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AICAR

AMPK Activator (Nucleoside Analog)Research use only

Half-life

≈0.5–2 hours (route-dependent); intracellular ZMP/PD effects persist several hours

Delivery

In vitro (media supplementation) or in vivo via IP/oral routes in animal models; IV used in cardioprotection trials—route/formulation per study design.

Dosage

Research Use Only

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Description

AICAR (5-aminoimidazole-4-carboxamide ribonucleoside) is a cell-permeable adenosine analog converted intracellularly to ZMP, an AMP mimetic used to activate AMPK and interrogate cellular energy-sensing pathways.

Usage

Metabolic and exercise-mimetic research: glucose homeostasis, lipid metabolism, insulin sensitivity, cardioprotection, and skeletal-muscle endurance models.

Mechanism of Action

Phosphorylated to ZMP, which allosterically activates AMPK and inhibits AMP-degrading enzymes, elevating AMPK signaling (e.g., ACC phosphorylation, fatty-acid oxidation, GLUT4 translocation, PGC-1α programs).

Benefits(5)

  • Increases skeletal-muscle glucose uptake (insulin-independent)
  • Enhances fatty-acid oxidation and reduces lipogenesis
  • Activates mitochondrial biogenesis–associated gene programs
  • Useful as an exercise-mimetic/comparator in preclinical models
  • Enables cardiometabolic studies (e.g., ischemia–reperfusion)

Side Effects(5)

  • Potential hypoglycemia with excessive glucose disposal
  • Gastrointestinal discomfort or nausea
  • Headache or fatigue
  • Altered uric-acid/purine metabolism (hyperuricemia risk)
  • Elevations in liver enzymes or renal load at high dose/duration