What is AICAR used for?

AICAR is a natural peptide known for stimulating AMPK activity in the skeletal muscle of the body. The increase in AMPK activity, as a result, potentially leads to fat-burning and increased energy production. AICAR is essentially a molecule that stands for 5-Aminoimidazole 4-carboxamide 1 ribonucleotide. The compound has gained immense popularity in the fields of biochemistry and medical research due to its potential effects on cellular metabolism and its possible applications in various health-related areas through its interaction with stem cells.


In order to find out more about AICAR, let us first analyze what AMPK is. AMP-activated protein kinase is an evolutionary enzyme best known for sensing conserved fuel in all mammalian b cells. Exercise enhances learning and memory in animals and humans alike. As the benefits of running on brain function have not been examined to the extent to which we would like, it is unknown whether AMP-kinase (AMPK) activation in muscle can predict the enhancement of brain plasticity. However, scientists do know that, during exercise, AMPK is activated in skeletal muscle in humans, and rodents such as mice, thereby increasing the AMP/ATP ratio {R}.

Product Information

This natural peptide analog of adenosine monophosphate (AMP) has made real headlines in cell biology. This stem cells-permeable nucleotide has been found capable of stimulating AMPK activity by affecting the cell cycle in the body which has not only made AICAR probably the best performance-enhancing drug on the market but is also known to increase fatty acid oxidation, hence resulting in fat burn.

Multiple studies have been conducted to investigate the potential effects of AICAR (5-Aminoimidazole 4-carboxamide 1 ribonucleotide). In one such study, it inhibited cholesterol synthesis in liver stem cells. A human study involving healthy male subjects has found that it may increase glucose uptake in skeletal muscle cells {R}.

In mice, administration of this led to improved cognition and motor coordination. A separate study found that AICAR inhibits cancer cell proliferation by different mechanisms. Lastly, in an animal model of myocardial infarction, it improved scar formation in the heart {R}.

How Does AICAR Work?

Biological Activity

AICAR activates AMPK cells including acadesine. Resultantly, Acadesine induces apoptosis of B-CLL cells in a dose-dependent manner. Let’s see how AICAR-treated cells work in simple terms:

  1. Energy Control Center: Think of your body as a machine that needs energy to run, like a car needing fuel. Inside your cells, there’s an “energy control center” called AMP-activated protein kinase, or AMPK for short. This control center monitors the energy levels in your cells.
  2. Low Energy Trigger: This can be compared to when your cells are running low on energy, like when you’re exercising really hard or not eating enough, hence activating AMPK. It’s like a warning light turning on in your car when the fuel is running low.
  3. AICAR as a Signal: AICAR is a chemical that can act like a signal to activate AMPK, “Hey, we need more energy!” So, when you take AICAR or introduce it into your cells, this AMPK activator acts like pressing a button to activate AMPK by telling your body to start increasing energy levels.
  4. Boosting Energy Production: When AMPK is activated by AICAR, it starts a chain reaction of AMP-activated protein kinase in your intact cells. This chain reaction helps your cells make more energy by breaking down sugar and fat. It’s like getting your car’s engine to work harder to produce more power.
  5. Exercise-Like Effects: AICAR can make your cells act as if you’re exercising, even if you’re not. It makes them more efficient at using energy and can improve their endurance, just like regular exercise does.

So, in simple terms, AICAR is like a message that tells your body’s energy control center to work harder, helping you make more energy and potentially improving your fitness. However, please note that AICAR should only be used under proper medical supervision.


AICAR has been one of the most widely used pharmacological modulators for activating AMPK activity. The majority of early studies on the role of AMPK or activating AMPK, both in the physiological regulation of metabolism and in cancer pathogenesis, were based solely on the use of AICAR in rat hepatocytes to activate AMPK in eukaryotic cells. Even with more complex models of AMPK down-regulation and knockout being introduced, AICAr remained a regular starting point for many studies focusing on AMPK biology. AICAR has shown beneficial effects for the treatment of diseases related to metabolism, hypoxia, exercise, nucleotide synthesis, and cancer-causing cells {R}.

