AICAR

• AMPK signaling, cellular energy homeostasis and controlled pathway-engagement studies
• Skeletal-muscle fatty-acid oxidation, glycogen metabolism, insulin-sensitivity and glucose-uptake research
• The 2008 Cell study reported a 44% increase in treadmill running endurance in sedentary mice after four weeks, a preclinical result that does not establish an exercise substitute or performance benefit in humans
• Earlier cardiac-surgery trials suggested benefit, but Phase 3 RED-CABG stopped for futility after 3,080 of a planned 7,500 participants were randomized and the primary endpoint occurred in 5.1% of the acadesine group versus 5.0% of the placebo group
• Autophagy research includes an in-vitro CML model in which the reported cell-death effect was AMPK-independent and PKC-dependent (PMC2775681)
• A multicenter Phase I/II Acadra study in 24 patients with relapsed or refractory CLL reported preliminary biological responses but did not establish an approved oncology use (PMC3579463)
• Mitochondrial-biogenesis, ischemia-reperfusion, metabolic and cytotoxicity findings remain model- and mechanism-specific research contexts
• A 2021 systematic review found that many effects historically attributed to AMPK activation are AMPK-independent, including effects on nucleoside transport, adenosine deaminase, purine-nucleotide synthesis and PKC signaling (PMC8147799).

CAS

2627-69-2

Formula

C₉H₁₄N₄O₅

Molecular weight

258.23-258.24 Da

Appearance

Lot-specific research material; confirm released-lot solid form and appearance on the COA

Purity

≥ 99.0% · target, verify batch COA

Storage

Store and ship according to the lot COA and validated stability data for the exact solid form, solvent, concentration, pH, container and intended assay. Generic minus 20 degrees Celsius, two-year and post-solution dating claims are not interchangeable. Use validated aliquoting where appropriate, avoid unvalidated freeze-thaw cycles and document excursions.

MOQ

On request

Lead time

10–18 days

The catalogue name AICAR commonly refers to AICAr/acadesine, 5-aminoimidazole-4-carboxamide ribonucleoside. Cells convert this riboside through adenosine kinase to the phosphorylated ribotide AICAR/ZMP (PubChem CID 65110), an AMP mimic that can activate AMPK. A 2008 mouse study reported increased treadmill endurance after four weeks, but it did not establish an exercise substitute in humans. The Phase 3 RED-CABG trial stopped for futility and found no improvement in its primary clinical endpoint. The current 2026 WADA list includes AICAR in S4.4.1 among AMPK activators prohibited at all times. This material remains RUO and is not for human or athletic use.

• AICAR is a classic experimental probe for AMPK and energy-metabolism pathways, but it also has important AMPK-independent effects
• The 2008 Cell mouse study reported improved endurance in sedentary mice and does not establish an exercise substitute in humans
• RED-CABG did not improve its primary clinical endpoint, and the small CLL Phase 1/2 study did not establish an approved oncology use
• Autophagy, mitochondrial, diabetes and cytotoxicity findings remain model- and mechanism-specific.

AICAr enters cells through nucleoside transporters and is phosphorylated by adenosine kinase to AICAR/ZMP. ZMP binds the AMPK gamma subunit, promotes AMPKα Thr172 phosphorylation and protects it from dephosphorylation, but is substantially less potent than physiological AMP and may accumulate at high intracellular concentrations. AICAr/ZMP also affects nucleoside transport, purine metabolism and other AMPK-independent pathways. Mechanistic studies therefore require direct pathway readouts, genetic controls and appropriate comparator agonists rather than treating AICAr as a selective AMPK switch.

• AICAR/acadesine is not an approved medicine and this material is not for human use
• RED-CABG enrolled thousands of surgical patients but stopped for futility rather than demonstrating clinical benefit
• The small CLL trial explored high intravenous doses and dose-limiting toxicity; it does not define a safe exposure for healthy people or an RUO batch
• Lactate, uric-acid and other metabolic effects, along with incomplete long-term, reproductive and carcinogenic evidence, require conservative laboratory controls
• WADA's 2026 Prohibited List explicitly includes AICAR under S4.4.1 AMPK activators, prohibited at all times
• Anti-doping prohibition does not establish chemical quality.

