AICAR

AICAR (Acadesine / AICA Riboside)

CAS: 2627-69-2

⚠️ This is not a peptide! It is a small-molecule nucleoside-based AMPK activator intended for laboratory research only;

Basic Information

– Full Name: 5-Aminoimidazole-4-carboxamide 1-β-D-ribofuranoside (AICA riboside)

– Molecular Formula: \(\mathbf{C_{9}H_{14}N_{4}O_{5}}\)

– Molecular Weight: 258.23 Da

– Properties: White / off-white crystalline lyophilized powder, highly soluble in water

Mechanism of Action (Core Research)

After AICAR enters the cell, it is phosphorylated by adenosine kinase to form ZMP; ZMP mimics AMP and allosterically activates AMPK (AMP-activated protein kinase, the cell’s master energy switch)

1. Skeletal Muscle: Induces non-insulin-dependent GLUT4 translocation, promoting glucose uptake; enhances fatty acid oxidation; upregulates PGC-1α, promoting mitochondrial biogenesis; commonly referred to in the literature as the “workout pill”

2. Liver: Inhibits gluconeogenesis, reduces triglyceride synthesis, and decreases hepatic lipid accumulation

3. Adipose Tissue: Activates AMPK, inhibits lipogenesis, and enhances adiponectin secretion

4. Cardiovascular / Ischemia Models: Used for myocardial ischemia-reperfusion protection and research on renal ischemic injury

Key Distinction: AICAR (AICA riboside, membrane-permeable, commonly used in research) vs. ZMP (AICAR monophosphate, the intracellular active form, which has difficulty crossing the cell membrane)

Pharmacokinetic Highlights

– In vivo half-life: Approximately 2–3 hours

– Metabolic pathway: Purine metabolic pathway; metabolized to uric acid; high doses may elevate serum uric acid levels and increase the risk of gout

– Administration: Subcutaneous or intraperitoneal injection is commonly used in animal studies; intravenous infusion is used in early-phase clinical trials

Dissolution and Storage (Laboratory Procedures)

1. Solvents: Sterile water, PBS, or BAC-inactivated water are all acceptable; it can also be dissolved in DMSO (for stock solution preparation); acetic acid-water (AA) is not required (unlike with peptides)

2. Lyophilized powder: Store long-term at -20°C in a dry, light-protected environment; stable for up to 2–3 years

3. Reconstituted solution: Refrigerate at 2–8°C and use within 14–21 days; aliquot and store at -20°C, avoiding repeated freeze-thaw cycles

## Research Combination References

– Metabolism / Endurance Models: AICAR + Epithalon

– Insulin Resistance, Fat Metabolism: AICAR + Adipotide

– Inflammation, Tissue Repair: AICAR + ARA290

⚠️ Important Notice

1. For in vitro cellular and preclinical animal research only; not approved for routine human use; self-administration in humans is strictly prohibited.

2. Listed on the WADA Prohibited List; use in any sporting event constitutes a doping violation.

3. High-dose risks: hyperuricemia, gout, fasting hypoglycemia, and lactic acidosis.

4. All information is based solely on chemical and preclinical literature and does not constitute guidance for human use.