AICAR (5-aminoimidazole-4-carboxamide ribonucleoside) is a cell-permeable nucleoside analog (MW ~258.2 g/mol) that is phosphorylated intracellularly to ZMP, which directly activates AMP-activated protein kinase (AMPK). As an exercise mimetic, it triggers many of the same metabolic adaptations as physical exercise — including enhanced glucose uptake, fatty acid oxidation, mitochondrial biogenesis, and improved insulin sensitivity — without requiring muscular contraction. It has been studied in Phase II/III trials for cardiac ischemia and is banned by WADA as a metabolic modulator.
1 independent Janoshik purity test cover AICAR across 1 vendor.
Category: Metabolic / Exercise Mimetic. Evidence rating: C (early/mixed human evidence).
Clinical status: Phase II/III clinical trials for cardiac ischemia (acadesine). WADA-banned metabolic modulator. No FDA approval.
AICAR enters cells via adenosine transporters and is phosphorylated by adenosine kinase to ZMP (AICA ribotide), an AMP analog. ZMP allosterically activates AMPK by mimicking AMP binding at the gamma subunit. Activated AMPK then phosphorylates downstream targets including ACC (increasing fatty acid…
Safety considerations: In clinical trials (IV acadesine): transient hyperuricemia, mild hypoglycemia at higher doses; Injection site reactions with SC administration; Theoretical risk of lactic acidosis with excessive AMPK activation.
Reviewed by the PeptideAtlas Editorial Team.
| Molecular formula | C9H14N4O5 |
|---|---|
| Molecular weight | ~258.2 g/mol |
| CAS number | 2627-69-2 |
| Half-life | ~1.5-3 hours |
| Production method | synthetic |
| Anti-doping status | Prohibited in sport (WADA) |
| US regulatory status | Not FDA-approved. Investigational drug (acadesine) for cardiac ischemia. Available as research chemical. |
| Vendor | Best tested purity |
|---|
AICAR activates many of the same metabolic pathways as exercise, but it cannot replicate the full spectrum of exercise benefits (mechanical loading, cardiovascular conditioning, neuromotor coordination, bone density). It may provide some metabolic benefits for those unable to exercise but is not a complete substitute.
WADA banned AICAR in 2009 because it provides exercise-mimetic benefits (enhanced endurance, fat oxidation, glucose utilization) without requiring actual training. It was classified as a metabolic modulator.
AICAR (5-Aminoimidazole-4-carboxamide ribonucleotide) is an AMP-kinase activator researched as an exercise mimetic, promoting fat oxidation and metabolic adaptation without physical activity.
AICAR has been studied for: AMPK activation, Fat oxidation, Exercise mimetic effects, Metabolic enhancement. AMPK activator; technically a nucleoside analog, commonly grouped with peptides in research contexts.
Activates AMP-activated protein kinase (AMPK), a master metabolic regulator that shifts cellular metabolism toward fat oxidation, glucose uptake, and mitochondrial biogenesis.
Vendors with independent lab tests for it: Qingdao Sigma Chemical QSC.
Coverage on this site: MOTS-c Peptide: Metabolism, Performance, and Stress Benefits.