AICAR

Technical data

INN name

Acadesine

Development code

GP-1-110

CAS

2627-69-2

Molecular formula

C9H14N4O5

Molecular weight

258.23 g/mol

Identity and composition

AICAR (acadesine; also known as AICA riboside) is an adenosine nucleoside analog used as a research compound to study AMPK activation and cellular energy metabolism. It is not a peptide, but a small molecule with a long track record in the preclinical literature.

Reference chemical identity data:

• CAS: 2627-69-2
• Molecular formula: C9H14N4O5
• Molecular weight: 258.23 g/mol
• PubChem CID: 17513
• Synonyms: Acadesine, AICA riboside, 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside, GP-1-110

Reference presentation: 50 mg and 10 mg × 100 tablets.

Product for research use.

Mechanism of action

AICAR enters cells through adenosine transporters and is phosphorylated by adenosine kinase to its monophosphate form, ZMP (AICA ribotide, an AMP analog). ZMP binds to the gamma subunit of the AMPK, allosterically activates it and promotes LKB1-mediated phosphorylation at Thr172, mimicking the effect of AMP (PMID 34064363).

It is important to qualify that, according to the systematic review, ZMP is notably less potent than AMP in the activation of AMPK and tends to accumulate at high cellular concentrations. For this reason, many effects historically attributed to AMPK are in reality AMPK-independent (for example, in nucleotide synthesis and the cell cycle) (PMID 34064363).

In in vitro models, AMPK activation has been associated with fatty-acid oxidation and with mitochondrial biogenesis and dynamics. These are observations in experimental systems, not effects demonstrated in humans.

Pharmacokinetics

The systematic review notes a very poor oral bioavailability in clinical trials, which is why the preferred route in the studies has been intravenous; this makes it poorly suited for chronic oral administration (PMID 34064363).

No specific numerical half-life (t1/2) value was confirmed in the open sources, so this parameter is described qualitatively and no specific figure is reported.

Scientific evidence

AICAR is a long-standing research compound. In the 1990s, acadesine (its clinical name) was evaluated in multicenter Phase III trials as a cardioprotective agent to reduce ischemia-reperfusion injury in coronary bypass surgery (CABG). The first multicenter international study, with intravenous administration, showed no significant difference in the primary endpoint in the overall population, although reductions were observed in high-risk subgroups; overall, the Phase III trials did not confirm a consistent benefit and development was discontinued (PMID 7475138).

Subsequently, it has been investigated in vitro and in preclinical models in oncology (lymphoblastic leukemia, prostate, breast), metabolism, autophagy, and mitochondrial biogenesis. The preliminary evidence in these fields is mostly preclinical or in vitro, and there is no regulator-approved indication. The results must be interpreted as exploratory and limited.

Research applications

Ideal for (research contexts):

• In vitro and preclinical studies on AMPK activation and cellular energy signaling.
• Research on metabolism, fatty acid oxidation and mitochondrial biogenesis/dynamics in experimental models.
• Mechanistic work to distinguish AMPK-dependent effects from AMPK-independent effects.

Not applicable for:

• Any therapeutic or diagnostic use: it has no indication approved by regulators.
• Chronic oral administration as a strategy, given its poor oral bioavailability.
• clinical use of any kind.

Product for research use.

Research protocols

In the coronary artery bypass graft (CABG) surgery clinical trial, acadesine was administered by intravenous infusion at a rate of 0.1 mg/kg/min for approximately 7 hours (PMID 7475138). This scheme corresponds to a historical intravenous clinical context and does not constitute a dosing recommendation.

For preclinical and in vitro use, concentrations and schedules depend on the specific experimental model; the consulted literature does not provide a validated generic range for these contexts, so no additional figures are reported. Any protocol must be defined according to the experimental design and the corresponding literature.

Reconstitution

AICAR in tablet presentation does not require reconstitution. When working with material that must be dissolved in the laboratory, standard practice is to use a vehicle compatible with the experimental design (for example, bacteriostatic water -water with approximately 0.9% benzyl alcohol- for preparations intended for standard sterile handling).

As a general laboratory guideline: add the diluent slowly down the wall of the vial, without vigorous shaking, and let the material dissolve by gentle diffusion. Label with date and concentration. These steps are standard handling technique and do not imply suitability for use in humans.

Stability and storage

As a general laboratory handling guideline:

• Solid material (tablets / powder): store in its original container, protected from humidity, light and heat; cold storage prolongs stability.
• Reconstituted material / in solution: keep refrigerated and use within a short window; for prolonged storage, freezing is generally preferred, avoiding repeated freeze-thaw cycles.

These ranges are standard laboratory handling practices and must be adjusted to the specific conditions of the reagent and the protocol.

Safety profile

The documented safety profile comes mainly from the context of intravenous clinical research. In the multicenter CABG trial no adverse events were attributed to treatment with acadesine, and early mortality was numerically lower in the treated group (PMID 7475138). Secondary sources indicate that high intravenous doses were tolerated with mild and transient side effects.

Important limitations that should be kept in mind:

• The safety for chronic oral use is not established.
• Oral bioavailability is poor.
• There is no indication approved by regulators.

As this is a product for research use, it must not be used in humans, nor should the above information be interpreted as a validated clinical safety profile.

Comparative context

As an AMPK activator, the active metabolite of AICAR (ZMP) is notably less potent than the physiological AMP, on the order of 40 to 50 times less potent according to the systematic review (PMID 34064363).

Unlike more selective direct AMPK activators (for example, A-769662-type compounds) or metformin (which acts through different mechanisms), AICAR presents marked AMPK-independent effects due to the accumulation of ZMP. This characteristic complicates the interpretation of its effects as purely AMPK-mediated and is one reason why it is used with caution as a mechanistic tool in research.

History and development

AICAR is a long-established research compound, not a peptide. Under the clinical name of acadesine, in the 1990s it was evaluated in multicenter Phase III trials as a cardioprotective agent to reduce ischemia-reperfusion injury in coronary bypass surgery (CABG). The first international multicenter study included 821 patients with intravenous administration (PMID 7475138).

As no consistent benefit on the primary endpoint was confirmed in the Phase III trials, clinical development was discontinued. Since then, the compound has maintained relevance in in vitro and preclinical research in areas such as oncology, metabolism, autophagy, and mitochondrial biogenesis, mainly as a tool to study the AMPK pathway.

FAQ

Customer reviews

Average rating: 5.0 out of 5, based on 3 customer ratings.

Certificate of analysis per batch

AICAR lots with certificate of analysis published in the COA catalog:

• Lot EXO010626088A — 50 mg, issued 2026-05-25
• Lot EXO010626088B — 100 mg, issued 2026-05-23

Scientific references (5)

Peer-reviewed literature on AICAR, with its PubMed identifier when available:

• 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.

Otras presentaciones de AICAR

• AICAR Oral

Other related research peptides

• AOD-9604
• Cagrilintide
• Cagrilintide + Semaglutide
• Combo Retatrutide 5 mg + Agua Bac 30 mL de Regalo
• HGH Frag 176-191
• Liraglutide
• Mazdutide
• MOTS-c
• NAD+ + MOTS-c + 5-Amino-1MQ
• Retatrutide