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Preclinical

AICAR

Also known as: AICAR, Acadesine

AICAR (Acadesine) is an AMPK-activating compound studied as an exercise-mimetic for endurance and metabolic effects in animals. Note: AICAR is a small-molecule nucleoside (an AMPK activator), not a peptide, but is commonly sold alongside research peptides.

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Mechanism of Action

AICAR is a cell-permeable nucleoside that is phosphorylated intracellularly to ZMP, an analog of AMP. ZMP allosterically activates AMP-activated protein kinase (AMPK), the cell's central energy sensor, without changing actual ATP levels. Activated AMPK promotes glucose uptake via GLUT4 translocation, stimulates fatty-acid oxidation by inhibiting acetyl-CoA carboxylase, and drives PGC-1alpha-mediated mitochondrial biogenesis, collectively mimicking some adaptations of endurance exercise.

Half-life
Short; on the order of minutes to a few hours
Administration Routes
subcutaneous, intravenous
Research Status
Preclinical

Reported Benefits

  • Activates AMPK, the master metabolic energy sensor
  • Increased endurance in sedentary rodent studies
  • Promotes fatty-acid oxidation and glucose uptake
  • Stimulates mitochondrial biogenesis via PGC-1alpha
  • Studied for improving insulin sensitivity

Potential Side Effects

  • Potential elevation of uric acid (purine metabolite)
  • Possible gastrointestinal discomfort
  • Limited human safety data outside cardiac trials
  • Banned by anti-doping agencies as a metabolic modulator

Common Dosing

For research use only: rodent endurance studies used roughly 250-500 mg/kg/day. There is no validated human performance dosing. Not personal medical advice.

The dosing information above is aggregated from research literature and anecdotal community reports for educational purposes only. It is not a recommendation, prescription, or medical advice. Peptides are sold as research chemicals only and are not intended for human use.

Contraindications

  • Gout or hyperuricemia
  • Pregnancy and breastfeeding
  • Use in sanctioned athletic competition (prohibited substance)
  • AMPK and PPARdelta agonists are exercise mimetics

    2008

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  • AICAr, a Widely Used AMPK Activator with Important AMPK-Independent Effects: A Systematic Review

    2021

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  • Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial

    2012

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  • AICAR administration causes an apparent enhancement of muscle and liver insulin action in insulin-resistant high-fat-fed rats

    2002

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In rodent studies AICAR activates AMPK and reproduces some endurance adaptations even without training, which is why it is described as an exercise-mimetic.

Yes. As a metabolic modulator, AICAR is on the World Anti-Doping Agency prohibited list.

PeptideChat is for educational and research purposes only. Nothing on this site constitutes medical advice. Peptides are sold as research chemicals only and are not intended for human use. These statements have not been evaluated by the FDA and are not intended to diagnose, treat, cure, or prevent any disease. PeptideChat is an independent educational resource — not a pharmacy, compounding, or 503A/503B outsourcing facility — and does not sell products or provide medical advice.