AICAR (also known as Acadesine, AICA riboside, CAS 2627-69-2) is the key in the lab that "tricks AMPK into opening the door." After entering the cell, it is phosphorylated by adenosine kinase into ZMP. ZMP looks like AMP, thus coaxing AMPK (the cell's master energy switch) to open-without actually running, muscles follow the "paths they should take during exercise."
Core Advantages and Functions
1. The "Swiss Army Knife" of Metabolic Research
AICAR's most valuable aspect is that it's a classic tool compound for AMPK research. Whether it's glucose uptake in skeletal muscle, inhibition of gluconeogenesis in the liver, or adiponectin secretion in adipose tissue, it provides a clear signaling pathway reading. Those working on diabetes, obesity, and NAFLD-related research almost universally rely on it.
2. A True "Exercise Mimic"
It can induce slow-twitch muscle fiber (Type I) phenotype and promote mitochondrial biosynthesis without exercise. For research on muscle atrophy and age-related sarcopenia, this is a godsend-which is also why it's banned.
3. A Veteran in Cardiovascular Protection
As early as the 1990s, Aicar, under the name Acadesine, entered clinical trials for cardiac surgery protection. Although large-scale Phase III trials later failed to replicate the early impressive data, its performance in ischemia-reperfusion injury models remains an important reference for cardiovascular research.
4. An Unexpected Surprise in Hematologic Oncology
In B-cell chronic lymphocytic leukemia (B-CLL), Aicar exhibited direct pro-apoptotic activity, and Phase I/II clinical trials showed acceptable safety and anti-tumor activity in refractory/relapsed patients. Many people are unaware of this-it's more than just a metabolic tool.
Storage Conditions
Powder: Store at -20°C in a cool, dry, and sealed container, protected from light. It should be stable for 1–4 years according to the supplier's specifications. Do not store in a humid environment at 4°C. Do not repeatedly open the container to absorb moisture.
DMSO Stock Solution: Aliquot 20–50 mg/mL, store at -20℃ or -80℃ protected from light. Absolutely avoid repeated freeze-thaw cycles. Use within 1–3 months of aliquoting for best stability.
Aqueous Solution/PBS: Approximately 2.5–7 mg/mL (within 50 mM) in water, lower in PBS; prepare fresh and use immediately, do not store overnight. Dilute residual DMSO to negligible levels.
Before opening, allow to warm to room temperature for 20–30 minutes to prevent condensation from contaminating the powder.
Precautions
The three names Acadesine / AICA Riboside / AICAR refer to the same product: Research Use Only. It is not a supplement, not a human drug, and not a sports enhancer. Storing even one bottle at home is non-compliant; athletes handling it will be a WADA violation.
The powder is irritating. Wear a lab coat, gloves, and a mask when weighing. Do not inhale or get it in your skin or eyes. Dispose of the waste liquid as hazardous chemical waste.
The working concentration for cells is commonly 0.5–5 mM (typically 0.5–2 mM, 30 min–24 h), but this varies greatly between different cell types. Do not blindly follow dosages found online for animal testing. In vivo saline/CMC-Na formulations must also be prepared fresh for each use.
It not only targets AMPK but also interferes with purine synthesis and is sensitive to adenosine deaminase (it will be degraded after prolonged incubation with serum). Before obtaining data, you should question whether this effect is truly AMPK-specific.
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