/DISCLAIMER · RESEARCH_COMPOUND

This page is reference information only. Most compounds described here are research chemicals, not FDA-approved medications. MyTRT does not sell, recommend, or endorse the use of these substances. Always consult a qualified physician.

/AICAR_AMPK_ACTIVATOR
Nucleotide Analog / Metabolic Modulator

AICAR

AMPK Activator (Nucleoside Analog)

/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.

/WHAT_IT_IS

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).

Reported Benefits

  • +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)

Reported Side Effects

  • 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

/STACKED_WITH

Metformin (complementary AMPK activation via complex I inhibition)Resveratrol or NAD+ boosters (SIRT1/PGC-1α axis exploration)Exercise/electrical-stimulation paradigms (exercise-mimetic designs)CPT1/FAO modulators for pathway mapping

/RESEARCH_NOTES

AICAR has AMPK-independent effects via purine/adenosine pathways—use genetic or pharmacologic controls (e.g., AMPKα loss-of-function). Monitor glucose, lactate, uric acid, and liver/renal panels in vivo.

/REFERENCE

https://pubmed.ncbi.nlm.nih.gov/7777520/

/RELATED

/TRACK_THIS

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Last reviewed: 2026-06-04 · Reference only. Not medical advice. Consult a qualified physician.