PRODUCT

AICAR (50 mg Vial)

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Quickstart Highlights

AICAR (5-aminoimidazole-4-carboxamide ribonucleoside) is a research compound that activates AMP-activated protein kinase (AMPK)[1], earning the nickname “exercise pill” after studies showed sedentary animals given AICAR experienced dramatic endurance improvements[2]. AICAR is prohibited in sports (WADA classifies it as a metabolic modulator) and is not approved for therapeutic use in humans[1]. This educational protocol presents a once-daily subcutaneous approach 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.

Reconstitution

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.
Label and refrigerate at 2–8 °C (35.6–46.4 °F), protected from light.

Protocol Overview

Research Goal:Activate AMPK pathways to mimic exercise-like metabolic effects[1][6].
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[14].

Dosage Protocols

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).
Frequency:Once per day (subcutaneous); maintain consistent AMPK activation[3].
Timing:Any consistent time; rotate injection sites daily.

Storage Instructions

Lyophilized:Store at −20 °C (−4 °F) in dry, dark conditions; stable up to 24 months[14].
Reconstituted:Refrigerate at 2–8 °C (35.6–46.4 °F); use bacteriostatic water; stable ~4 weeks[14]. Freeze–Thaw: Avoid repeated cycles; consider aliquots for long-term storage at −20 °C (−4 °F) (3–6 months)[14].

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[11].
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[1].

How It Works

AICAR functions as an AMPK agonist, essentially mimicking an energy-depleted cellular state[6]. After administration, AICAR enters skeletal muscle and other cells where it is metabolized to ZMP (AICAR monophosphate), an analog of AMP that directly activates AMP-activated protein kinase (AMPK)[6]. AMPK serves as the master regulator of cellular energy homeostasis, and its activation stimulates glucose uptake and fatty-acid oxidation in muscle while promoting mitochondrial biogenesis to boost cellular energy output[1][6]. This metabolic shift “tricks” cells into responding as if exercising or fasting, activating pathways that improve energy metabolism and endurance capacity without actual physical activity.

Lifestyle Factors

Maintain a 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) to optimize cellular recovery and energy metabolism.
Monitor hydration status, especially during endurance activities.

Injection Technique

Clean the vial stopper and injection site with alcohol swabs; allow to dry completely[11].
Pinch a skinfold at the chosen site; insert the needle at 45–90° angle into subcutaneous tissue[12].
Inject slowly and steadily; do not aspirate for subcutaneous injections[12].
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[11].
Apply gentle pressure with gauze if minor bleeding occurs; do not rub the injection site[11].

Benefits and Side Effects

Benefits

Endurance Enhancement: Sedentary mice treated with AICAR showed a remarkable +44% increase in endurance without training[2], demonstrating exercise-mimetic effects.
Metabolic Improvements: Increases mitochondrial enzymes, fatty-acid oxidation capacity, and skeletal muscle glucose uptake[3][6]; improves insulin sensitivity in animal models.
Therapeutic Potential: Research suggests potential for diabetic neuropathy protection and metabolic syndrome treatment in animal models[7].

Side Effects

Important: Despite promising preclinical results, AICAR remains experimental; no confirmed clinical benefit in humans has been established, and long-term risks are unknown.

AICAR (50 mg Vial)

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