Interactions reported in the literature

• AICAR is often combined with metformin, GW501516, dorsomorphin or chemotherapy agents as an experimental comparator or pathway probe
• Such combinations are research designs, not validated stacks
• Because AICAR has AMPK-independent effects, reversal by one AMPK inhibitor is not sufficient proof of pathway specificity
• AICAR and relevant PPAR-delta agonists are prohibited in sport; combining them compounds compliance concerns rather than establishing safety or efficacy.

AICAR50 mg · WHJLP-AICAR50-260605-A

AICAR100 mg · WHJLP-AICAR100-260605-A

Representative records, refreshed periodically

Published COAs show representative factory batches and may not be the latest available. For a current quote or shipment, our sales team can confirm the applicable lot and provide its COA.

Independent testing, arranged on request

Third-party reports are not routinely published. If independent verification is required, we can agree the laboratory, method, acceptance criteria and remedy before testing. If the agreed specification is not met, an appropriate resolution—including a refund where applicable—can be discussed under the agreed terms. Unless otherwise agreed in writing, the buyer pays the cost of this optional testing.

Help reviewing your COA

Need help reading a factory COA or third-party report? Our sales team can clarify test items, specifications and how the results relate to the lot under discussion.

Ask for the current packet, not a generic certificate

• A white powder and HPLC area percentage do not establish correct nucleoside identity, assay or absence of ZMP and related impurities
• Require orthogonal identity such as high-resolution LC-MS plus spectroscopic confirmation, chromatographic purity and impurity profile with raw data, quantitative assay, water, residual solvents and elemental impurities where relevant, and lot-specific stability
• The COA must distinguish AICAR/acadesine from phosphorylated ZMP by mass, retention and structural evidence
• A third-party logo or RUO label alone is not quality evidence.

Store and ship according to the lot COA and validated stability data for the exact solid form, solvent, concentration, pH, container and intended assay. Generic minus 20 degrees Celsius, two-year and post-solution dating claims are not interchangeable. Use validated aliquoting where appropriate, avoid unvalidated freeze-thaw cycles and document excursions.

State destination, season, acceptable transit exposure and whether your protocol requires insulated or cold-chain service. Additional temperature-control cost is quoted explicitly.

• PubChem CID 17513 and related standardized records support AICAR/acadesine chemistry, while PubChem CID 65110 supports ZMP distinction. Narkar et al. 2008 is a mouse exercise-metabolism study. The 2012 RED-CABG randomized trial is decisive negative Phase 3 clinical evidence, while the earlier JAMA meta-analysis explains why development proceeded. The CLL Phase 1/2 study supplies limited high-dose oncology safety data. The 2021 systematic review is essential for AMPK-independent effects. Salk's release is institutional context, USADA explains athlete risk, and the current official WADA list controls anti-doping status.

1. 01

   AMPK and PPARdelta agonists are exercise mimetics

   Cell · 2008 · peer-reviewed original research

   Open source
2. 02

   Effect of Adenosine-Regulating Agent Acadesine on Morbidity and Mortality Associated With Coronary Artery Bypass Grafting: The RED-CABG Randomized Controlled Trial

   JAMA · 2012 · randomized controlled trial (peer-reviewed)

   Open source
3. 03

   Effects of Acadesine on Myocardial Infarction, Stroke, and Death Following Surgery: A Meta-analysis of the 5 International Randomized Trials

   JAMA · 1997 · meta-analysis of randomized controlled trials (peer-reviewed)

   Open source
4. 04

   Acadesine for patients with relapsed/refractory chronic lymphocytic leukemia (CLL): a multicenter phase I/II study

   Cancer Chemotherapy and Pharmacology · 2013 · phase I/II clinical trial (peer-reviewed)

   Open source
5. 05

   AICAr, a Widely Used AMPK Activator with Important AMPK-Independent Effects: A Systematic Review

   Cells · 2021 · systematic review (peer-reviewed)

   Open source
6. 06

   Exercise in a Pill

   Salk Institute for Biological Studies · 2008 · institutional press release

   Open source
7. 07

   What Athletes Should Know About AICAR and Other Prohibited AMP-Activated Protein Kinase Activators

   U.S. Anti-Doping Agency (USADA) · 2023 · regulatory/anti-doping body educational article

   Open source