How do AICAR and AMPK impact performance?

Activated protein kinase ampk plays a major role in maintaining energy homeostasis within stem cells by responding to changes in the ratio of AMP (adenosine monophosphate) to ATP (adenosine triphosphate), which are key indicators of cellular energy status. When cellular ATP levels decrease, leading to an increase in AMP, AMPK (amp-activated protein kinase) is activated to restore energy balance. Allosteric mechanisms allow effectors to bind to the protein resulting in a change in protein dynamics.

AICAR mimics this process and activates AMPK through a mechanism involving its conversion to an AMP analog. Here’s a simplified explanation of how AICAR activates AMPK.

  • Conversion to ZMP: When AICAR enters cells, it forms ZMP (5-aminoimidazole-4-carboxamide ribotide). This conversion is facilitated by cellular enzymes.
  • Mimicking AMP: ZMP structurally resembles AMP (adenosine monophosphate). AMPK, the cellular energy sensor, normally detects an increase in the AMP: ATP ratio as a signal of low energy. ZMP essentially “tricks” AMPK into thinking that there is an energy deficit because it closely resembles AMP.
  • Binding to AMPK: ZMP binds to the regulatory subunits of AMPK, causing a change that exposes the catalytic sub-units of the enzyme.
  • Activation of AMPK: With the catalytic subunits now exposed, AMPK becomes active. Active AMPK can phosphorylate a variety of target proteins involved in metabolic pathways to promote energy-producing processes (e.g., glucose uptake and fatty acid oxidation) and inhibit energy-consuming processes (e.g., protein synthesis and lipid synthesis).

AICAR (5-Aminoimidazole 4-carboxamide 1 ribonucleotideis) is a potential tool in research and medicine for studying cellular energy regulation and treating conditions related to energy metabolism, such as obesity and type 2 diabetes.


Popularity in Body-building Industry

AICAR has lately become very popular in the bodybuilding industry as it has shown anabolic effects on skeletal muscles (through osteogenic differentiation) and fat reduction. Here are some of the benefits that make AICAR a treat for bodybuilders:

  • AICAR may enhance insulin sensitivity, making cells more responsive to insulin’s actions. This effect could be beneficial for individuals with insulin resistance or type 2 diabetes.
  • AICAR has been studied for its potential to promote fat loss by increasing the utilization of fatty acids for energy. It may help reduce body fat in animal models.
  • AICAR has demonstrated potential benefits for the cardiovascular system. It may protect against heart damage and improve cardiac function, especially in the context of ischemic conditions.
  • AICAR has been shown to improve endurance and exercise stamina. This could be valuable for athletes and individuals looking to enhance their physical performance.

AICAR Peptide as a drug

AICAR (50 mg)

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While the above benefits are purely performance-enhancing tools, AICAR (5-aminoimidazole 4 carboxamide 1 β) has shown its potential in the treatment of numerous diseases including:


  • AICAR has shown promising results in treating Type 2 diabetes. As discussed earlier, AICAR activates acadesine. In return, acadesine induces apoptosis in human cells (adenosine kinase). A human study provides evidence that AICAR acts to prevent and treat type-2 diabetes, that too, in lower concentrations. The study demonstrates a reduction of glucose production and improvement in glucose level regulation in diabetes patients with aicar-treated cells. {R}

Brain Improvement

  • Brain improvement is another breakthrough that may be achieved through AICAR in the coming years. Results obtained from various tissues of an animal study of isolated hepatocytes show that it improves cognition and motor coordination in young and aged mice. Furthermore, the brain, genes relevant to neuronal development and plasticity were enriched following AICAR administration. {R}

Heart Health

  • AICAR demonstrated its remarkable potential when it successfully facilitated the healing of a heart scar in a rodent experiment. A rat study was conducted to determine whether it stimulates myocardial glycogenolysis, decreases oxidative stress, and abrogates placental ischemia-induced hypertension.
  • In a rodent model of reperfused MI, it improved scar formation in the aged heart. This was accompanied by enhanced collagen deposition and collagen fiber maturation in the heart. These findings show a potential therapeutic strategy to prevent adverse remodeling in the aging heart. {R}


