Alias: AICAR; AICA-RIBOSIDE; AMPK; Z-RIBOSIDE
Molecular Formula: C9H14N4O5
Molecular Weight: 258.23
Apperance: White or off-white powder.
Usage: Pharmaceutical intermediates. For the treatment of cardiovascular diseases
AICAR (AICA-Riboside) strongly inhibits the transcription of PPAR&alpha and the coactivation of PPAR&alpha. In adipocyte studies it has been shown to antagonize lipolysis induced by isoprenaline and has been suggested for use in kinase cascade research. Additionally, research indicates that AICAR blocks the differentiation of 3T3-L1 (sc-2243) adipocytes. Studies demonstrate that AICAR can mimic the activity of insulin (sc-211647) by activating AMPK (AMP-activated protein kinase), and affecting the expression of PEPCK-M (PEPCK) and glucose-6-phosphatase (G6Pase). The 5-aminoimidazole-4-carboxamide ribonucleoside (ZMP) is the monophosphorylated derivative of AICA-Riboside, and it can serve as the substrate for the aminoimidazole carboxamide ribonucleotide transformylase/inosine monophosphate cyclohydrolase (ATIC). AICAR is an inhibitor of Hsp90, mTOR and p70 S6 Kinase.
AMP-activated protein kinase (AMPK) functions as a metabolic sensor that regulates lipid and glucose metabolism to maintain cellular energy homeostasis and to protect against metabolic stress.AICAR is a selective activator of AMPK in both hepatocytes and adipocytes. At 0.5 mM it inhibits the synthesis of fatty acids and sterols and inactivates HMG-CoA reductase in rat hepatocytes.AICAR (0.5 mM) inhibits insulin-stimulated glucose uptake to 62% of controls and reduces GLUT4 translocation 2.5-fold in 3T3-L1 adipocytes. 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.
AICAR is a cell permeable activator of AMP-activated protein kinase (AMPK), a metabolic master regulator that is activated in times of reduced energy availability (high cellular AMP:ATP ratios) and serves to inhibit anabolic processes. In vivo, pharmacologic activation of AMPK with AICAR mimics exercise and triggers insulin-independent glucose uptake by skeletal muscle.
Cell-permeable, allosteric activator of AMP-activated protein kinase (AMPK). Augments proliferation, differentiation and mineralization of osteoblastic MC3T3-EI cells and attenuates psychosine-induced expression of proinflammatory cytokines and iNOS in astrocytes. Promotes osteogenic differentiation of hAMSCs and BM-MSCsin vitro.
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