AICAR
Also called AICA riboside; acadesine; converts to ZMP inside cells
An experimental metabolic compound, not a peptide, widely used in labs to activate AMPK, the cell's energy sensor. The famous "exercise in a pill" result came from mice, and a large human surgery trial was stopped for lack of benefit.
Overview
What it is
5-aminoimidazole-4-carboxamide ribonucleoside, a small molecule. Inside cells it becomes ZMP, which mimics AMP and switches on AMPK.
How it works
AMPK helps cells respond to energy demand by shifting fuel use and gene activity. It is not a simple fat-burning switch, and effects depend heavily on tissue and exposure.
What the research shows
A 2008 Cell study found four weeks of AICAR increased treadmill endurance by 44% in sedentary mice. In humans, the RED-CABG trial tested acadesine around heart bypass surgery and was stopped after 3,080 patients because it was unlikely to show benefit.
Studied for
- Endurance and metabolic genesmice
- Heart bypass surgery outcomeslarge human trial, no benefit
Safety and regulatory status
Safety and side effects
There is no established benefit-risk profile for repeated self-directed use. Product identity and quality add more uncertainty.
Regulatory status
Not approved for therapeutic use in humans. Prohibited at all times in sport by WADA/USADA as a metabolic modulator.
Mixing and dosing reference
Reference information only. Read before using this section.
AICAR (50 mg Vial) Dosage Protocol
- Vial
- 50 mg AICAR
- Add diluent
- 3 mL
- Concentration
- 16.67 mg/mL
- 1 unit (U-100)
- 166.67 mcg in 0.01 mL
- Route
- Subcutaneous
- How often
- Once per day (subcutaneous); maintain consistent AMPK activation.
- Typical range
- 1,000–3,000 mcg daily (conservative); up to 5,000 mcg in advanced protocols.
Standard / Gradual Approach
| Week/Phase | Daily Dose | Units (per injection) (mL) |
|---|---|---|
| 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) |
Advanced Protocol (Higher Doses)
| Week/Phase | Daily Dose | Units (per injection) (mL) |
|---|---|---|
| Weeks 1–2 | 2,000 mcg (2 mg) | 12 units (0.12 mL) |
| Weeks 3–6 | 3,000 mcg (3 mg) | 18 units (0.18 mL) |
| Weeks 7–12 | 5,000 mcg (5 mg) | 30 units (0.30 mL) |
How to mix
- Draw 3.0 mL bacteriostatic water with a sterile syringe.
- Inject slowly down the vial wall; avoid foaming.
- Gently swirl/roll until dissolved (do not shake).
- Label and refrigerate at 2–8 °C (35.6–46.4 °F), protected from light.
Dosing details
- Start: 1,000 mcg daily; increase by 1,000 mcg every 2 weeks as tolerated.
- Target: 2,000–3,000 mcg daily by Weeks 3–8 (conservative).
- Advanced: Up to 5,000 mcg daily if supported by protocol design.
- Frequency: Once per day (subcutaneous); maintain consistent AMPK activation.
- Timing: Any consistent time; rotate injection sites daily.
Storage
- Lyophilized: Store at −20 °C (−4 °F) in dry, dark conditions; follow the product’s validated shelf life.
- Reconstituted: Refrigerate at 2–8 °C (35.6–46.4 °F); bacteriostatic water does not establish AICAR stability or a universal use-by period.
- Freeze–Thaw: Avoid repeated cycles; do not assume that aliquoting or freezing extends the use-by period without exact-formulation stability data.
- Allow vials to reach room temperature before opening to minimize condensation.
Administration technique
- Clean the vial stopper and injection site with alcohol swabs; allow to dry completely.
- Pinch a skinfold at the chosen site; insert the needle at 45–90° angle into subcutaneous tissue.
- Inject slowly and steadily; do not aspirate for subcutaneous injections.
- Wait a few seconds after full injection before withdrawing the needle.
- Rotate sites systematically (abdomen at least 2 inches from navel, outer thighs, back of upper arms) to prevent lipohypertrophy.
- Apply gentle pressure with gauze if minor bleeding occurs; do not rub the injection site.
Important notes
- Use new sterile insulin syringes for each injection; dispose in a sharps container.
- Rotate injection sites (abdomen, thighs, upper arms) to reduce local irritation.
- Inject slowly; wait a few seconds before withdrawing the needle.
- Document daily dose, administration time, and site rotation for consistency.
- AICAR is prohibited by WADA and not approved for human therapeutic use.
Protocol source: PeptideDosages.com
Common questions
Is AICAR a peptide or a steroid?
Neither. It is a ribonucleoside.
Does AICAR replace exercise?
No. The mouse results reproduced selected metabolic responses, not the full benefits of exercise.
Is it allowed in sports?
No. It is banned in and out of competition.
Related in Performance and Recovery
Sources and further reading (5)
- Corton JM, et al. AICA riboside: a specific method for activating AMPK in intact cells? Eur J Biochem, 1995.
- Narkar VA, et al. AMPK and PPARdelta agonists are exercise mimetics. Cell, 2008.
- Effect of acadesine on outcomes after CABG: RED-CABG. JAMA, 2012.
- USADA. What athletes should know about AICAR and other prohibited AMPK activators.
- Source summary: PeptideDosages.com research overview (rewritten for NVO).