AICAR

Third-Party Tested

Independent lab verified

Batch-Specific CoA

Publicly accessible

YPB.250

Reference number

50mg

Lyophilized vial

Origin

AICAR (5-aminoimidazole-4-carboxamide ribonucleoside, also known as acadesine) was first synthesized in the 1950s and was initially investigated as a purine metabolism intermediate. Its role as an AMPK activator was established by Corton et al. in 1995, and it gained prominence when Narkar et al. demonstrated exercise-mimetic effects in sedentary mice in 2008.

Research Lineage

The landmark 2008 study by Narkar, Evans, and colleagues at the Salk Institute published in Cell demonstrated that AICAR could increase running endurance by 44% in sedentary mice without exercise training. This generated significant interest in AMPK as a pharmacological target. AICAR is now the most widely used pharmacological AMPK activator in metabolic research.

Mechanism of Action

AICAR is phosphorylated intracellularly to ZMP (AICAR monophosphate), which mimics AMP and activates AMPK (AMP-activated protein kinase) allosterically. AMPK activation triggers catabolic pathways including glucose uptake, fatty acid oxidation, and mitochondrial biogenesis while inhibiting anabolic pathways. It is a key energy-sensing enzyme that shifts cellular metabolism toward ATP production.

Structural Notes

Nucleoside analog. Molecular formula: C9H14N4O5. Molecular weight: 258.23 Da. Cell-permeable prodrug — converted to active ZMP by adenosine kinase.