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Peptide Profile

AICAR

Acadesine · AICA ribonucleotide · 5-aminoimidazole-4-carboxamide ribonucleotide

AICAR (5-aminoimidazole-4-carboxamide ribonucleotide; acadesine) is a non-peptide, cell-permeable nucleoside analog and prodrug that is phosphorylated intracellularly to its monophosphate form (ZMP), which mimics AMP to activate…

MetabolicInvestigationalResearch Only
Routes
subcutaneous, intravenous

Educational research information — not medical advice. Review primary sources and consult a qualified professional before any decision.

Educational research tools — not medical advice.

Overview

What AICAR is

About AICAR

Converted intracellularly to ZMP, a potent AMPK activator. AMPK activation increases fatty acid oxidation, glucose uptake, and mitochondrial biogenesis — the same metabolic pathways activated by sustained aerobic exercise.

AICAR (5-aminoimidazole-4-carboxamide ribonucleotide; acadesine) is a non-peptide, cell-permeable nucleoside analog and prodrug that is phosphorylated intracellularly to its monophosphate form (ZMP), which mimics AMP to activate AMP-activated protein kinase (AMPK) — the primary cellular energy sensor — producing metabolic effects that partially phenocopy those of exercise and caloric restriction. AMPK activation by AICAR upregulates GLUT4 expression and glucose uptake, stimulates fatty acid oxidation, increases mitochondrial biogenesis via PGC-1alpha, and suppresses hepatic gluconeogenesis; a landmark 2008 preclinical study demonstrated that AICAR administration in sedentary mice increased running endurance and activated exercise-related gene expression programs without physical training, generating significant research interest in its potential as an exercise mimetic. The only published human clinical trial involved intravenous AICAR administration in patients with type 2 diabetes, where it reduced hepatic glucose output and inhibited whole-body lipolysis via AMPK, validating the pathway pharmacology in humans; the exercise-mimetic effects observed in rodents have not been replicated or evaluated in any human study, and no oral or injectable form has been assessed for human performance use in published research. AICAR is not a peptide and has no FDA approval; it is prohibited in sport by WADA, available only as a research chemical, and all performance-related interest derives from preclinical rodent data that has not been translated to human investigation; the IV metabolic effects in diabetic patients should not be extrapolated to an athletic or performance context.

AICAR Benefits & Research Areas

endurancefat oxidationmitochondrial biogenesisAMPK activation
The Research

What the evidence says about AICAR

Research Evidence

Clinical

based on 12 studies · 1 RCT · most recent 2026

Regulatory Status

Availability Status
Research Only
FDA Status
Investigational

Regulatory status reflects publicly available information and may change. This is not legal or medical advice.

Research Sources

12 sources cited · 12 moderate

1 RCT · 10 Cohorts · 1 Review

  • Targeting AMPK Networks for Male Reproductive Health: Mechanisms and Emerging Therapies.

    Cells · 2026

    # Summary Research found that AMPK (AMP-activated protein kinase) functions as a key regulator connecting metabolic health to male reproductive processes, including sperm production and testosterone synthesis, with dysfunction linked to reduced sperm quality and fertility issues. This study demonstrated that pharmacological agents targeting AMPK signaling pathways, including AICAR among other approaches, show promise as potential therapeutic strategies for improving male reproductive outcomes in the context of metabolic dysfunction.

    ReviewModeratePMID 42121908
  • Thapsigargin-induced autophagic flux impairment and inflammation are potentiated by CLN3 deficiency and alleviated by 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) in human ARPE-19 cells.

    Biochem Biophys Res Commun · 2026

    CohortModeratePMID 42308764
  • The AMPK-PGC-1α-SIRT3 axis mediates mitochondrial metabolic dysfunction and neuronal senescence induced by Al(mal)(3) exposure in HT22 hippocampal neuronal cells.

    Free Radic Biol Med · 2026

    CohortModeratePMID 42263892
Show 9 more sources
  • Berberine Regulates Hepatic Fatty Acid Metabolism via AMPK/SIRT1/PGC-1α Pathway.

    Chin J Integr Med · 2026

    # Summary Research found that berberine regulates hepatic fatty acid metabolism and reduces liver lipid accumulation through activation of the AMPK/SIRT1/PGC-1α signaling pathway. This study demonstrated that berberine's effects involve modulating the expression of proteins involved in fatty acid transport, synthesis, and breakdown, with results suggesting potential therapeutic relevance for non-alcoholic fatty liver disease concurrent with type 2 diabetes.

    CohortModeratePMID 42126802
  • Pharmacological inhibition of TRPM4 channel stabilizes atherosclerotic plaque via inhibiting AMPK-Beclin1-mediated autophagy.

    Eur J Pharmacol · 2026

    # Summary Research found that AICAR, an AMPK agonist, reversed the protective effects of TRPM4 inhibition against excessive autophagy and apoptosis in endothelial cells exposed to oxidized low-density lipoprotein. This study demonstrated that AICAR's activation of the AMPK signaling pathway could counteract the beneficial cellular responses achieved through TRPM4 channel inhibition in the atherosclerotic disease model.

    CohortModeratePMID 42203062
  • MiR-27b-3p suppresses proliferation and testosterone synthesis in goat Leydig cells by activating the AMPK pathway through PPARG targeting.

    Anim Reprod Sci · 2026

    # Summary Research found that miR-27b-3p suppresses Leydig cell proliferation and testosterone synthesis by targeting PPARG, which in turn regulates AMPK signaling. This study demonstrated that activating AMPK through this regulatory pathway can partially restore cellular functions impaired by PPARG suppression, revealing a molecular mechanism relevant to testicular development and reproductive function in male goats.

