AICAR
AICAR (acadesine) is an AMPK activator studied clinically for cardioprotection and famous as an 'exercise mimetic'. By switching on AMPK it boosts fatty-acid oxidation and glucose uptake, making it a research-grade metabolic and endurance agent that is banned in sport.
01 Overview
AICAR is metabolised to ZMP, a mimic of AMP that activates AMP-activated protein kinase (AMPK), the cell's energy sensor. Activated AMPK increases glucose uptake, fatty-acid oxidation and mitochondrial biogenesis, which is why AICAR raised endurance in sedentary mice and became a byword for exercise-in-a-pill.
It has genuine clinical study as a cardioprotective agent (acadesine) but requires large intravenous doses, and its use as a metabolic/endurance aid is off-label and prohibited in competition. Practical oral efficacy in humans for fat loss is poorly established.
02 Mechanism
Converted to ZMP intracellularly, mimicking AMP to activate AMPK, which upregulates glucose uptake, fatty-acid oxidation and mitochondrial biogenesis while suppressing anabolic energy use.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Cardioprotection (trials) | 60–100 mg | IV | Weight-based IV infusion in cardiac surgery studies (mg/kg/min protocols) |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Increased fatty-acid oxidationAMPK activation shifts metabolism toward fat burning. | Preclinical | ||
| Improved endurance / glucose uptakeRaised endurance and insulin-independent glucose uptake in animal models. | Preclinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Poor oral bioavailability / impracticalityLarge doses needed; oral fat-loss use is largely ineffective and costly. | Mild | Inherent | Clinical | |
| Elevated uric acidPurine-analogue metabolism can raise uric acid. | Moderate | Uncommon | Clinical |