AICAR 5mg

£25.00

(NOT FOR HUMAN CONSUMPTION RESEARCH USE ONLY) 

AICAR (5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside) is an adenosine analogue used as a research tool to activate the enzyme AMP-activated protein kinase (AMPK), a key regulator of cellular energy, and is not a peptide. It is primarily studied for its potential in treating metabolic disorders and improving endurance. 

 

 

 
 
 

 

 

Mechanism of Action

AICAR is naturally produced in the body as an intermediate in purine synthesis. When synthetically administered, it penetrates cell membranes and is converted into ZMP (AICAR monophosphate), which mimics the function of AMP to activate AMPK. 

Once activated, AMPK acts as a metabolic master switch, initiating changes that: 

  • Increase Energy Availability: Promotes fat oxidation (burning fat for energy) and glucose uptake in muscle cells.
  • Boost Mitochondria: Encourages cells to create more mitochondria, the powerhouses of the cell.
  • Regulate Metabolism: Inhibits processes that use up energy, such as protein and cholesterol synthesis. 

These metabolic effects are what led to its nickname "exercise-in-a-pill" in early research, as they largely mimic the cellular changes induced by physical exercise. 

 

Health Benefits and Research

AICAR is being evaluated in preclinical research and human clinical trials for several therapeutic applications: 

  • Diabetes and Insulin Resistance: Studies have shown that AICAR can improve glucose homeostasis and insulin sensitivity by increasing the metabolic activity of tissues.
  • Cardiovascular Health: Research suggests it may support endothelial function, reduce oxidative stress, and regulate vascular tone, offering potential for studying conditions like atherosclerosis and hypertension.
  • Neurological Protection: Animal studies indicate it can attenuate inflammation in brain cells and potentially offer transient benefits to brain function after injury.
  • Muscular Dystrophy: In mice models of Duchenne muscular dystrophy, chronic AICAR treatment helped ameliorate the dystrophic muscle phenotype and reduce muscle atrophy. 

 

Safety and Regulatory Status

Despite its potential, AICAR's status is highly regulated: 

  • FDA Status: AICAR is an investigational drug and is not FDA-approved for human consumption or medical use outside of clinical trials in the U.S..
  • WADA Prohibited: It has been on the World Anti-Doping Agency (WADA) Prohibited List since 2009 because of its performance-enhancing potential and is strictly tested for in athletes.
  • Safety: While safe in physiological concentrations, high, sustained doses are expected to be toxic. Adverse effects in clinical studies at very high doses included transient anemia and mild hyperuricemia. Long-term safety data in humans is not extensive.