Aicar 50mg

Dragon Pharma AICAR (5-Aminoimidazole-4-carboxamide ribonucleotide) 

Dragon Pharma AICAR 50 mg is a high-purity research reagent commonly used to study metabolic regulation, AMPK pathway activation, cellular energy sensing, and mitochondrial biogenesis in controlled laboratory settings.

Product Overview

AICAR (also known as ZMP or Acadesine) is an adenosine analog frequently used by researchers to activate AMP-activated protein kinase (AMPK), the master cellular energy sensor. By increasing intracellular ZMP levels, AICAR mimics low-energy states, prompting AMPK-driven metabolic changes that make it valuable for preclinical studies.

This compound is provided as a research-only lyophilized powder and is not intended for human, clinical, or veterinary use.

Mechanism of Action

Cellular Uptake and Conversion

• AICAR enters cells via nucleoside transporters.
• Inside the cell, AICAR is phosphorylated to form ZMP (AICAR monophosphate), which functions as an AMP analog.
• ZMP mimics AMP, the natural activator of AMPK, allowing researchers to study energy-sensing pathways independently of actual energy depletion.

Activation of AMPK

• AMPK is normally activated under low-energy conditions (high AMP:ATP ratio).
• ZMP binds to the γ-subunit of AMPK, resulting in:
• Allosteric activation of AMPK.
• Enhanced phosphorylation at Thr172 on the α-subunit by upstream kinases (e.g., LKB1), sustaining AMPK activation.
• This process allows prolonged AMPK activation independent of actual cellular AMP levels.

Downstream Effects

Activation of AMPK by AICAR triggers a coordinated metabolic response to restore cellular energy balance:

Increased Catabolic Pathways (ATP-Generating)

• Stimulates glucose uptake via GLUT4 translocation in muscle cells.
• Enhances fatty acid oxidation.
• Promotes mitochondrial biogenesis and oxidative metabolism.

Inhibited Anabolic Pathways (ATP-Consuming)

• Suppresses fatty acid synthesis through inhibition of acetyl-CoA carboxylase (ACC).
• Reduces cholesterol synthesis via inhibition of HMG-CoA reductase.
• Inhibits protein synthesis through mTOR pathway downregulation.

How to Use

• Form: Lyophilized powder (e.g., 50 mg per vial depending on product listing)
• Reconstitution: Use sterile or bacteriostatic water to achieve the desired concentration. Gently swirl until dissolved.
• Aliquoting: Divide into single-use aliquots immediately after reconstitution to prevent freeze–thaw degradation.
• Application: Test a range of concentrations to determine AMPK activation thresholds in your model. Perform pilot studies for optimization.

Benefits of AICAR & Observed Effects

In controlled laboratory experiments, AICAR has been used as a metabolic probe to:

• Activate AMPK signaling reliably
• Increase cellular glucose uptake in multiple tissue models
• Enhance fatty-acid oxidation and mitochondrial output
• Model exercise-like metabolic responses at the cellular level
• Shift energy utilization pathways under stress conditions

Side Effects & Model Observations

Depending on concentration, cell type, and exposure duration, researchers have documented:

• Altered ATP:AMP ratios
• Modulation of mitochondrial activity
• Changes in gene expression related to metabolism
• Concentration-dependent cytotoxicity in sensitive cell lines

These findings vary by experimental model and setup.

Storage & Stability

Form: Lyophilized powder

• Short-term storage: 2–8 °C (refrigerated)
• Long-term storage: −20 °C to −80 °C for extended shelf life
• Handling: Store protected from light, air, and moisture; avoid repeated freeze–thaw cycles
• Solution stability: Reconstituted solutions may be stored at 4 °C for up to several weeks (depending on buffer) or frozen for long-term use

Why Researchers Use AICAR

• Highly reliable activation of AMPK pathways
• Suitable for metabolic and mitochondrial research models
• Reagent-grade purity for reproducibility
• Versatile tool in energy-sensing investigations