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How does AICAR activate AMPK?  

04/14/2022

AICAR, short for 5-aminoimidazole-4-methamide-1-molar D-ribofuranoside, also known as AICARiboside or Acadesine,  is a kind of activated agent that permeates cell membrane AMP-activated protein kinase(AMPK) .  
AMPK is a key protein in metabolic regulation, which can regulate cell energy and control cell metabolism.  
AICAR is a recognized AMPK activator that plays an important role in the medical field. How does AICAR activate AMPK?  

AMPK is a complex heterotrimer structure consisting of a catalytic subunit and two regulatory subunits. α subunit (α1 and α2) is a catalytic subunit with a molecular weight of 63KD.  β and γ subunits are regulatory subunits. β subunit contains β1 and β2 isomers.  There are 3 isomers of γ1, γ2 and γ3 in γ subunit.  AMPK is widely distributed in eukaryotic cells. AMPKα1 is mainly distributed in liver, kidney, heart, lung, brain and islet β cells.  AMPKα2 is mainly distributed in skeletal muscle, heart and liver.  In terms of cell distribution, AMPKα1 and AMPKα2 are also different, with AMPKα1 mainly distributed in the cytoplasm and AMPKα2 mainly in the nucleus.  

AMPK activity is regulated by energy changes in cells, and is a monitor of cell energy changes, mainly regulated by AMP/ATP ratio in cells.  Under normal conditions, the RATIO of AMP/ATP remains stable to maintain the basic metabolic energy requirements of cells. When cells are under stress, such as ischemia, hypoxia, starvation, intracellular PH changes, oxidative stress and creatine/phosphate ratio increase, the RATIO of AMP/ATP will increase.  Thus, AMPK is activated and downstream signal molecules are activated or suppressed, which reduces anabolism, promotes catabolic process, improves ATP production, and restores AMP/ATP ratio to normal and maintains stability.  

AICAR is an adenosine analogue that catalyzes the formation of its mononucleotide derivative ZMP by adenosine kinase in vivo or in cells. ZMP has an AMp-like effect, resulting in an increase in AMP/ATP ratio and activation of AMPK.  

The AMPK pathway has been found to inhibit tumor cell formation in normal tissues and has been shown to be toxic to most human tumor cell lines in vitro, making AMPK a new target for cancer therapy. AICAR, which can activate AMPK, also has antitumor effects.  

Based on the role of AMPKα1 in islet cells, ACTIVATION of AMPK by AICAR inhibits fat synthesis, thereby reducing fat content in the body at its root.  

Based on the role of AMPKα2 in skeletal muscle, AICAR activates AMPK, which contributes to muscle growth and is therefore suitable for fitness.  

With the deepening of research on AICAR, AICAR, a new powder, has come into people’s sight. However, after understanding AICAR and its functions, no matter what purpose AICAR is used for, the quality of the powdr needs to be paid attention to first.  

We are the manufacturer of AICAR, providing AICAR powder with purity higher than 99%. HPLC,MS, and HNMR tests are used for each batch of products to ensure product quality.  

If you are interested in our products, you can contact us for more product information.  

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