AICAR

Overview

AICAR (acadesine / AICA riboside) is a purine nucleoside analog and AMP-mimetic AMPK activator — not a peptide. It was studied in registered human trials as acadesine (for cardioprotection and leukemia, not performance), is not FDA-approved, and is WADA-prohibited at all times. It is sold on the gray market as an "exercise mimetic."

Mechanism of Action

AICAR is phosphorylated intracellularly to ZMP, an AMP-mimetic that allosterically activates AMPK (binding the γ-subunit CBS domains and protecting Thr172 from dephosphorylation). Because ZMP reaches high intracellular levels, AICAR also has substantial AMPK-independent effects on other AMP-sensitive enzymes and nucleotide metabolism (Visnjic et al., 2021).

Research Summary

As acadesine, AICAR was tested in registered human trials by IV infusion: the large RED-CABG cardioprotection trial (JAMA 2012) was stopped for futility, and a Phase I/II study in relapsed/refractory CLL established 210 mg/kg IV as the optimal dose. No human trial evaluated AICAR for exercise, fat loss, or longevity, and no validated non-IV dosing exists. Not FDA-approved; not a peptide.

Vendors selling AICAR

Scored vendors carrying AICAR, ranked by trust grade. Grades are computed from indexed Certificates of Analysis. Full $/mg pricing is on the comparison page.

Reported Side Effects

• In supervised IV trials: hyperuricemia (managed with allopurinol), transient creatinine elevation, infusion-related hypotension, mild transient anemia/thrombocytopenia
• The large RED-CABG cardioprotection trial was stopped for futility — no demonstrated benefit
• WADA-prohibited at all times (S4.4) as an AMPK-activating metabolic modulator
• No human safety data for oral/subcutaneous or chronic self-administered use

Compare AICAR with Others

Research References

• Narkar VA, et al. AMPK and PPARδ agonists are exercise mimetics. Cell. 2008. PMID 18674809.
• Newman WH, et al. RED-CABG randomized controlled trial of acadesine. JAMA. 2012. PMID 22782417.
• Višnjić D, et al. AICAr, a widely used AMPK activator with AMPK-independent effects: systematic review. Cells. 2021. PMID 34064363.

Frequently asked questions

Has AICAR been independently lab-tested?

Disclosed Labs has collected 3 Certificates of Analysis (COA) for AICAR from 3 independent testing labs. 3 vendors have submitted material for testing. Products average 99.3% tested purity across the corpus. Full testing data is available at https://www.disclosedlabs.com/peptides/aicar/testing.

What is the average purity of AICAR on the market?

Based on 3 COAs analyzed by Disclosed Labs, AICAR products average 99.3% (±0.2%) tested purity. Individual vendor results vary; see per-vendor COA data at https://www.disclosedlabs.com/peptides/aicar/coas.

Which labs have tested AICAR?

Independent labs that have tested AICAR include: ILS Labs (Grade B). Full lab credibility grades and profiles are at https://www.disclosedlabs.com/labs.

Where can researchers source AICAR?

2 vendors with Disclosed Labs trust grades currently list AICAR, including Peptide Tech, Kimera Chems. Compare live prices and lab-verified COAs at https://www.disclosedlabs.com/prices/aicar.

How does AICAR work?

AICAR is phosphorylated intracellularly to ZMP, an AMP-mimetic that allosterically activates AMPK (binding the γ-subunit CBS domains and protecting Thr172 from dephosphorylation). Because ZMP reaches high intracellular levels, AICAR also has substantial AMPK-independent effects on other AMP-sensitive enzymes and nucleotide metabolism (Visnjic et al., 2021).

What does the research say about AICAR?

As acadesine, AICAR was tested in registered human trials by IV infusion: the large RED-CABG cardioprotection trial (JAMA 2012) was stopped for futility, and a Phase I/II study in relapsed/refractory CLL established 210 mg/kg IV as the optimal dose. No human trial evaluated AICAR for exercise, fat loss, or longevity, and no validated non-IV dosing exists. Not FDA-approved; not a peptide.