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AICAR

Studied for skeletal muscle glucose uptake, blood glucose in type 2 diabetes and endurance capacity. A nucleoside that cells convert into an AMP mimic, described as an AMPK activator in 1995 and developed as the cardiac drug acadesine.

categorylongevity
clinical evidenceearly human
community adoptionniche
uses graded4
sources10
last reviewed24 Aug 2026
compound file

The answer, first. A nucleoside that cells convert into an AMP mimic, described as an AMPK activator in 1995 and developed as the cardiac drug acadesine.

The strongest evidence is for skeletal muscle glucose uptake, graded C — small or open-label human only. Muscle 2-deoxyglucose uptake rose 2.1-fold three hours after AICAR in 29 healthy men, against 4.7-fold for cycling.

Whole-body disposal moved 7% 2. Acute infusion only. The rest of what it is sold for — endurance capacity, cardiac protection in bypass surgery — grade D or E: animal or mechanism data only, or a claim the human trials have already tested and not supported.

What it is used for

Every use graded on its own evidence, not the compound as a whole. 4 outcomes, ranked by what the human record supports.

#outcome · human · animal · gradewhat the best evidence actually shows
01Skeletal muscle glucose uptake1 controlled trial, n=29 · broad rodent recordgrade CMuscle 2-deoxyglucose uptake rose 2.1-fold three hours after AICAR in 29 healthy men, against 4.7-fold for cycling. Whole-body disposal moved 7% 2. Acute infusion only.
02Blood glucose in type 2 diabetes1 infusion study, n=10 · Zucker rat infusionsgrade CIntravenous AICAR at 0.75 mg per kilogram per minute cut hepatic glucose output and lowered plasma glucose in ten men with type 2 diabetes 3. Uptake blunts with age 4.
03Endurance capacityno trial · 1 landmark mouse studygrade DFour weeks of AICAR raised treadmill running endurance 44% in sedentary mice 1. No human endurance or performance trial has been published in the eighteen years since.
04Cardiac protection in bypass surgery1 phase 3, n=3080 · ischaemia modelsgrade EA 3080-patient randomised trial stopped for futility: 5.1% against 5.0% on placebo for death, stroke or severe ventricular dysfunction 5. A 4043-patient meta-analysis had been positive 6.
gradewhat it means
ARegulatory approval, or multiple adequately-powered trials agreeing with each other
BAt least one well-powered human randomised trial, with the direction replicated
CSmall or open-label human trials only
DAnimal or mechanism data only, with no controlled human outcome
EA claim the human trials have already killed

How it works

The proposed mechanism, in three steps. A mechanism is a reason to run a trial, never a substitute for one.

1targetA nucleoside, not a peptide. Cells convert it to ZMP, which mimics AMP and allosterically activates AMP-activated protein kinase.
2signalAMPK then switches biosynthesis off. It inactivates HMG-CoA reductase and halts fatty-acid and sterol synthesis in hepatocytes.
3effectIn mice, four weeks induced oxidative-metabolism genes and raised running endurance without training. In isolated adipocytes it blocks lipolysis.

What it does not do

Claims the current record does not support. Worth knowing before you set expectations.

not supported by the evidence

How it is used

What published protocols administered, and what the community reports doing. Descriptive on both counts, and never a recommendation.

routeEvery published human study used intravenous infusion. Doping-control work also tracked a single oral dose 238.
formatSold as a white powder for reconstitution, and as oral capsules.
published dosesInfusions ran 0.75 mg per kilogram per minute in ten men with type 2 diabetes 3. Cardiac surgery used 0.1 mg per kilogram per minute for seven continuous hours, n=3080 5. The leukaemia study set 210 mg per kilogram as the maximum tolerated single dose over four hours, n=24 9. Descriptive of trial protocols.
human pharmacokineticsNo human half-life published in the trials reviewed. AICAR occurs naturally in urine, which complicates any exposure reading 8.
reported conventionsAs reported on Reddit r/Peptides and endurance and cycling forums, 2010 to 2026: milligram amounts taken orally or injected in short blocks around competition. Reports are sparse, inconsistent on both route and amount, and orders of magnitude below the per-kilogram infusions the trials used. Convention, not guidance.
commonly paired withMOTS-c

This site does not publish protocols to follow. The doses above are what studies administered or what users report, stated as facts about the literature and the market. How protocols are structured, mixing and storage and the reconstitution calculator cover the arithmetic.

