At a glance
Effects
- Endurance / exercise-mimetic effect: In sedentary mice, 4 weeks of AICAR increased running endurance by roughly 44–45% without training; no equivalent human performance data exists[2][3].
- Increased fat oxidation: AMPK activation inhibits acetyl-CoA carboxylase, lowering malonyl-CoA and enabling skeletal-muscle fatty-acid oxidation[6][1].
- Improved glucose uptake / insulin sensitivity: Drives insulin-independent GLUT4 translocation and glucose uptake into skeletal muscle; lowered blood glucose in diabetic rodent models[6][7].
- Mitochondrial biogenesis: Activates the AMPK–PGC-1α axis, promoting mitochondrial biogenesis and mitophagy[4][6].
AMPK activator / adenosine nucleoside analog (acadesine)
No FDA-approved use; investigational only
IV in trials; sold for SubQ/IV — poor oral bioavailability
Parent riboside ~90 min (reported); active ZMP longer
WADA-banned S4.4 (in & out of competition)
About AICAR
Every point here is drawn from public medical and harm-reduction sources. A bracketed number after a claim — like [1]— is a reference: tap it to open the exact source it's based on (numbered list at the bottom). It is not a rating or score. Educational information, not medical advice.
Product specifics
- Est. delivery
- 3–7 business days · EU tracked
Product details as stated by the vendor (claims, not independently verified). Delivery is our standard EU estimate.
What it is
AICAR (acadesine; 5-aminoimidazole-4-carboxamide ribonucleoside) is a small-molecule nucleoside analog of adenosine that acts as an activator of AMP-activated protein kinase (AMPK), the cell's master energy sensor[1][6]. It is an investigational research compound with no FDA-approved medical use; it was studied for cardioprotection and leukemia but never gained approval, and it is now used mainly as a laboratory tool and, controversially, as a performance/endurance "exercise mimetic"[3][7].
How it works
AICAR is cell-permeable; once inside cells it is phosphorylated by adenosine kinase to ZMP (AICAR monophosphate), an AMP-mimetic that allosterically activates AMPK by binding its gamma subunit[6][1]. Activated AMPK switches on energy-generating (catabolic) pathways and switches off energy-consuming (biosynthetic) ones, driving insulin-independent glucose uptake via GLUT4, increased fatty-acid oxidation, mitochondrial biogenesis, and autophagy[6][2]. Note that AICAR also has well-documented AMPK-independent "off-target" effects because ZMP accumulates to high concentrations, so its biology is more complex than "pure AMPK activation"[1].
Risks & side effects
Most important: AICAR has barely been studied in healthy humans: its only human data come from cardiac-surgery and oncology trials, and regulators warn that excessive or wrong-tissue AMPK activation can cause serious effects including neurodegeneration and blocked cell division, while naturally accumulating AICAR is linked to metabolic disorders[8][3]. There is no established safe recreational dose, and because it can both suppress and (in some tumors) support cancer-cell survival, a personal or family history of cancer is treated as a contraindication[5][8].
Common
Serious
- Excess or mis-targeted AMPK activation can cause neurodegeneration or prevent cells from dividing[8]
- Potential cardiac hypertrophy with long-term or uncontrolled use[11]
- ZMP can become ion-trapped and accumulate in red blood cells and endothelial cells to toxic levels, especially with IV dosing[10]
- Can lower blood pressure via AMPK-mediated vasorelaxation — additive with antihypertensives[10]
Safety & harm reduction
- Anyone with a personal or family history of cancer, particularly metabolically active cancers (relative contraindication)[5][8]
- Competitive athletes subject to anti-doping rules — banned at all times by WADA[5][9]
- People with cardiovascular disease, given signals of possible cardiac hypertrophy and blood-pressure lowering[11][10]
Dosage context
There is no established or prescribable human dose for performance or metabolic use, and no completed human efficacy trial supports any regimen[3][9]. For context only (NOT a recommendation): the pivotal mouse endurance study used 500 mg/kg/day for 4 weeks, and human cardiac-surgery (acadesine) trials used IV infusion at 0.1 mg/kg/min for ~7 hours[2][5]. Oral dosing is unreliable because most AICAR is excreted unchanged in urine[10].
Sources
- 1.PubChem / AICAR AMPK activator background (PureLab references PubChem & Cells review)
- 2.Narkar et al., AMPK and PPARδ Agonists Are Exercise Mimetics (Cell, 2008) — PMC
- 3.Superpower — AICAR (Acadesine) guide (regulatory/trial status, PubChem CID 378611)
- 4.Chronic AICAR, glycogen & fatty-acid oxidation in skeletal muscle — PMC
- 5.MyPeptideMatch — AICAR dosing/WADA/cancer cautions
- 6.Višnjić et al., AICAr AMPK activator with AMPK-independent effects (Cells, 2021) — PMC
- 7.SeekPeptides — AICAR overview (purine intermediate, CABG meta-analysis)
- 8.USADA — What athletes should know about AICAR and AMPK activators
- 9.WADA Prohibited List — S4 Hormone and Metabolic Modulators (AICAR named)
- 10.USPTO patent — AICAR oral bioavailability, IV/ZMP ion-trapping pharmacokinetics
- 11.AnabolicPlanner — AICAR side effects (cardiac hypertrophy, appetite) and dosing context
This information is provided for educational and harm-reduction purposes only. It is not medical advice. These substances can carry serious health risks; effects and safe use vary by individual. Consult a qualified healthcare professional before use. Legal status varies by country — it is your responsibility to know your local law. We do not encourage misuse.