AICAR
Acadesine / AICA Ribonucleotide / Aminoimidazole Carboxamide Ribonucleotide / ZMP precursor
An AMP-activated protein kinase (AMPK) activator that mimics the metabolic effects of exercise. AICAR is phosphorylated intracellularly to ZMP, which allosterically activates AMPK — the master metabolic switch that triggers glucose uptake, fatty acid oxidation, mitochondrial biogenesis, and insulin sensitization. Gained notoriety as an 'exercise in a pill' after a 2008 mouse study in which treated sedentary mice ran 44% farther. Listed on WADA's prohibited substances list since 2009.
Half-life
~2–3 hours
Typical Dose
150–500 mg/day SC (research); varies widely
300/500Route
subcutaneous
Category
metabolic
Evidence Overview
Strength of evidence across clinical, expert, and experimental lanes.
How AICAR is dosed in practice
Usually taken by subcutaneous (SubQ) injection. Typical range: 150–500 mg/day SC (research); varies widely. Half-life: ~2–3 hours. Each card gives the dose, frequency and duration from one evidence lane: Clinical (human trials), Expert (practitioner protocols) or Experimental (early or animal data). These ranges describe what has been studied or used; they are not a prescription.
Work out the units to draw with the reconstitution calculator, how long a vial lasts with the vial duration calculator, and how levels fall between doses with the half-life calculator.
Human use has been IV infusion only. Heart-surgery trials, including a phase 3 trial stopped for futility in 2012 (3,080 patients), found no reduction in death, stroke or heart failure; a leukemia study used much higher 4-hour infusions. No SubQ or exercise-performance trials exist in humans.
- Multicenter trial in heart surgery (1995)
- Phase 3 trial in heart surgery (2012)
- Phase 1/2 study in leukemia (2013)
Research compound with legitimate exercise-mimetic properties but practical limitations. The large doses required (hundreds of milligrams) make it expensive. Some performance medicine practitioners explore it for metabolically compromised patients who cannot exercise. WADA ban underscores its efficacy.
- Sports medicine and exercise physiology research
- WADA prohibited list — rationale for AICAR inclusion
- Metabolic medicine practitioners — AMPK activation protocols
Niche compound in the biohacking community due to high cost and large dose requirements. Users who have tried it report improved endurance and fat oxidation. Subcutaneous injection site reactions are common. Some users combine with other metabolic enhancers but the evidence base is thin for human use.
- Performance enhancement forums — AICAR experience reports
- Endurance sport biohacking community
- WADA anti-doping case reports involving AICAR detection
Unlock Full Evidence Sources
Get complete clinical data, expert protocols, and experimental research for AICAR and 90+ other compounds with Pro.
Upgrade to ProSafety & Contraindications
- Cardiac conditions (AMPK activation affects cardiac metabolism)
- Hypoglycemia risk (enhances glucose uptake independent of insulin)
- Competitive athletes (WADA banned substance)
AICAR: common questions
What is AICAR?
An AMP-activated protein kinase (AMPK) activator that mimics the metabolic effects of exercise. AICAR is phosphorylated intracellularly to ZMP, which allosterically activates AMPK — the master metabolic switch that triggers glucose uptake, fatty acid oxidation, mitochondrial biogenesis, and insulin sensitization. Gained notoriety as an 'exercise in a pill' after a 2008 mouse study in which treated sedentary mice ran 44% farther. Listed on WADA's prohibited substances list since 2009.
How is AICAR dosed?
AICAR is usually taken by subcutaneous (SubQ) injection. Typical range in DoseCraft's library: 150–500 mg/day SC (research); varies widely. Clinical (human trials), intravenously (IV): 0.05–0.1 mg/kg/min IV for 7 hours around heart surgery; higher 4-hour infusions in a leukemia study; Single infusion around surgery; Hours; no multi-week human dosing. Expert (practitioner protocols): 150–500 mg/day SC; Once daily; 4–8 week cycles. Experimental (early or animal data): 150–500 mg/day SC; Once daily, pre-exercise; 4–6 week cycles. These ranges describe what has been studied or used; they are not a prescription.
Is AICAR FDA-approved?
No. AICAR is not approved by the FDA for any use in people.
What is the half-life of AICAR?
DoseCraft's library lists a half-life of ~2–3 hours. Half-life sets how often a compound is dosed and how long it takes to clear: about five half-lives.
Who should not use AICAR?
Listed contraindications: Cardiac conditions (AMPK activation affects cardiac metabolism); Hypoglycemia risk (enhances glucose uptake independent of insulin); Competitive athletes (WADA banned substance).
Information is for educational purposes only. Always consult a licensed healthcare provider before starting any peptide regimen.
Page updated . How we grade evidence: methodology.