Description
AICAR (5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside, also called acadesine) is a classical AMPK activator and one of the most established compounds for studies on the cellular energy sensing axis. Structurally, AICAR is not a peptide but a nucleotide analog phosphorylated to ZMP (AICAR monophosphate) after cellular uptake, an AMP mimetic.
The research mechanism lies in the activation of AMPK (AMP-activated protein kinase). AMPK is the central cellular energy sensor. It is activated at low ATP and high AMP levels and switches metabolic pathways: increased fatty acid oxidation, enhanced glucose uptake, reduced anabolic synthesis, activation of mitochondrial biogenesis. AICAR bypasses energetic triggering and activates AMPK directly via the ZMP signal.
In preclinical studies, AICAR has been extensively characterized. It is one of the central tools in research on metabolic syndrome, diabetes, mitochondrial function and exercise mimetics. In fact, AICAR was originally discussed in scientific literature as “exercise in a pill” since many AMPK-mediated adaptations resemble those of physical activity.
A particularity: AICAR has a substantial research history reaching back into the 1980s. The data is comprehensively documented; the compound is mechanistically clearly defined.
AICAR is available in 50mg vials as 10-vial packs.
This information is for research and educational purposes only. No medical recommendations.
Risks & Safety
AICAR is, as an AMPK activator, one of the longest-researched metabolic compounds and mechanistically clearly defined, but it intervenes deeply in cellular energy regulation.
Observed in research and user reports:
- Metabolic intervention: direct AMPK activation shifts several metabolic pathways simultaneously. Preclinical studies document altered glucose and fatty acid utilization as a result.
- Circulation: isolated reports of circulatory effects and transient fatigue shortly after application.
- Injection site: redness or pressure at the injection site is among the more common observations.
- No long-term data: despite a long research history, no robust human studies on longer-term non-clinical use exist. The profile rests on animal models and cell studies.
This classification does not replace medical advice. Risk and responsibility for any actual use lie entirely with the buyer.
Studies
- 5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells? - European Journal of Biochemistry 1995: Classic characterization: in hepatocytes AICAR is phosphorylated to ZMP, which mimics both activating effects of AMP on AMPK without altering cellular ATP, ADP or AMP levels. Fatty acid and sterol synthesis almost completely ceased.
- AICA riboside increases AMP-activated protein kinase, fatty acid oxidation, and glucose uptake in rat muscle - American Journal of Physiology - Endocrinology and Metabolism 1997: In perfused rat hindlimbs, AICAR activated AMPK in skeletal muscle, lowered malonyl-CoA and increased fatty acid oxidation 2.8-fold as well as glucose uptake.
- AMPK: a nutrient and energy sensor that maintains energy homeostasis - Nature Reviews Molecular Cell Biology 2012: Review of AMPK as a cellular energy sensor: when energy status falls it switches on catabolic pathways and switches off biosynthetic pathways. It also regulates energy balance at the whole-body level.
- Exercise mimetics targeting AMPK - Cell 2008: AICAR in the exercise mimetic context.
