AICAR
Metabolic Health · AMPK activator / exercise mimetic
Tier D
High-risk evidence profile
Bottom line
Read Off Label grades AICAR as D (3.3/10) based on preclinical evidence, high benefit magnitude, and a unknown-high-risk safety profile.
Its high-risk evidence profile reflects a Safety score of 3/10; reported benefits and harms can differ by indication, dose, route, duration, and population.
WADA coverage: AICAR and the broader AMPK-activator exercise-mimetic class.
Studied, labeled, or reported-use context: No approved performance dose — Research/clinical-research compound; WADA S4 prohibited; not individualized guidance.
Frontier potential — editorial judgment, not evidence
This is a separate axis from the grade above. It asks a different question: if this worked in humans, how much would it matter? It is our judgment, it is not part of the composite score, and it cannot raise a grade. A high number here is a statement about the idea, not about whether it works or whether anyone should take it.
What the ceiling rests on
A direct AMPK activator that increased endurance in sedentary mice — the original "exercise in a pill" result — and AMPK is a well-validated node in the nutrient-sensing pathways that matter for ageing.
Why it may not get there
Poor oral bioavailability means it must be injected in large quantities, which is impractical and expensive. Human trials have been limited and unimpressive, AMPK activation has effects on tumour metabolism that cut both ways, and the mouse endurance result has not translated. WADA-prohibited.
What would change this A human trial with a functional endurance endpoint.
What the evidence says
WADA coverage: AICAR and the broader AMPK-activator exercise-mimetic class. Strong interest comes from the exercise-in-a-pill story, not from proven human longevity benefit. Additional WADA alias coverage: Peroxisome proliferator-activated receptor delta (PPARdelta) agonists and the GW1516/GW501516 chemical entry are covered here as the broader exercise-mimetic class and by the dedicated Cardarine row.
Mechanism
AICAR activates AMPK-linked signaling and became famous as an “exercise mimetic” after preclinical endurance studies; human enhancement evidence is thin.
Studied, labeled, or reported dose & route
No approved performance dose
This records doses and routes described in studies, approved labeling, clinical practice, or documented use. It is not individualized guidance and does not establish safety; context changes with indication, formulation, health history, monitoring, and other medicines.
Citations
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Common questions
- What does the evidence show about AICAR's effects?
- Read Off Label rates the evidence for AICAR as Preclinical and the benefit magnitude as high, producing an overall grade of D (3.3/10). WADA coverage: AICAR and the broader AMPK-activator exercise-mimetic class.
- What safety findings are reported for AICAR?
- AICAR has a unknown-high risk profile in the database. Unknown-High (limited human enhancement data, metabolic/cardiac uncertainty, research-chemical quality risk) Legal status: Research/clinical-research compound; WADA S4 prohibited.
- What does the low Safety score for AICAR represent?
- The Safety score is 3/10. It records the substantial harms described for one or more use contexts; the Benefit score, indication, dose, route, duration, population, and legal status remain separate parts of the evidence profile.
- What doses or routes are reported for AICAR?
- No approved performance dose This is context from studies, approved labeling, clinical practice, or documented use; it is not individualized guidance and does not establish safety.
- How does AICAR work?
- AICAR activates AMPK-linked signaling and became famous as an “exercise mimetic” after preclinical endurance studies; human enhancement evidence is thin.
This is an independent synthesis of published research by a non-clinician. Scores are opinions supported by citations, not prescriptions. See the full disclaimer and methodology for how this score was produced and what it does and doesn't mean.