    CohortModeratePMID 42134159
  • Protective effects of adiponectin receptor agonists against equine lamellar endoplasmic reticulum stress.

    Equine Vet J · 2026

    # Summary Research found that adiponectin receptor agonists, including AICAR, reduced endoplasmic reticulum stress markers in equine lamellar cells exposed to chemical stressors. This study demonstrated that these compounds decreased expression of stress-response proteins and inflammatory markers, suggesting a potential protective mechanism relevant to laminitis pathophysiology.

    CohortModeratePMID 42161434
  • Spatially resolved in vivo ratiometric imaging of mitochondrial quality control using co-registered confocal-OCT.

    Biomed Opt Express · 2026

    CohortModeratePMID 42311307
  • Thapsigargin-induced autophagic flux impairment and inflammation are potentiated by CLN3 deficiency and alleviated by 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) in human ARPE-19 cells.

    Biochem Biophys Res Commun · 2026

    CohortModeratePMID 42308764
  • The AMPK-PGC-1α-SIRT3 axis mediates mitochondrial metabolic dysfunction and neuronal senescence induced by Al(mal)(3) exposure in HT22 hippocampal neuronal cells.

    Free Radic Biol Med · 2026

    CohortModeratePMID 42263892
  • Neuroprotective effects of Platycladus orientalis ethyl acetate fraction on retinal Müller cells: modulation of AKT1/mTOR and Raf-1/MEK1/2 pathways via AMPK activation.

    Front Mol Biosci · 2026

    CohortModeratePMID 42256312
  • Intravenous AICAR administration reduces hepatic glucose output and inhibits whole body lipolysis in type 2 diabetic patients

    Diabetologia · 2008

    Research in a crossover clinical trial found that intravenous AICAR administration activated the AMPK pathway, reduced hepatic glucose output, and decreased circulating free fatty acids in male patients with type 2 diabetes, demonstrating in vivo AMPK activation as a metabolic regulatory mechanism.

    RCTn=10ModeratePMID 18709353

AICAR Side Effects & Safety Considerations

Research-use compound with limited human data. Evidence strength varies — see the Evidence section.

No established clinical contraindications. This is an investigational compound with limited human data and has not been evaluated by the FDA for safety in this context. Consult a qualified clinician.

Consult a qualified healthcare professional before making any health decisions. This information is educational only and does not constitute medical advice.

Certificates of Analysis

1 COA on record for AICAR
  • Vendor-publishedRUO

    AICAR · Lot AI002 · May 6, 2026

PeptideBase reports these lab-published figures and does not itself test, endorse, or certify any product. Verified results come from an independent third-party lab database lookup. Vendor-published results are reported by the vendor itself and have not been independently verified by PeptideBase or a third-party lab.

PeptideBase provides educational research tools and provider discovery. It does not provide medical advice, diagnosis, treatment, prescribing guidance, or dosing instructions. Consult a qualified healthcare professional before making health decisions.

Frequently Asked Questions — AICAR

AICAR (5-aminoimidazole-4-carboxamide ribonucleotide; acadesine) is a non-peptide, cell-permeable nucleoside analog and prodrug that is phosphorylated intracellularly to its monophosphate form (ZMP), which mimics AMP to activate AMP-activated protein kinase (AMPK) — the primary cellular energy sensor — producing metabolic effects that partially phenocopy those of exercise and caloric restriction. AMPK activation by AICAR upregulates GLUT4 expression and glucose uptake, stimulates fatty acid oxidation, increases mitochondrial biogenesis via PGC-1alpha, and suppresses hepatic gluconeogenesis; a landmark 2008 preclinical study demonstrated that AICAR administration in sedentary mice increased running endurance and activated exercise-related gene expression programs without physical training, generating significant research interest in its potential as an exercise mimetic.

endurance, fat oxidation, mitochondrial biogenesis, AMPK activation.

Research on AICAR primarily documents effects related to endurance and fat oxidation and mitochondrial biogenesis and AMPK activation. These are areas covered in preclinical and clinical literature — individual response varies and effects depend on context of use.

For AICAR, its FDA status is investigational (not FDA-approved), and it is designated for research use only. Regulatory status reflects publicly available information and may change. This is not legal or medical advice.

3 providers in the directory currently offer AICAR.

Across 12 research vendors tracked on PeptideBase, AICAR has a median price of about $0.90 per mg, typically ranging $0.64–$1.11 per mg. This reflects research-use vendor pricing, not clinical or prescription costs.

# Summary Research found that AMPK (AMP-activated protein kinase) functions as a key regulator connecting metabolic health to male reproductive processes, including sperm production and testosterone synthesis, with dysfunction linked to reduced sperm quality and fertility issues. This study demonstrated that pharmacological agents targeting AMPK signaling pathways, including AICAR among other approaches, show promise as potential therapeutic strategies for improving male reproductive outcomes in the context of metabolic dysfunction.

Access

How to get AICAR

Market Pricing

12 vendors
$0.64/mgBudget
$0.90/mgMedian
$1.11/mgPremium
$0.64
$0.90
$1.11

Price per mg varies by quantity, vendor type, and formulation. Research use only.

Data verified July 2026 · AICAR price intelligence

Where to buy AICAR

3 providers
3 in stock

Coverage expanding

No verified providers currently list AICAR. Get notified when one does, or explore providers carrying similar peptides in the Performance category.

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Last updated

Cite this page

Data last updated July 27, 2026

Free to reference and republish with attribution to PeptideBase. Choose a format:

PeptideBase. (2026). AICAR — Per-mg Price Benchmark. Retrieved July 28, 2026, from https://peptidebase.io/peptides/aicar

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