AICAR
Aliases: Acadesine · 5-Aminoimidazole-4-carboxamide ribonucleoside · AICA ribonucleoside · ZWAC
Last verified: 2026-09-24
The short version
AICAR is one of the few gray-market substances with a serious academic pedigree — and an ending worth listening to. As acadesine, it went through a real clinical development path and lost. The gray-market narrative sells it as 'exercise in a pill' based on a single 2008 mouse study. AMPK activation is indeed a central metabolic switch, but chronic, systemic activation of every cellular energy sensor is not the same as a 45-minute run — and nobody has measured that in humans. A serious risk the community ignores: AMPK is also an oncogenesis-related signaling node, and WADA treats it as classic doping.
Identity & type
- Molecular type
- small molecule
- Molecular weight
- 258 Da
- Origin
- A nucleoside (ribose analog), an intermediate in de novo purine synthesis; pharmaceutically developed as acadesine.
Mechanism of action
A nucleoside that enters the pentose phosphate pathway → forms ZMP (monophosphate), which activates AMPK (5'-AMP-activated protein kinase), the master cellular energy sensor; the result is increased beta-oxidation, glucose uptake and inhibited lipogenesis — hence the 'exercise in a pill' label.
not confirmed in humans
Dosing & routes
Official / clinical context
No approved documents exist; development was stopped by a negative trial. Everything sold under the name AICAR is a research chemical.
Regulator-approved labeling and published study designs — never a recommendation.
Community-reported practice
Most common regimen: 500–1000 mg/day orally or subcutaneously, 4–8 weeks, often paired with GW501516 in an 'endurance' stack. Reports include mild endurance and thermogenesis increases; none of it has been objectively measured.
Unverified self-reports. Not medical advice. Not endorsement.
Protocol — official vs community
Official / label
No official protocol exists — this compound has no approved product.
Community (anecdotal)
Doping-literature regimens cite 500–1,000 mg/day, orally or subcutaneously — unvalidated, sourced from grey-market 'endurance stack' practice rather than any human trial.
- Cycle:
- 4–8 weeks in those same unverified accounts.
- Break:
- Undefined.
AICAR circulates almost exclusively in endurance-doping niches, often stacked with GW501516, and is WADA-prohibited at all times (S4). The one rigorous human program (as acadesine) was negative, so every dose figure above is an unmeasured self-report, not a protocol.
Human evidence
Human data exist — but as acadesine in a cardiac indication, where the large randomized trial was negative. There is no evidence for effects on endurance, fat or muscle in humans.
Preclinical evidence
Strong: in mice AICAR increases endurance and shifts the muscle phenotype via AMPK/PPAR-delta; metabolic effects are well described in cell and animal models.
Known risks
- Theoretical risk of chronic AMPK activation (metabolic and tumor signaling node)theoretical
- Gray-market product quality is unverified; nucleosides are hygroscopic and unstablecharacterized
Teal: characterized in clinical/labeling contexts. Amber: theoretical or reported outside controlled settings.
Unknowns & evidence gaps
- Effect on endurance or body composition in humans
- Long-term safety of chronic use in healthy people
Frequently asked questions
References
- Narkar VA et al. AMPK and PPARdelta agonists are exercise mimetics. Cell, 2008
- Acadesine (hypothesis) trials in coronary revascularization — negative pivotal result
- WADA Prohibited List — S4 Metabolic Modulators