AICAR (Acadesine)

5-Aminoimidazole-4-carboxamide Ribonucleotide | AMPK Activator

Weight: 338.21 Da
Half-life: ~2-3 hours
2 studies
2012 latest
limited
Dose 1-5mg daily
Frequency Once daily
Cycle 8-12 weeks
Storage Lyophilized: -20°C; Reconstituted: 2-8°C for 4 weeks
Accumulation Plotter

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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.

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.

01 AMPK pathway activation
02 Enhanced fatty acid oxidation
03 Improved glucose uptake
04 Potential endurance enhancement
05 Mitochondrial biogenesis stimulation

Molecular Data

Molecular Weight
338.21 Da
Type
Nucleoside analog
Peak 0.0 mcg
Trough 0.0 mcg
SS Peak 0.0 mcg
SS Trough 0.0 mcg

Research Indications

Metabolic
AMPK Activation most effective

Directly activates the master metabolic regulator through ZMP accumulation.

Fatty Acid Oxidation effective

Increases fat burning through AMPK-mediated pathways.

Glucose Metabolism effective

Enhances glucose uptake independent of insulin in some tissues.

Performance
Endurance Enhancement moderate

Animal studies showed increased running endurance; human data limited.

Mitochondrial Biogenesis moderate

AMPK activation promotes new mitochondria formation over time.

Cardioprotection
Ischemia Protection moderate

Original clinical interest; may protect heart tissue during reduced blood flow.

Dosing Protocols

Subcutaneous injection once daily. Progressive dosing protocols are common to assess tolerance.

GoalDoseFrequencyRoute
Standard Protocol1-3mgDailySubQ
Gradual Introduction1mg → 2mg → 3mgDaily, titrating over 4 weeksSubQ
Advanced Protocol3-5mgDaily for 8-12 weeksSubQ

Reconstitution Instructions

Materials Needed:
  • AICAR lyophilized powder (typically 50mg vial)
  • Bacteriostatic water (3.0mL recommended)
  • Insulin syringes (29-31 gauge)
  • Alcohol swabs
  1. 1 Allow vial to reach room temperature
  2. 2 Clean rubber stopper with alcohol swab
  3. 3 Add 3.0mL bacteriostatic water for ~16.7mg/mL concentration
  4. 4 Inject slowly along vial wall to avoid foaming
  5. 5 Gently swirl to dissolve; never shake
  6. 6 Label with date and store refrigerated at 2-8°C
  7. 7 Use within 4 weeks of reconstitution

Interactions

~
Metformin
Both activate AMPK through different mechanisms. Combined use may have additive effects on glucose metabolism.
monitor
++
GW501516
Different pathways (AMPK vs PPARδ) that may complement metabolic effects. Popular research combination.
synergistic
++
SR9009
Rev-ErbA agonist with complementary metabolic effects.
synergistic

What to Expect

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

Side Effects & Safety

Common Side Effects

  • Injection site reactions
  • Mild fatigue during adaptation
  • Potential hypoglycemia

Stop Signs - Discontinue if:

  • 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)

Quality Checklist

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

Bad Signs

  • Discolored or clumped powder
  • Cloudy solution after reconstitution
  • Particulate matter visible

References

  • 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.

Disclaimer

This information is for educational and research purposes only. Consult a healthcare professional before use.