AICAR (5-aminoimidazole-4-carboxamide ribonucleoside) is a cell-permeable adenosine analog converted intracellularly to ZMP, an AMP mimetic used to activate AMP…
Half-life
≈0.5–2 hours (route-dependent); intracellular ZMP/PD effects persist several hours
Delivery
In vitro (media supplementation) or in vivo via IP/oral routes in animal models; IV used in cardioprotection trials—route/formulation per study design.
Suggested dosage
Not specified
Usage
Metabolic and exercise-mimetic research: glucose homeostasis, lipid metabolism, insulin sensitivity, cardioprotection, and skeletal-muscle endurance models.
Mechanism of action
Phosphorylated to ZMP, which allosterically activates AMPK and inhibits AMP-degrading enzymes, elevating AMPK signaling (e.g., ACC phosphorylation, fatty-acid oxidation, GLUT4 translocation, PGC-1α programs).
Benefits (5)
- Increases skeletal-muscle glucose uptake (insulin-independent)
- Enhances fatty-acid oxidation and reduces lipogenesis
- Activates mitochondrial biogenesis–associated gene programs
- Useful as an exercise-mimetic/comparator in preclinical models
- Enables cardiometabolic studies (e.g., ischemia–reperfusion)
Side effects (5)
- Potential hypoglycemia with excessive glucose disposal
- Gastrointestinal discomfort or nausea
- Headache or fatigue
- Altered uric-acid/purine metabolism (hyperuricemia risk)
- Elevations in liver enzymes or renal load at high dose/duration
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