Aicar CAS 2627-69-2

Description

AICAR (chemical name: 5-Aminoimidazole-4-carboxamide ribonucleotide) is a peptide, which is an intermediate within the generation of inosine monophosphate and directly related to metabolic regulation. The most important mechanism that AICAR is known for is its ability to block enzymes both in intracellular and extracellular levels, which, in turn, allows for an accelerated stimulation of glucose uptake and increase protein kinases in skeletal muscle tissue. These two functions allow for more energy conversion, which helps burn fat and also sustain output in activity. This is what scientists and athletes/bodybuilders are interested in, but there are some amazing side effects.

Interestingly, AICAR has been shown to protect against ischemic injury. This type of injury is directly related to the restriction of blood to tissues, which can cause insufficient amounts of oxygen and glucose needed to keep the tissue alive. This can lead to thrombosis, embolisms, and vasoconstriction. AICAR can be used as a stabilizing peptide for ischemic episodes, and it can allow for proper blood flow to the myocardium (heart). This function is very interesting, as AICAR could be fundamentally used to treat the heart muscle in the aftermath of a heart attack. This might reduce the possibility for ischemic injuries. Abnormal growths of heart tissues and heart valve function have also been altered in animal studies that used the peptide AICAR, which is a downside.

Dosage

Dosages range from 150 milligrams (mg) per day (if stacked with GW), up to 500mg a day when used solo. Considering the fact that each bottle typically comes in 50mg dosages, that is quite expensive, as already mentioned above. Economically, it makes most sense to run AICAR during the 4 weeks leading up to your competition.

Function

AICAR 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, 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.

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