  • Perhaps the biggest benefit the world is waiting for is the potential of AICAR in potential treatment of cancer cells and associated cell lines. One study investigated the effects of this substance in the treatment of tumor growth in human osteosarcoma, both in specific methods in vitro and in vivo. The findings in this study strongly suggest that it could be considered a potential therapeutic agent for treating human osteosarcoma.
  • Another study substantiated the effects of this regulatory-associated protein on thyroid cancer. It noted that it reduces thyroid cancer cell growth, invasion, and metastasis. {R}

AICAR and Sperm Motility

Sperm motility is the ability of sperm to move fluently through the woman’s reproductive tract for better fertility chances. Poor sperm motility is one of the various factors responsible for male factor infertility. Studies in chickens have shown signs of improving motion characteristics and fertilizing ability of cryo-preserved sperm, to the control. {R}
Lastly, treatment of various metabolic disorders is also known to be another potential massive benefit of this supplement.

Dosage AICAR

Dosages range from 150 mg per day up to 500 mg when used solo. Considering the fact that each bottle typically comes in 50 mg dosages, that is quite expensive, as already mentioned above. With the above in view, AICAR is more feasible to be used fr 4 weeks at a time.  It is, however, recommended to take professional guidance before use of AICAR (5-aminoimidazole 4 carboxamide aica ribonucleotide).

Potential Side Effects:

Since it affects various cell types during blood flow, AICAR-treated cells can cause less blood to go to your brain and heart valve tissues. This significant difference in blood flow can result in side effects such as diarrhea and thirst are common. Other less common side effects of its mechanistic target may include:

  • Metabolic Effects/ Adenosine Deaminase (ADA)
  • Cardiovascular Effects
  • Exercise-Related Effects

Is AICAR Legal?

The legal status of AICAR (5-aminoimidazole 4 carboxamide 1 ribonucleotide) varies by country and jurisdiction. In many countries, AICAR is not approved for clinical use or over-the-counter sale as it is primarily used for research purposes. However, it may be available for purchase from research chemical suppliers for laboratory or scientific research purposes.

Further research is needed to fully understand its mechanisms and assess its safety and efficacy in humans in terms of Aicar treatment. Moreover, the World Anti-Doping Agency and FDA are yet to approve the drug in sports.

Where to Buy AICAR

This is one nitric oxide supplement that you should buy if fat loss and performance enhancement are what you’re after. PureRawz is the best place to buy AICAR online.

In order to be the best supplier of research peptides, we provide reference materials with every product we sell. In addition, all our research chemicals come with an independent, third-party-issued Certificate of Analysis for identification, purity, and concentration.

We offer free international shipping on all orders above $100. You can pay for your purchase through various methods, including PayPal and Bitcoin. Click on the ‘Reviews’ tab to check out what existing customers say about our products and great customer service. {R}

About Author

Calvin Ramos

Calvin Ramos is a dedicated research and fitness enthusiast with a passion for helping individuals achieve their health and wellness goals. With years of experience in the fitness industry and a deep commitment to staying up-to-date with the latest research and developments in the field, Calvin brings a wealth of knowledge and expertise to his articles. As a fitness coach and nutrition specialist, Calvin has helped countless clients transform their lives through personalized training programs and evidence-based dietary recommendations. He holds a Bachelor's degree in Exercise Science and Nutrition from University and is certified in personal training and sports nutrition. Calvin's writing reflects his commitment to providing accurate and trustworthy information to empower readers on their fitness journeys. He believes in the power of education and strives to make complex fitness concepts accessible to everyone. His articles are thoroughly researched, drawing on the latest scientific studies and expert insights. When he's not writing or coaching, you can find Calvin in the gym, experimenting with new workout routines, or exploring the latest advancements in fitness technology. His dedication to the field of fitness and wellness is evident in his articles, which aim to inspire and inform readers on their path to a healthier, happier life.