AICARAnti-AgingSafety Rating 6/10

Primary research areaEndurance enhancement

Research-literature reference data, NOT patient instructions. Not for human use. Consult a licensed clinician for any human application.

Research dose rangeResearch protocols: 500 mg – 2 g SC or IV daily. Animal studies use 500 mg/kg. Human dosing not established.
AdministrationInjection
Safety6/10 · Not FDA-approved
NCAA D1Banned

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Overview

About AICAR

Mechanism of action

AMP-kinase (AMPK) activator; mimics energy-depletion state; stimulates mitochondrial biogenesis, fatty acid oxidation, and glucose uptake; upregulates PGC-1α; exercise mimetic.

Safety profile

Generally well-tolerated in research. Potential: hypoglycemia, uric acid changes, GI discomfort. Long-term human data limited. · Used in cardiac surgery trials; well-tolerated at clinical doses; hyperuricemia at high doses; WADA banned

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Related pages

More on AICAR

Research

Studies & key findings

  • Narkar et al. (Cell, 2008) demonstrated that 4 weeks of AICAR in sedentary mice enhanced treadmill running endurance by 44% and upregulated oxidative metabolism genes in skeletal muscle without any exercise — establishing AICAR as the prototypical 'exercise in a pill' and leading to its addition to WADA's prohibited list.
  • AICAR activates AMPK by mimicking AMP, triggering downstream phosphorylation of ACC and PGC-1α activation, which drives mitochondrial biogenesis, fatty acid oxidation, and slow-twitch (type I) fiber specification; however, systematic review evidence confirms that numerous AICAR effects are AMPK-independent, including some NF-κB suppression in human macrophages.

7 peer-reviewed sources cited — clinical, preclinical, and regulatory.

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