For laboratory and research use only. Not for human consumption.
Metabolic

AICAR

Also known as: Acadesine, AICA riboside, 5-Aminoimidazole-4-carboxamide ribonucleoside, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside, ARA-100

Clinical Trials
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Key Facts: AICAR

Category
Metabolic
FDA Status
Not FDA Approved
Clinical Status
Not approved - No FDA or EMA approval for any use. Developed as acadesine (IV) for cardioprotection in heart surgery; phase 3 RED-CABG stopped for futility (2012). Phase I/II leukemia studies did not lead to approval. WADA: prohibited at all times under S4.4.1 (activators of AMPK, AICAR named explicitly) on the 2026 Prohibited List.
Banned in Sport (WADA)
Prohibited at all times under WADA S4 (metabolic modulators, AMPK activators), where AICAR is named.
Administration
Intravenous infusion in human trials; intraperitoneal injection in mice
Typical Dose
No established dose; human data are IV infusions only
Frequency
Single infusions or short cycles in trials
Duration
Single infusions or short cycles in human trials; 4 weeks in the mouse endurance study
Also Known As
Acadesine, AICA riboside, 5-Aminoimidazole-4-carboxamide ribonucleoside, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside, ARA-100

How does AICAR work?

Once inside cells, AICAR is phosphorylated to ZMP (AICAR monophosphate), which behaves like AMP and activates AMP-activated protein kinase (AMPK). AMPK is the master switch cells flip when energy runs low: it pushes glucose uptake and fat oxidation up and energy-costly processes like fat and protein synthesis down. In mouse muscle, AMPK activation by AICAR turned on a set of oxidative, endurance-type genes overlapping with those controlled by PPAR-delta. The catch is that ZMP is not a clean AMPK switch: it also affects other AMP-sensitive enzymes and the adenosine system, which is why acadesine was originally developed as an "adenosine regulating agent" for the heart. Effects in mice also do not automatically translate to people. A 2011 human study found that IV AICAR during an insulin clamp caused vasodilation (higher heart rate, lower blood pressure) but no direct effect on glucose uptake.

What does the research show?

The headline study is Narkar and colleagues (Cell, 2008): four weeks of AICAR at 500 mg/kg/day by injection in untrained mice induced metabolic genes and increased running endurance by 44%. That paper is the source of nearly all the hype, and it was in mice at a huge dose. Human work is a different picture. As acadesine, it went into the RED-CABG phase 3 trial (JAMA 2012), giving 0.1 mg/kg/min IV for 7 hours around bypass surgery. The trial was stopped for futility after 3,080 patients: the primary outcome was 5.1% with acadesine versus 5.0% with placebo, so no benefit. A phase I/II study in relapsed chronic lymphocytic leukemia (Van Den Neste et al., Cancer Chemotherapy and Pharmacology) set the maximum tolerated single IV dose at 210 mg/kg; at 315 mg/kg two of three patients had dose-limiting toxicity (tumor lysis syndrome and kidney injury), and hyperuricemia was a recurring problem that required allopurinol. There are no human trials showing AICAR improves endurance, body composition, or longevity in healthy people. It is also one of the more catchable doping agents: anti-doping labs use carbon isotope ratio testing to separate injected AICAR from the body's natural AICAR.

Trial Progress:Phase III
Pre
I
II
III
IV
FDA

What doses have been studied?

Human Trials·Human IV trials in surgery and leukemia (phase 3 failed); endurance effects shown only in mice

Typical Dosingⓘ

Community experience

Common Dose

No established dose; human data are IV infusions only

Range

25-210 mg/kg per IV infusion in clinical studies

Frequency

Single infusions or short cycles in trials

Every human dose in the literature is a supervised intravenous infusion in a hospital or research setting, usually in sick patients. The mouse endurance dose (500 mg/kg/day) does not translate to people. No published research supports the small subcutaneous doses discussed online, and their effect is unknown.

