AICAR
Also known as: Acadesine, AICA-Riboside, ZMP precursor
5-Aminoimidazole-4-carboxamide Ribonucleotide | AMPK Activator
Overview
AICAR is a cell-permeable nucleoside analog that activates AMP-activated protein kinase (AMPK), a key regulator of cellular energy homeostasis. Originally studied for cardiac ischemia protection, it gained attention as an 'exercise mimetic' due to its metabolic effects.
Key benefits
- AMPK pathway activation
- Enhanced fatty acid oxidation
- Improved glucose uptake
- Potential endurance enhancement
- Mitochondrial biogenesis stimulation
Mechanism of action
Once inside cells, AICAR is phosphorylated to ZMP, which mimics AMP and activates AMPK. This triggers metabolic pathways typically activated during exercise: increased glucose uptake, fatty acid oxidation, and mitochondrial biogenesis.
Molecular data
- Type
- Nucleoside analog
- Half-life
- ~2-3 hours
Indications
What the research community uses this compound for, with self-reported effectiveness.
Metabolic
AMPK Activation
Most effectiveDirectly activates the master metabolic regulator through ZMP accumulation.
Fatty Acid Oxidation
EffectiveIncreases fat burning through AMPK-mediated pathways.
Glucose Metabolism
EffectiveEnhances glucose uptake independent of insulin in some tissues.
Performance
Endurance Enhancement
ModerateAnimal studies showed increased running endurance; human data limited.
Mitochondrial Biogenesis
ModerateAMPK activation promotes new mitochondria formation over time.
Cardioprotection
Ischemia Protection
ModerateOriginal clinical interest; may protect heart tissue during reduced blood flow.
Dosing protocols
Common protocols by delivery method. Adjust the curve below to model accumulation in your own cycle.
Injectable
Subcutaneous injection once daily. Progressive dosing protocols are common to assess tolerance.
| Protocol | Dose | Frequency | Route / duration |
|---|---|---|---|
| Standard Protocol | 1-3mg | Daily | SubQ |
| Gradual Introduction | 1mg → 2mg → 3mg | Daily, titrating over 4 weeks | SubQ |
| Advanced Protocol | 3-5mg | Daily for 8-12 weeks | SubQ |
Preparation
You will need
- AICAR lyophilized powder (typically 50mg vial)
- Bacteriostatic water (3.0mL recommended)
- Insulin syringes (29-31 gauge)
- Alcohol swabs
Steps
- Allow vial to reach room temperature
- Clean rubber stopper with alcohol swab
- Add 3.0mL bacteriostatic water for ~16.7mg/mL concentration
- Inject slowly along vial wall to avoid foaming
- Gently swirl to dissolve; never shake
- Label with date and store refrigerated at 2-8°C
- Use within 4 weeks of reconstitution
Work out the water volume and syringe units in the reconstitution calculator →
Interactions
Pairwise interactions with other compounds you might be cycling — the same data behind the cycle builder's safety check.
Metformin
MonitorBoth activate AMPK through different mechanisms. Combined use may have additive effects on glucose metabolism.
GW501516
SynergisticDifferent pathways (AMPK vs PPARδ) that may complement metabolic effects. Popular research combination.
SR9009
SynergisticRev-ErbA agonist with complementary metabolic effects.
Timeline
Typical week-by-week effects reported in clinical and observational data.
- Week 1-2
Subtle changes in energy levels; body adjusting to AMPK activation
- Week 3-4
Potential improvements in endurance capacity and metabolic markers
- Week 5-8
Cumulative metabolic adaptations; enhanced fat oxidation
- Week 8-12
Full effects on mitochondrial density and metabolic efficiency
Safety
Reported adverse effects, contraindications, and what to monitor on cycle.
Common side effects
- Injection site reactions
- Mild fatigue during adaptation
- Potential hypoglycemia
Stop signs — stop and seek advice
- Severe hypoglycemia symptoms
- Lactic acidosis symptoms (muscle pain, weakness, difficulty breathing)
- Unusual cardiac symptoms
- Severe fatigue or weakness
Contraindications
- Diabetes (risk of hypoglycemia)
- Cardiac conditions
- Pregnancy or breastfeeding
- Competitive athletes (WADA prohibited)
Monitoring
- Not FDA-approved for any indication
- WADA prohibited substance
- Monitor blood glucose, especially if diabetic
- Limited human safety data at research doses
Quality checks
What a legitimate product looks like, what should give pause, and what should make you stop.
Good signs
- White to off-white lyophilized powder
- Clear solution after reconstitution
- Certificate of Analysis with purity testing
Warning signs
- Slight yellowing may occur but should dissolve clearly
Stop signs — don't use
- Discolored or clumped powder
- Cloudy solution after reconstitution
- Particulate matter visible
References
Primary literature and clinical-trial data informing this entry.
AMPK and Exercise: Glucose Uptake and Insulin Sensitivity
2012
Review of AMPK role in exercise-induced metabolic adaptations and AICAR as pharmacological activator.
AICAR Mouse Endurance Study
2008
Mice treated with AICAR showed 44% increase in running endurance without training.
Last updated . How this page was sourced is described in the methodology.