AICAR (50mg)
AICAR (5-aminoimidazole-4-carboxamide ribonucleoside) is a research compound that activates AMP-activated protein kinase (AMPK), earning it the nickname 'exercise in a pill' after studies showed sedentary animals on AICAR experienced dramatic improvements in endurance. AICAR is banned in sports (WADA) and is not approved for therapeutic use in humans. This protocol outlines a daily subcutaneous approach for research purposes only.
Reviewed by the AllPeptides.eu Editorial Team·Last reviewed: 2026-06-16
Educational information. Not medical advice, and no efficacy claim is implied. Regulatory approval is not a use recommendation by AllPeptides.eu.
⚠️ For informational/educational purposes only. Not medical advice. We do not sell any products. Self-treatment carries serious risks — consult a healthcare professional. Disclaimer
Research monograph
See the full AICAR encyclopedia page with mechanism, evidence tier, related variants and research context.
How It Works
AICAR functions as an AMPK agonist, essentially mimicking a state of cellular energy depletion. After administration, it enters skeletal muscle cells where it is metabolized into ZMP (AICAR monophosphate), an AMP analog that directly activates AMPK. AMPK is a master regulator of cellular energy homeostasis; its activation stimulates glucose uptake and fatty acid oxidation in muscles while promoting mitochondrial biogenesis. This metabolic shift 'tricks' the cells into responding as if they were exercising or fasting.
Quick Start
- Reconstitution: Add 3.0 mL bacteriostatic water → ~16.7 mg/mL concentration.
- Research Dosing Range: 1,000–3,000 mcg once daily (titration approach).
- Storage: Lyophilized: −20 °C; after reconstitution, refrigerate at 2–8 °C for up to 4 weeks; avoid freeze-thaw cycles.
Standard / Titration Approach (3 mL = ~16.7 mg/mL)
Route: Subcutaneous | Frequency: Once daily
| Week | Dose | Units (per injection) |
|---|---|---|
| Weeks 1–2 | 1,000 mcg (1 mg) | 6 Units (0.06 mL) |
| Weeks 3–4 | 2,000 mcg (2 mg) | 12 Units (0.12 mL) |
| Weeks 5–8 | 3,000 mcg (3 mg) | 18 Units (0.18 mL) |
Studies report administration once daily subcutaneously.
Related compounds
Reconstitution Steps
- Draw up 3.0 mL of bacteriostatic water.
- Slowly inject against the vial wall; avoid foaming.
- Gently swirl/roll (do not shake vigorously).
- Label and refrigerate at 2–8 °C, protecting from light.
Protocol Overview
- Research Goal: Activate AMPK pathways to mimic metabolic effects of exercise.
- Schedule: Daily subcutaneous injections for 8–12 weeks.
- Storage: Lyophilized frozen; reconstituted refrigerated for up to 4 weeks.
Dosing Protocol
- Initiation: 1,000 mcg daily; increase by 1,000 mcg every 2 weeks.
- Target: 2,000–3,000 mcg daily (Wks 3–8).
- Advanced: Up to 5,000 mcg daily if supported by protocol design.
- Frequency: Once daily (subcutaneous).
- Timing: Any consistent time; rotate sites.
- Break between cycles: Post-cycle, a pause of 4–6 weeks is recommended. AICAR activates AMPK—the pause prevents metabolic adaptation and tolerance.
Washout & Cycle Restart
When can I restart?
Post-cycle, a pause of 4–6 weeks is recommended. AICAR activates AMPK—the pause prevents metabolic adaptation and tolerance.
Minimum wait period: 4 weeks
Storage Instructions
- Lyophilized: Store at −20 °C; stable for up to 24 months.
- Reconstituted: Refrigerate at 2–8 °C; use bacteriostatic water; stable for ~4 weeks.
- Freeze-Thaw: Avoid cycles; consider aliquoting for long-term storage.
- Allow vials to reach room temperature before opening.
Important Notes
- Regulatory Note: AICAR is banned by WADA and is not approved for human therapeutic use.
Potential Benefits & Side Effects
Potential Benefits:
- Endurance Enhancement: Sedentary mice on AICAR showed a +44% increase in endurance without training.
- Metabolic Improvements: Increases mitochondrial enzymes, fat oxidation capacity, and glucose uptake.
- Therapeutic Potential: Potential protection against diabetic neuropathy in animal models.
- Safety Profile: Human trials (acadesine, IV) tolerated up to 210 mg/kg.
- Generally well-tolerated; potential for mild injection site reactions.
Potential Side Effects:
- Hypoglycemia (rare).
- Gastrointestinal discomfort.
- Fatigue (transient).
- Potential impact on uric acid.
⚠️ Serious Warnings & Long-Term Risks
The following warnings are based on published literature, FDA labels, and post-marketing surveillance. They do not constitute medical advice. Consult a healthcare professional.
Bradycardia & hypotension
AICAR (acadesine) caused bradycardia and hypotension in IV clinical trials. Data for subcutaneous research use is limited.
📄 J Am Coll Cardiol 1996Uric acid increase & gout risk
Metabolized to AMP → IMP → uric acid. Chronic use may increase serum uric acid.
📄 Am J Physiol 1998References
- U.S. Anti-Doping Agency (USADA) — AICAR and Prohibited AMPK Activators
View Source - PubMed (2017) — AICAR endurance enhancement in sedentary animals
View Source - PMC (2010) — AICAR normalizes skeletal muscle dysregulation in obesity
View Source - PubMed (2013) — Acadesine Phase I/II: maximum tolerated dose 210 mg/kg IV
View Source - Cell Signaling Technology — AICAR (Acadesine): AMPK activation mechanism
View Source
External Sources & Regulatory Status
Regulatory Approvals
Cardiac surgery / AMPK
Phase II (cardioprotection)
Educational information. Not medical advice, and no efficacy claim is implied. Regulatory approval is not a use recommendation by AllPeptides.eu.
Continue Your Research
Explore tools and guides related to this protocol.
Important Disclaimer
The content of this website is provided exclusively for informational and educational purposes within the context of research literature.
Read the full Disclaimer →