AICAR: Scientific Profile
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Acadesine (AICAR, AICA ribonucleoside; CAS 2627-69-2) is a nucleoside analog and allosteric activator of AMPK. It is phosphorylated intracellularly to ZMP, an AMP mimetic, activating AMPK without altering the AMP/ATP ratio. Reagent for in vitro and preclinical metabolic research.
Acadesine (AICAR; also AICA ribonucleoside or AICA riboside; CAS 2627-69-2; molecular formula C9H14N4O5; molecular weight 258.23 g/mol) is a nucleoside analog, an intermediate of purine biosynthesis. Within the cell it is phosphorylated by adenosine kinase to ZMP, an AMP mimetic that binds to the γ (Bateman) domain of AMPK and allosterically activates it without altering the AMP/ATP ratio; AMPK acts as a master sensor of the cell's energy state. In in vitro and preclinical research, this activation promotes GLUT4 translocation and insulin-independent glucose uptake, stimulates fatty acid oxidation, induces mitochondrial biogenesis via PGC-1α with conversion of fibers toward the type I oxidative phenotype, and inhibits NF-κB, which is associated with inflammatory modulation and ischemic protection. Reconstitution: dissolve the lyophilizate in bacteriostatic water (2-3 mL per vial) as a laboratory stock solution. Storage: keep the lyophilizate at -20 °C and, once reconstituted, maintain at 2-8 °C for up to 14 days. Reagent for research (RUO).
Mechanism of action
AICAR functions as a precursor of ZMP, which mimics the effects of AMP by binding to the allosteric site of the gamma subunit of AMPK. This binding promotes the phosphorylation of AMPK by the hepatic kinase LKB1. Once activated, AMPK inhibits ATP-consuming anabolic processes (such as fatty acid synthesis through the inactivation of ACC) and stimulates ATP-producing catabolic processes, such as beta-oxidation and myocellular glucose uptake.
Mechanism summary
It is phosphorylated intracellularly to ZMP, an AMP mimetic that allosterically activates AMPK (γ/Bateman domain) without altering the AMP/ATP ratio. This induces GLUT4 translocation and insulin-independent glucose uptake, fatty acid oxidation, mitochondrial biogenesis via PGC-1α and inhibition of NF-κB.
Clinical Studies (5)
- Cardiovascular and renal effects of 5-aminoimidazole-4-carboxyribonucleoside (AICAR) in the deoxycorticosterone acetate (DOCA)-salt rat model of hypertension (Dennis MR et al. · Life Sciences · 2025) PMID 40947048.
- Administration of AICAR, an AMPK Activator, Prevents and Reverses Diabetic Polyneuropathy (DPN) by Regulating Mitophagy (Chandrasekaran K et al. · International journal of molecular sciences · 2024) PMID 39795939.
- AICAr, a Widely Used AMPK Activator with Important AMPK-Independent Effects: A Systematic Review (Višnjić D et al. · Cells · 2021) PMID 34064363.
- 5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells? (Corton, et al. · European Journal of Biochemistry · 1995) PMID 7744080.
- AMPK and PPARdelta agonists are exercise mimetics (Narkar, et al. · Cell · 2008) PMID 18674809.
Warnings
AICAR is a compound exclusively for research use (RUO); the following warnings and handling considerations apply to its use in the laboratory:
- Product exclusively for use in research laboratories
- Requires handling under sterile conditions
- Its use in living subjects has not been approved by health authorities
- May interfere with assays that measure lactate and purines
- Study subjects with hyperuricemia or congenital gout
- Models with established renal insufficiency
- Presence of hepatic pathologies that compromise gluconeogenesis
Technical data
- CAS
- 2627-69-2
- Molecular formula
- C9H14N4O5
- Molecular weight
- 258.23 Da
- Compound type
- metabolic
- Storage
- -20 °C liofilizado; 2-8 °C reconstituido
- Shelf life (lyophilized)
- 24 months
- Shelf life (reconstituted)
- 7-14 days refrigerated
- Light-sensitive
- No
Available for research
AICAR is available as a research reagent (RUO):
Frequently asked questions about AICAR
What is AICAR?
Acadesine (AICAR, AICA ribonucleoside; CAS 2627-69-2) is a nucleoside analog and allosteric activator of AMPK. It is phosphorylated intracellularly to ZMP, an AMP mimetic, activating AMPK without altering the AMP/ATP ratio.
What is the mechanism of action of AICAR?
It is phosphorylated intracellularly to ZMP, an AMP mimetic that allosterically activates AMPK (γ/Bateman domain) without altering the AMP/ATP ratio. This induces GLUT4 translocation and insulin-independent glucose uptake, fatty acid oxidation, mitochondrial biogenesis via PGC-1α and inhibition of NF-κB.
What is AICAR researched for?
In preclinical research, AICAR is studied mainly in: Research on the activation of mitochondrial biogenesis; Study of fatty acid oxidation in obesity models; Modulation of insulin-independent glucose uptake. Material exclusively for scientific research.
What are the chemical properties of AICAR?
Molecular formula C9H14N4O5; molecular weight 258.23 Da; CAS number 2627-69-2.
How is AICAR stored?
Condiciones de conservación: -20 °C liofilizado; 2-8 °C reconstituido; estabilidad liofilizado: 24 meses; una vez reconstituido: 7-14 días refrigerado.
What routes of administration are studied for AICAR?
In research models the following are described: Subcutaneous, Intraperitoneal, Intravenous. Use is exclusively for scientific research.