AICAR
An AMPK activator and metabolic modulator that mimics the cellular effects of exercise - enhancing glucose uptake, mitochondrial biogenesis, and fat oxidation.
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Compound Profile
AICAR
Key Data
Research reference only
Research Focus
Preclinical data
⚠ Research & Educational Use Only. AICAR is a research chemical documented here for scientific education. All information references peer-reviewed literature and preclinical/clinical study data. Not for human consumption. Not medical advice. Consult a licensed researcher or healthcare professional before any laboratory use.
- Activates AMPK (AMP-activated protein kinase) - the master metabolic sensor and regulator of cellular energy balance
- Increases glucose uptake in skeletal muscle independently of insulin - relevant for insulin resistance research
- Enhances insulin sensitivity and may reduce insulin resistance in metabolic syndrome models
- AICAR is not FDA-approved for human use. It is a research chemical for scientific study only.
Research At a Glance
- Activates AMPK (AMP-activated protein kinase) - the master metabolic sensor and regulator of cellular energy balance
- Increases glucose uptake in skeletal muscle independently of insulin - relevant for insulin resistance research
- Enhances insulin sensitivity and may reduce insulin resistance in metabolic syndrome models
- Stimulates mitochondrial biogenesis - increases mitochondrial number and oxidative capacity
In Plain English
Simple summaryAICAR (5-aminoimidazole-4-carboxamide ribonucleotide) is a cell-permeable nucleotide that mimics AMP, the low-energy signal that activates AMPK -- the cellular energy sensor that responds to exercise and caloric restriction. When AMPK is activated, cells switch into energy-conservation mode: they upregulate fat oxidation, suppress anabolic processes, improve insulin sensitivity, and increase mitochondrial biogenesis. The appeal is obvious: AICAR activates the same metabolic switch that exercise does, without the exercise. In mouse models, AICAR-treated sedentary mice showed increased endurance capacity by 44%, improved glucose tolerance, and metabolic gene expression patterns resembling trained athletes -- which is why it was banned by WADA in 2009 before any approved human use existed.
- Activates AMPK - the master metabolic sensor and regulator of cellular energy balance
- Increases glucose uptake in skeletal muscle independently of insulin - relevant for insulin resistance research
- Enhances insulin sensitivity and may reduce insulin resistance in metabolic syndrome models
The full scientific detail, mechanisms, citations, and dosing data, follows below.
What is AICAR?
Tap any underlined term for an instant definition.
AICAR (5-Aminoimidazole-4-carboxamide ribonucleotide, also known as AICA riboside or Acadesine) is a nucleoside analogue that functions as an activator of AMPK (AMP-activated protein kinase) - the enzyme often called the "master regulator" of cellular energy metabolism. By mimicking cellular energy depletion, AICAR triggers a cascade of metabolic adaptations that closely parallel those induced by exercise.
AICAR is taken up by cells and phosphorylated to the monophosphate form (ZMP), which accumulates and activates AMPK. AMPK is activated when the AMP:ATP ratio rises - indicating that cellular energy stores are being depleted. Exercise causes exactly this shift, which is why AICAR is sometimes described as an "exercise mimetic." When AMPK is activated, it coordinates a comprehensive metabolic response to restore energy balance.
The downstream effects of AICAR-mediated AMPK activation include: increased glucose transporter GLUT4 translocation to the cell surface (enhancing glucose uptake independent of insulin), upregulation of fatty acid oxidation enzymes, stimulation of mitochondrial biogenesis via PGC-1alpha activation, suppression of mTOR signalling (reducing anabolic processes to conserve energy), and inhibition of inflammatory NF-kB signalling. The combination of increased glucose uptake, improved insulin sensitivity, and enhanced fat oxidation makes AICAR particularly relevant for metabolic syndrome and Type 2 diabetes research.
Perhaps the most striking published research on AICAR concerns physical performance. A landmark study in mice showed that AICAR treatment for 4 weeks increased running endurance by approximately 44%, even without exercise training. This effect was attributed to the remodelling of skeletal muscle toward a more oxidative, fatigue-resistant fibre type. This finding attracted significant interest from sports science researchers and also led WADA to add AICAR to the prohibited substances list.
The cardioprotective properties of AICAR are also well-documented. Multiple studies have shown that AICAR pre-treatment or administration during ischemia reduces myocardial infarct size and improves cardiac function in ischemia-reperfusion injury models. This effect is mediated through AMPK's ability to increase myocardial glucose utilisation even under anaerobic conditions (glycogenolysis) and through adenosine receptor activation.
By the Numbers
Key Research Benefits
Documented effects observed in preclinical and clinical studies on AICAR. See all Metabolic & Weight peptides for comparison.
Common Stacks
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Side Effects & Risks
Adverse effects reported in the research literature. All data sourced from preclinical and clinical study reports. View all peptides' side effects →
Dosing Data from the Literature
Doses referenced below are sourced from published preclinical and clinical studies. Use the peptide dose calculator to convert these values to injection volume.
AICAR research doses are typically 500 mg per day, administered subcutaneously or intravenously. Most published research uses 0.5-1 mg/kg/min in acute protocols or 500 mg/day in longer-duration studies.
Standard research dose: 500 mg/day (subcutaneous) Acute infusion protocol: 0.5-1 mg/kg/min IV (in controlled research settings) Cycle length: typically 4-8 weeks in published studies Monitor blood glucose during use - particularly at the start of protocols
Administration in Research Settings
Standard reconstitution and administration methodology for laboratory research use.
Reconstitute lyophilised AICAR powder with sterile water or bacteriostatic water. Administer subcutaneously once daily. Refrigerate reconstituted solution. Due to hypoglycaemia risk, avoid administration in a deeply fasted state without monitoring.
What the research doesn't show
Despite the dramatic mouse results, AICAR has no approved human therapeutic use and limited human pharmacology data. The 44% endurance improvement in sedentary mice is genuine -- but sedentary mice and trained human athletes are different situations, and the doses used in rodent studies would translate to very large human doses with unknown safety profiles. The 'exercise pill' narrative has not led to any completed Phase 2 human efficacy trials.
Medical Expert Videos
Physicians, researchers, and pharmacologists explain AICAR, covering mechanisms of action, clinical context, and study findings.
Videos sourced from YouTube search. KnowYourPeptide does not endorse any individual creator. For research education only.
The Bottom Line
AICAR has a growing body of preclinical evidence and a well-characterised safety profile in research settings. The most-studied application is: activates ampk - the master metabolic sensor and regulator of cellular energy balance.
The most commonly reported side effect in research subjects is hypoglycaemia risk - aicar increases glucose uptake which may cause blood sugar drops, especially if combined with insulin or other hypoglycaemic agents. It is a research chemical, not approved for human use.
Frequently Asked Questions
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Quick Reference
How It Compares
Metformin is the most widely used AMPK activator in humans -- prescribed to hundreds of millions diabetics, now being studied for longevity applications. MOTS-c activates AMPK through a different, mitochondria-derived pathway. AICAR's advantage over metformin is more direct and potent AMPK activation; its disadvantage is no approved human use and limited human safety data. For exercise mimetic research, the Narkar/Evans Cell paper made AICAR famous but human translation hasn't materialized.
Compare AICAR side-by-sideResearch Use Only
This information is for educational research purposes only. This is not medical advice. Consult a qualified healthcare professional.