What to expect

Where a trial measured it, the trial. Where only the community reports it, that is said out loud.

onsetHuman effects were measured acutely: muscle glucose uptake at three hours 2, hepatic glucose output during the infusion itself 3. The endurance result is a four-week mouse finding 1. No trial has measured onset for any performance outcome.
most common reportAs reported: little or nothing felt. No human trial has measured a subjective effect, and the reported cluster is absence rather than sensation.
adverse effectsGrade 2 or worse hyperuricaemia was common in leukaemia dosing but resolved with allopurinol. Transient anaemia, renal impairment and infusion hypotension also occurred, n=24 9. In cardiac surgery, events matched placebo apart from a transient uric acid rise, n=4043 6.
the stop signalTrial record: the leukaemia study set 210 mg per kilogram as the maximum tolerated single dose, above which toxicity limited dosing 9. No community stop signal is reported.

Approval and status

What regulators and sport bodies have actually said, separately from what the evidence shows.

approvalNever approved. Acadesine failed its phase 3 cardiac surgery trial in 2012 5.
FDANo FDA approval for any indication. Sold in the United States as a research chemical, not as a medicine.
sport [WADA]Prohibited at all times, S4.4.1 AMPK activators, named 10.
sold asresearch chemical

Check the vial

The grade above describes a molecule studied under controlled conditions. It says nothing about the powder in a particular vial.

That gap is the one part of this market a reader can actually close. How to read a certificate of analysis covers the five measures in five minutes, and the 2026 audit grades vendors on the documents they publish against a rubric printed in full.

Questions we get

What is AICAR used for?

It is sold as an exercise mimetic. That claim rests on mice: four weeks of AICAR raised treadmill endurance 44% in sedentary animals, and no human endurance trial has followed.

The human record sits elsewhere. As the cardiac drug acadesine it was given to 3080 bypass patients and failed. It has also been infused in small metabolic studies in healthy men and in type 2 diabetes.

How is AICAR used?

Descriptively: every published human study infused it intravenously. Metabolic studies ran 0.75 mg per kilogram per minute. Cardiac surgery ran 0.1 mg per kilogram per minute for seven hours.

The leukaemia study reached 210 mg per kilogram as a single four-hour infusion. Vendors sell powder and capsules for oral or subcutaneous use in milligram amounts. That is far below anything a trial gave, and by a route no trial used.

How long does AICAR take to work?

For anything a buyer wants, no trial has measured it. Human studies read acute effects: muscle glucose uptake at three hours, hepatic glucose output during the infusion itself.

The endurance finding is a four-week result in mice. There is no published human half-life, and AICAR occurs naturally in urine, which makes even exposure hard to read.

Is AICAR an approved drug?

No. AICAR is sold as a research chemical, not as an approved medicine. As acadesine it reached phase 3 in cardiac surgery and failed in a 3080-patient trial in 2012.

It is prohibited in sport at all times, named on the WADA list under AMPK activators. On our index it is graded early human on clinical evidence and niche on community adoption, and those two are rated separately on purpose.

References

  1. Narkar VA, et al. AMPK and PPARdelta agonists are exercise mimetics. Cell. 2008. PMID 18674809
  2. Cuthbertson DJ, et al. 5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men. Diabetes. 2007. PMID 17513706
  3. Boon H, et al. Intravenous AICAR administration reduces hepatic glucose output and inhibits whole body lipolysis in type 2 diabetic patients. Diabetologia. 2008. PMID 18709353
  4. Babraj JA, et al. Blunting of AICAR-induced human skeletal muscle glucose uptake in type 2 diabetes is dependent on age rather than diabetic status. Am J Physiol Endocrinol Metab. 2009. PMID 19190259
  5. Newman MF, et al. Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial. JAMA. 2012. PMID 22782417
  6. Mangano DT, et al. Effects of acadesine on myocardial infarction, stroke, and death following surgery. A meta-analysis of the 5 international randomized trials. JAMA. 1997. PMID 9002496
  7. Corton JM, et al. 5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells? Eur J Biochem. 1995. PMID 7744080
  8. Piper T, et al. Determination of 13C/12C ratios of endogenous urinary 5-amino-imidazole-4-carboxamide 1-beta-D-ribofuranoside [AICAR]. Rapid Commun Mass Spectrom. 2014. PMID 24760559
  9. Van Den Neste E, et al. Acadesine for patients with relapsed/refractory chronic lymphocytic leukemia [CLL]: a multicenter phase I/II study. Cancer Chemother Pharmacol. 2013. PMID 23228986
  10. World Anti-Doping Agency. Prohibited List 2026, International Standard, in force 1 January 2026. Section S4.4.1, activators of the AMP-activated protein kinase. wada-ama.org

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