-69-2), also known as ARA100, is a selective activator of AMP-activated protein kinase (AMPK) in both hepatocytes and adipocytes. AICAR inhibits the synthesis of fatty acids and sterols and inactivates HMG-CoA reductase in rat hepatocytes. It also blocks the expression of pro-inflammatory cytokines (TNF-α/IL-1β and IL-6), iNOS, COX-2, and MnSOD genes in glial cells and macrophages by inhibiting NFκB and C/EBP pathways.
1. Brain Res Bull. 1990 Jul;25(1):203-6.
5-Aminoimidazole-4-carboxamide riboside (AICAr) administration reduces cerebral ischemic damage in the Mongolian gerbil.
Clough-Helfman C(1), Phillis JW.
(1)Department of Physiology, Wayne State University School of Medicine, Detroit, MI 48201.
Cerebral ischemic damage in gerbils was assessed by locomotor activity studies and histopathological examination of the hippocampal CA1 pyramidal cell layer. Pretreatment with AICAr (50 and 500 mg/kg) 30 min prior to a 5-min ischemic episode in unanesthetized gerbils, significantly attenuated the degree of ischemic neuronal damage as measured by either technique with the 500 mg/kg dose; the 50 mg/kg dose, although showing a trend, was not significant. A potential mechanism for AICAr-induced cerebroprotection may be that it is metabolized to uric acid, a free radical scavenger.
2. Am J Physiol. 1989 Sep;257(3 Pt 1):C488-94.
Utility of AICAr for metabolic studies is diminished by systemic effects in situ.
Foley JM(1), Adams GR, Meyer RA.
(1)Department of Physiology, Michigan State University, East Lansing 48824.
It has been reported that intraperitoneal infusion of 5-amino-4-imidazolecarboxamide riboside (AICAr) inhibits the purine nucleotide cycle, resulting in rapid fatigue of isometric twitch force during stimulation of rat muscle. In this study, peak isometric twitch force was recorded from gastrocnemius muscles of pentobarbital-anesthetized rats stimulated in situ at 0.75 Hz after intraperitoneal infusion of 9ml/100 g body wt of 250 mM AICAr or isotonic saline. Excluding the two AICAr-infused rats that died during infusion or stimulation, there was no difference in twitch force between groups, although mean arterial pressure in the AICAr group declined to values 20 Torr below those of the control group during drug infusion. High-resolution 1H nuclear magnetic resonance (NMR) spectroscopy of extracts verified the presence of AICAr and AICA ribotide (AICAR) in muscles of experimental animals. In a second study in which rats were mounted head down in an NMR spectrometer, AICAr infusion resulted in decreased mean arterial pressure and impairment of phosphocreatine recovery after stimulation but no significant difference in twitch force during stimulation. These results demonstrate that AICAr infusion has systemic effects and that the previously reported decline in muscle force with AICAr infusion may not be attributable to purine nucleotide cycle inhibition.