AICAR Acadesine CAS 2627-69-2 platelet aggregation inhibitor
Acadesine (INN), also known as 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, AICA-riboside, and AICAR, is an AMP-activated protein kinase activator which is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as diabetes.
Acadesine is an adenosine regulating agent developed by PeriCor Therapeutics and licensed to Schering-Plough in 2007 for phase III studies. The drug is a potential first-in-class agent for prevention of reperfusion injury in CABG surgery. Schering began patient enrollment in phase III studies in May, 2009. The trial was terminated in late 2010 based on an interim futility analysis.
Product Name: Acadesine
Other Name: AICAR, GP 1-110
Appearance: White powder
Application of Acadesine:
AICAR also known as ZMP is an analog of AMP that is capable of stimulating AMPdependent protein kinase activity (AMPK). AICAR is being clinically used to treat and protect against cardiac ischemic injury. If left untreated, it may lead to a myocardial infarct. Cardiac Ischemia is caused by insufficient blood flow and oxygen to the myocardium .The drug was first used in the 1980’s as a method to preserve blood flow to the heart during surgery. Currently, the drug has also been shown as a potential treatment for diabetes by increasing the metabolic activity of tissues by changing the physical composition of muscle.
(1) Applied in phamaceutical field, it is used as phamaceutical raw material to treat injuries from fall, infectious hepatitis and epidemic cerebrospinal meningitis.
(2) Applied in healthcare field, it is used in the health products to nourish brain, protect liver and improve sleep quality.
(3) Applied in comestics, it is used to promote skin metabolism and make skin more tender and firm.
ACTIVITY OF AICAR:
AICAR (5-amino-1-β-D-ribofuranosyl-imidazole-4-carboxamide), also known as ZMP, is an analog of AMP that is capable of stimulating AMP-dependent protein kinase activity (AMPK). AICAR is being clinically used to treat and protect against cardiac ischemic injury. If left untreated, it may lead to a myocardial infarct. Cardiac Ischemia is caused by insufficient blood flow and oxygen to the myocardium The drug was first used in the 1980s as a method to preserve blood flow to the heart during surgery. Currently, the drug has also been shown as a potential treatment for diabetes by increasing the metabolic activity of tissues by changing the physical composition of muscle.
AICAR (commonly under the name Acadesine) is an analog of adenosine that enters cardiac cells to inhibit adenosine kinase and adenosine deaminase. It enhances the rate of nucleotide re-synthesis increasing adenosine generation from adenosine monophosphate only during conditions of myocardial ischemia. In cardiac myocytes, AICA-riboside is phosphorylated to AICA-ribotide (ZMP) to activate AMPK without changing the levels of the nucleotides. ZMP is able to enter the de novo synthesis pathway for adenosine synthesis to inhibit adenosine deaminase causing an increase in ATP levels and adenosine levels.
Descriptions of Acadesine:
Acadesine is an activator that permeates the cell membrane AMP-activatedproteinkinase (AMPK). AMPK is a key protein in metabolic regulation. When the energy supply is insufficient, the ratio of AMP/ATP increases, and AMPK will be activated to inhibit the synthesis of metabolism. AICAR activates AMPK, but does not affect the level of ATP, ADP, and AMP. At the cellular or animal level, AICAR can promote glucose uptake of skeletal muscle non-insulin dependence by activating AMPK. An AICAR induced glucose intake of skeletal muscle cannot be blocked by a PI3K inhibitor.
AICAR Test Report(COA):
Related substance (HPLC)
Total impurity ≤0.5%
100% pass 80 mesh
Loss on Drying
Total Plate Count
Yeast & Mold
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AICAR acts by entering nucleoside pools, significantly increasing levels of adenosine during periods of ATP breakdown.