Quickstart Highlights
AICAR (5-aminoimidazole-4-carboxamide ribonucleoside) is a research compound known to activate AMP-activated protein kinase (AMPK), leading to its informal description as an “exercise pill” after studies demonstrated that sedentary animals administered AICAR showed marked improvements in endurance. AICAR is prohibited in competitive sports, with the World Anti-Doping Agency (WADA) classifying it as a metabolic modulator, and it is not approved for therapeutic use in humans. This educational protocol outlines a once-daily subcutaneous administration approach intended for research purposes only.
- Reconstitute: Add 3.0 mL bacteriostatic water → ~16.7 mg/mL concentration.
- Research dosing range: 1,000–3,000 mcg once daily (conservative gradual approach).
- Easy measuring: At 16.7 mg/mL, 1 unit = 0.01 mL ≈ 167 mcg on a U-100 insulin syringe.
- Storage: Lyophilized: freeze at −20 °C (−4 °F); after reconstitution, refrigerate at 2–8 °C (35.6–46.4 °F) for up to 4 weeks; avoid freeze–thaw cycles.
Dosing & Reconstitution Guide
Standard / Gradual Approach (3 ml = ~ 16.7 mg/ml)
| 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) |
Frequency: Inject once daily subcutaneously. For ≤10-unit (≤0.10 mL) administrations, consider 30- or 50-unit insulin syringes for improved readability.
Reconstitution Steps
- 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.
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) |
Note: Higher-dose protocols should only be considered when explicitly supported by literature. Research doses remain well below human safety studies (up to 210 mg/kg IV), providing a wide safety margin.
Supplies Needed
Plan based on an 8-week research protocol (conservative dosing).
- Peptide Vials (AICAR, 50 mg each):
- 8 weeks (gradual 1–3 mg/day) ≈ 3 vials
- 12 weeks (2–5 mg/day advanced) ≈ 8 vials
- Insulin Syringes (U-100, or 30/50-unit for precision):
- Per week: 7 syringes (1/day)
- 8 weeks: 56 syringes
- 12 weeks: 84 syringes
- Bacteriostatic Water (10 mL bottles): Use 3.0 mL per vial for reconstitution.
- 8 weeks (3 vials): 9 mL → 1 × 10 mL bottle
- 12 weeks (8 vials): 24 mL → 3 × 10 mL bottles
- Alcohol Swabs: One for the vial stopper + one for the injection site each day.
- Per week: 14 swabs (2/day)
- 8 weeks: 112 swabs → recommend 2 × 100-count boxes
- 12 weeks: 168 swabs → recommend 2 × 100-count boxes
Protocol Overview
Concise summary of the once-daily research regimen.
- Research Goal: Activate AMPK pathways to mimic exercise-like metabolic effects.
- Schedule: Daily subcutaneous injections for 8–12 weeks (research protocols).
- Dose Range: 1,000–3,000 mcg daily (conservative); up to 5,000 mcg in advanced protocols.
- Reconstitution: 3.0 mL per 50 mg vial (~16.7 mg/mL) for precise measurements.
- Storage: Lyophilized frozen at −20 °C (−4 °F); reconstituted refrigerated 2–8 °C (35.6–46.4 °F) for up to 4 weeks.
Dosing Protocol
Suggested gradual titration approach for research.
- 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 Instructions
Proper storage preserves peptide stability and potency.
- Lyophilized: Store at −20 °C (−4 °F) in dry, dark conditions; stable up to 24 months.
- Reconstituted: Refrigerate at 2–8 °C (35.6–46.4 °F); use bacteriostatic water; stable ~4 weeks.
- Freeze–Thaw: Avoid repeated cycles; consider aliquots for long-term storage at −20 °C (−4 °F) (3–6 months).
- Allow vials to reach room temperature before opening to minimize condensation.
Important Notes
Practical considerations for research protocols.
- 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.
How This Works
AICAR acts as an agonist of AMPK, effectively simulating a state of cellular energy depletion. Following administration, AICAR enters skeletal muscle and other tissues, where it is converted to ZMP (AICAR monophosphate), an AMP analog that directly activates AMP-activated protein kinase (AMPK). AMPK functions as a central regulator of cellular energy balance, and its activation enhances glucose uptake and fatty-acid oxidation in muscle while stimulating mitochondrial biogenesis to increase cellular energy production. This metabolic shift effectively “tricks” cells into behaving as though they are exercising or fasting, triggering pathways that improve energy metabolism and endurance capacity without actual physical activity.
Potential Benefits & Side Effects
Observations from preclinical and limited human research.
- Endurance Enhancement: Sedentary mice administered AICAR demonstrated an approximate 44% increase in endurance without training, illustrating exercise-mimetic effects.
- Metabolic Improvements: Increases mitochondrial enzyme activity, fatty-acid oxidation capacity, and skeletal muscle glucose uptake; improves insulin sensitivity in animal models.
- Therapeutic Potential: Preclinical research suggests possible benefits for diabetic neuropathy protection and metabolic syndrome intervention in animal models.
- Safety Profile: Human studies using acadesine (intravenous) reported acceptable tolerability at single doses up to 210 mg/kg, with only mild and transient adverse effects; research subcutaneous doses are substantially lower.
- Side Effects: Generally well tolerated in studies; mild injection-site reactions (redness, irritation) may occur with subcutaneous administration.
- Important: Despite encouraging preclinical findings, AICAR remains experimental; no confirmed clinical benefit in humans has been established, and long-term risks are unknown.
Lifestyle Factors
Complementary strategies for research protocols.
- Maintain a balanced, protein-adequate diet to support metabolic adaptations.
- Combine with structured exercise programs to potentially enhance AMPK-mediated benefits.
- Prioritize sleep quality (7–9 hours) to support cellular recovery and energy metabolism.
- Monitor hydration status, particularly during endurance-related activities.
Injection Technique
General subcutaneous guidance from clinical best-practice resources.
- 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.
Recommended Source
We recommend Ion Peptide for high-purity AICAR (50 mg) research peptides.
Why Ion Peptide?
- High-purity, third-party-tested lots with batch Certificates of Analysis (COAs).
- Consistent quality control and ISO-aligned handling procedures.
- Reliable cold-chain shipping to help preserve peptide integrity.
- Comprehensive product documentation and storage guidelines.
Shop at Ion Peptides
Important Note
This content is provided for therapeutic educational purposes only and does not constitute medical advice, diagnosis, or treatment. AICAR is intended for research use only and is not approved for human consumption. AICAR is prohibited for use in competitive sports by the World Anti-Doping Agency (WADA).
