AICAR (50mg)

What is the AICAR Peptide?

AICAR or 5-Aminoimidazole-4-carboxamide ribonucleotide is a synthetic adenosine monophosphate analog. It was developed to stimulate the AMP-dependent protein kinase (AMPK) activity^[1]. It is currently being investigated as a protective agent against ischemic damage in the cardiac myocytes in the event of cardiac injury. The AMP-activated protein kinase is an enzyme and a protein that plays a regulatory role in several metabolic pathways. Its expression has been observed in several tissues, including the skeletal muscles, liver, and brain. In all these tissues, it appears to have a net effect on lipogenesis, and may inhibit cholesterol synthesis and ketogenesis. It may also modulate insulin secretion and skeletal muscle fatty acid oxidation with glucose uptake. Several energy deficit states in the body can trigger the release of AMPK, like hypoxia or hypoglycemia. This process makes AICAR an important investigational peptide for its potential of being used as a treatment for diabetes. It has also been investigated for its role in reversing cardiac ischemic injury.

Specifications

SYNONYMS: Z-nucleotide, 5-amino-4-imidazolecarboxamide ribotide, 5′-Phosphoribosyl-5-amino-4-imidazolecarboxamide

MOLECULAR WEIGHT: 338.213 g/mol

MOLECULAR FORMULA: C₉H₁₅N₄O₈P

PUBCHEM:CID 65110

RECONSTITUTION: Required

Research

AICAR and the Heart
The incidence of cardiovascular disease (CVD) in the modern world and the fatalities associated are growing. Its prevalence makes it one of the most widely researched diseases in the medical field. AICAR has been researched for its potential two-way protective role in protecting the heart from the ischemia associated with CVD. Inflammation is a significant contributor to the disease pathology in atherosclerosis and other heart diseases. Research conducted on rabbits has posited that AICAR may surpress vascular smooth muscle proliferation^[3]. The control of vascular inflammation reduces the risk of short-term and long-term complications of stent placement, and also contributes to the overall health of the heart. One of the immune responses that trigger a heart attack is macrophage proliferation in response to high LDL (bad cholesterol) levels. AICAR may play a role in suppressing this immune response^[4]. This potential would mitigate the risk of precipitation of a heart attack.
If a heart attack does occur, AICAR has been studied for its potentially protective properties, delaying the process of cell death by a process called preconditioning. By the same coin, AICAR, in an ischemic heart, appears to reduce the frequency and size of the infarct by up to 25%. It may also improve the overall blood flow to the heart.

AICAR and Insulin Resistance
Insulin resistance results from inflammation in the fatty tissues. This process results in raised blood glucose levels. The suppression of inflammation results in increased insulin sensitivity with improved glucose homeostasis. AICAR, via its possible anti-inflammatory role in different metabolic pathways, may improve insulin sensitivity and lipid metabolism. In diabetic mice, AICAR administration was observed to reduce blood glucose levels without body weight changes^[5]. AICAR appears to mimic the effect that exercise has on glucose uptake by muscles. It has the potential to upregulate the GLUT-4 receptors on muscles that are prime transporters involved in glucose uptake.

AICAR and Cancer
AICAR, via its AMPK activation, may play a role in cancer cell metabolism. In research conducted on cell cultures and rats, prolonged AICAR administration appeared to slow down the metabolism of cancer cells and hence their proliferation^[6]. It also may make the cancerous cells more vulnerable to harsh environmental factors. This vulnerability in cancer cells may support future AICAR trials to explore its suitability for cancer treatment adjunctive use with chemotherapeutic agents. Thyroid cancer cell research has also suggested that AICAR may induce apoptosis in cancer cells by p21 induction and caspase-3 activations, potentially causing inhibition of cancer cell proliferation.

AICAR and Fertility
For a very long time, a large amount of AICAR research has been directed toward its potential benefit in improving male fertility. Various studies on cats, dogs, and mice have observed that AMPK activation appears to improve fertility^[7]. Since AICAR is an apparently effective AMPK activator, its long-term administration may lead to improved sperm motility. Since AICAR may regulate the activity of all the active enzymes involved in sperm motility, its administration has the potential to provide a profound positive effect on fertilization.

AICAR and Inflammation
AMPK activation appears to have an overall anti-inflammatory effect at a cellular level. Inflammation forms a part of the pathogenesis of several diseases in the body. The same is valid for diabetes, making AICAR an potential for diabetic therapy. But its potential as an anti-inflammatory in disease processes does not stop here. Animal research has shown its potential benefit in various inflammatory disorders like hepatitis, acute lung injury, asthma, colitis, and atherosclerosis^[8]. To conclude, AICAR may have significant cardioprotective properties. It has been studied for its possible abilities to improve metabolic health and complications associated with it. It finds use in cancer treatment studies and a variety of inflammatory condition research as well.

References