Overview
AICAR (5-aminoimidazole-4-carboxamide ribonucleoside) is a research compound that activates AMP-activated protein kinase (AMPK), often called an “exercise pill” because sedentary animals given AICAR showed dramatic endurance improvements in studies.
Key Status
– Not approved for human therapeutic use
– Prohibited by WADA (classified as metabolic modulator)
– Research use only
Reconstitution & Storage
Standard Reconstitution
– Volume: Add 3.0 mL bacteriostatic water to 50 mg vial
– Final Concentration: ~16.7 mg/mL
– Measurement: 1 unit on U-100 insulin syringe ≈ 167 mcg
Storage Instructions
| Form | Temperature | Duration | Notes |
|---|---|---|---|
| Lyophilized | −20°C (−4°F) | Up to 24 months | Dry, dark conditions |
| Reconstituted | 2–8°C (35.6–46.4°F) | ~4 weeks | Use bacteriostatic water; avoid freeze–thaw cycles |
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Dosage Protocols
Conservative/Gradual Approach (8 weeks)
| Week/Phase | Daily Dose | Units (U-100) | Volume (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 |
Frequency: Once daily subcutaneous injection
Advanced Protocol (12 weeks)
| Week/Phase | Daily Dose | Units (U-100) | Volume (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 |
Note: Higher-dose protocols should only be used when explicitly supported by literature. Research doses remain well below human safety studies (up to 210 mg/kg IV).
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Reconstitution Steps
1. Draw 3.0 mL bacteriostatic water with sterile syringe
2. Inject slowly down vial wall; avoid foaming
3. Gently swirl/roll until dissolved (do not shake)
4. Label and refrigerate at 2–8°C, protected from light
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Mechanism of Action
AICAR enters cells and metabolizes to ZMP, an AMP analog that directly activates AMPK. This “master regulator of cellular energy” stimulates:
– Glucose uptake and fatty-acid oxidation in muscle
– Mitochondrial biogenesis
– Enhanced cellular energy output
The effect essentially mimics an energy-depleted state, triggering exercise-like metabolic responses without physical activity.
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Injection Technique
Preparation
– Clean vial stopper and injection site with alcohol swabs; allow to dry completely
– Pinch skinfold at injection site
Administration
– Insert needle at 45–90° angle into subcutaneous tissue
– Inject slowly and steadily
– Do not aspirate for subcutaneous injections
– Wait a few seconds before withdrawing needle
– Apply gentle pressure with gauze if bleeding occurs; do not rub
Site Rotation
Rotate injection sites systematically to prevent lipohypertrophy:
– Abdomen (at least 2 inches from navel)
– Outer thighs
– Back of upper arms
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Supplies Needed
For 8-Week Conservative Protocol
– AICAR Vials: ~3 vials (50 mg each)
– Insulin Syringes (U-100): 56 syringes (1 per day)
– Bacteriostatic Water: 1 × 10 mL bottle (need 9 mL total)
– Alcohol Swabs: 2 × 100-count boxes (112 swabs needed)
For 12-Week Advanced Protocol
– AICAR Vials: ~8 vials (50 mg each)
– Insulin Syringes (U-100): 84 syringes (1 per day)
– Bacteriostatic Water: 3 × 10 mL bottles (need 24 mL total)
– Alcohol Swabs: 2 × 100-count boxes (168 swabs needed)
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Protocol Overview
| Aspect | Details |
|---|---|
| Goal | Activate AMPK pathways to mimic exercise-like metabolic effects |
| Schedule | Daily subcutaneous injections for 8–12 weeks |
| Dose Range | 1,000–3,000 mcg daily (conservative); up to 5,000 mcg (advanced) |
| Frequency | Once per day; maintain consistent AMPK activation |
| Timing | Any consistent time; rotate injection sites daily |
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Important Notes & Best Practices
– Use new sterile insulin syringes for each injection; dispose in sharps container
– Rotate sites daily to reduce local irritation
– Inject slowly; wait seconds before withdrawing needle
– Document daily dose, administration time, and site rotation
– AICAR is prohibited by WADA and not approved for human therapeutic use
– For ≤10-unit administrations, consider 30- or 50-unit insulin syringes for improved readability
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Complementary Lifestyle Factors
– Maintain balanced, protein-adequate diet to support metabolic adaptations
– Combine with structured exercise programs to potentially amplify AMPK-mediated benefits
– Prioritize sleep quality (7–9 hours) for optimal cellular recovery and energy metabolism
– Monitor hydration status, especially during endurance activities
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Disclaimer
This content is for educational research purposes only and does not constitute medical advice, diagnosis, or treatment. AICAR is research use only and not approved for human consumption. AICAR is prohibited by WADA for use in competitive sports. Always consult qualified healthcare professionals before beginning any research protocol.