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AICAR

Begrenzte Forschung

5-Aminoimidazole-4-carboxamide Ribonucleotide | AMPK Activator

MetabolischLeistung

AICAR is a cell-permeable nucleoside analog that activates AMP-activated protein kinase (AMPK), a key regulator of cellular energy homeostasis.

Molekulare und Forschungsdaten

Molekulargewicht
338.21 Da
Halbwertszeit
~2-3 hours
Primäre Ziele
ampk
Wege (Forschung)
injectable
Lagerung
Lyophilized: -20°C; Reconstituted: 2-8°C for 4 weeks

Overview

AICAR is a cell-permeable nucleoside analog that activates AMP-activated protein kinase (AMPK), a key regulator of cellular energy homeostasis. Originally studied for cardiac ischemia protection, it gained attention as an ‘exercise mimetic’ due to its metabolic effects.

Mechanism of action

Once inside cells, AICAR is phosphorylated to ZMP, which mimics AMP and activates AMPK. This triggers metabolic pathways typically activated during exercise: increased glucose uptake, fatty acid oxidation, and mitochondrial biogenesis.

Key research findings

  • AMPK pathway activation
  • Enhanced fatty acid oxidation
  • Improved glucose uptake
  • Potential endurance enhancement
  • Mitochondrial biogenesis stimulation

Research applications

Metabolic

  • AMPK Activation — Directly activates the master metabolic regulator through ZMP accumulation.
  • Fatty Acid Oxidation — Increases fat burning through AMPK-mediated pathways.
  • Glucose Metabolism — Enhances glucose uptake independent of insulin in some tissues.

Performance

  • Endurance Enhancement — Animal studies showed increased running endurance; human data limited.
  • Mitochondrial Biogenesis — AMPK activation promotes new mitochondria formation over time.

Cardioprotection

  • Ischemia Protection — Original clinical interest; may protect heart tissue during reduced blood flow.

AICAR Häufig gestellte Fragen

Does AICAR actually work as an 'exercise mimetic' in humans?+

Animal studies show AICAR increased running endurance by 44% without training. However, this was mice, not humans. Humans have never been adequately tested for AICAR's endurance effects, so calling it an exercise mimetic is speculative. The compound does activate AMPK and increase fat oxidation, but real-world performance gains in people are unproven.

Is AICAR banned in sports and why?+

Yes, AICAR is WADA prohibited. While it's not anabolic per se, it provides competitive advantage through enhanced metabolic efficiency and endurance. Athletes competing under WADA rules must avoid it entirely due to testing likelihood and strict liability regulations.

What's the risk of hypoglycemia on AICAR if I'm not diabetic?+

AICAR increases glucose uptake independent of insulin in some tissues, creating theoretical hypoglycemia risk especially in non-diabetics with normal insulin sensitivity. Diabetics face more serious risk, which is why AICAR is contraindicated in diabetes. Monitor blood glucose closely, particularly during initial doses.

How does AICAR differ from GW501516 for metabolic enhancement?+

AICAR activates AMPK, the master metabolic regulator, increasing fatty acid oxidation and glucose uptake. GW501516 is a PPARδ agonist with different downstream effects. They're often stacked because they target complementary pathways—AMPK plus PPARδ activation produces synergistic metabolic effects.

References

  1. [1]AMPK and Exercise: Glucose Uptake and Insulin SensitivityReference
  2. [2]AICAR Mouse Endurance StudyReference

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