Research Dosingⓘ

Scientific studies

Doses from published research (IV in humans, injection in mice). No approved or validated human dose exists.

Duration

Single infusions or short cycles in human trials; 4 weeks in the mouse endurance study

Administration

Intravenous infusion in human trials; intraperitoneal injection in mice

When and how is AICAR taken?

Best Time to Take

No evidence-based timing in healthy people

Not established outside clinical trials

Food Recommendation

With or without food

Why This Timing?

All human research used one-off or short-cycle IV infusions in clinical settings, so there is no data on ideal daily timing. Claims about pre-workout timing come from mouse studies, not human trials.

What are the side effects of AICAR?

Not everyone experiences these effects. Individual responses vary based on dosage, duration, and personal factors.

  • ●Hyperuricemia (high uric acid), seen repeatedly in human trials
  • ●Kidney injury at high IV doses
  • ●Tumor lysis syndrome in leukemia patients at high doses
  • ●Lower blood pressure and faster heart rate from vasodilation
  • ●Anemia, nausea, and diarrhea reported in the leukemia trial
  • ●No long-term human safety data outside of hospital IV use
  • ●Positive doping test risk (WADA S4, detectable by isotope ratio testing)

References

Research This Peptide Further

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Frequently Asked Questions

What does AICAR do?

AICAR is not a peptide at all. It is a small nucleoside (a building block related to the purine pathway) that cells convert into ZMP, a molecule that mimics AMP and switches on AMPK, the cell's energy sensor. It became famous in 2008 when a Salk Institute study showed sedentary mice on AICAR ran 44% further, earning it the "exercise in a pill" label. Human data tell a much less exciting story: it was tested as an intravenous drug (acadesine) for heart surgery and leukemia, the big heart trial failed, and nothing is approved.

How does AICAR work?

Once inside cells, AICAR is phosphorylated to ZMP (AICAR monophosphate), which behaves like AMP and activates AMP-activated protein kinase (AMPK). AMPK is the master switch cells flip when energy runs low: it pushes glucose uptake and fat oxidation up and energy-costly processes like fat and protein synthesis down. In mouse muscle, AMPK activation by AICAR turned on a set of oxidative, endurance-type genes overlapping with those controlled by PPAR-delta. The catch is that ZMP is not a clean AMPK switch: it also affects other AMP-sensitive enzymes and the adenosine system, which is why acadesine was originally developed as an "adenosine regulating agent" for the heart. Effects in mice also do not automatically translate to people. A 2011 human study found that IV AICAR during an insulin clamp caused vasodilation (higher heart rate, lower blood pressure) but no direct effect on glucose uptake.

Is AICAR FDA approved?

No, AICAR is not currently FDA approved. Current status: Not approved - No FDA or EMA approval for any use. Developed as acadesine (IV) for cardioprotection in heart surgery; phase 3 RED-CABG stopped for futility (2012). Phase I/II leukemia studies did not lead to approval. WADA: prohibited at all times under S4.4.1 (activators of AMPK, AICAR named explicitly) on the 2026 Prohibited List.

Is AICAR banned in sport?

Prohibited at all times under WADA S4 (metabolic modulators, AMPK activators), where AICAR is named.

What are the side effects of AICAR?

Reported side effects include: Hyperuricemia (high uric acid), seen repeatedly in human trials, Kidney injury at high IV doses, Tumor lysis syndrome in leukemia patients at high doses, Lower blood pressure and faster heart rate from vasodilation, Anemia, nausea, and diarrhea reported in the leukemia trial. Individual responses vary based on dosage, duration, and personal health factors.

What is the typical dose of AICAR?

Community-reported common dose: No established dose; human data are IV infusions only (Single infusions or short cycles in trials). Range: 25-210 mg/kg per IV infusion in clinical studies. Administration: Intravenous infusion in human trials; intraperitoneal injection in mice. Community-reported doses. Not medical advice. Consult healthcare provider.

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