Imapextide | CAS No. 3004569-93-8 | Supplier Manufacturer

Description

Product Description

Imapextide (CAS No. 3004569-93-8) is a synthetic glucagon-like peptide-1 (GLP-1) receptor antagonist designed to block the actions of endogenous GLP-1 (glucagon-like peptide-1). GLP-1 is a central incretin hormone that enhances insulin secretion, suppresses glucagon release, delays gastric emptying, and promotes satiety. While GLP-1 receptor agonists are widely studied for their therapeutic benefits in type 2 diabetes and obesity, antagonists such as Imapextide serve the equally important purpose of dissecting GLP-1 biology by enabling the suppression of its physiological effects.

Research Significance

The use of Imapextide provides researchers with a powerful pharmacological tool to explore:

• Mechanisms of hypoglycemia caused by excess insulin release.

• The cross-talk between insulin and glucagon secretion.

• The role of GLP-1 receptor signaling in metabolic disorders.

• Potential therapeutic strategies for conditions where GLP-1 activity may be detrimental.

Structural Features

• Peptide-based antagonist with structural similarity to endogenous GLP-1.

• Modified to ensure selective receptor blocking activity.

• Provides stability and reproducibility in experimental settings.

Applications in Biomedical Research

1. Hypoglycemia Research

   • By blocking GLP-1’s stimulation of insulin release, Imapextide helps scientists understand how exaggerated incretin responses contribute to low blood sugar episodes.

2. Endocrine Studies

   • Used to delineate the contribution of GLP-1 versus other incretins in pancreatic islet regulation.

   • Helps clarify the interaction between insulin, glucagon, and somatostatin secretion.

3. Metabolic Disease Models

   • Provides a negative control when evaluating GLP-1 agonists and dual agonists.

   • Useful in experiments involving type 2 diabetes progression, obesity, and energy metabolism.

4. Pharmacological Testing

   • Essential for comparative studies of agonist vs antagonist effects.

   • Used to model scenarios of blocked incretin signaling.

Product Specifications

Mechanism of Action

Imapextide functions as a competitive antagonist at the GLP-1 receptor (GLP-1R), a class B G-protein coupled receptor.

GLP-1 Receptor Biology

• GLP-1R location: Pancreatic β-cells, α-cells, CNS, and cardiovascular tissues.

• Normal GLP-1 function: Enhances glucose-dependent insulin secretion, reduces glucagon release, delays gastric emptying, and suppresses appetite.

Antagonist Action of Imapextide

• Binding: Imapextide competes with endogenous GLP-1 and exogenous GLP-1 analogues.

• Signal blockade: Prevents GLP-1-induced cAMP accumulation.

• Downstream effects: Suppresses insulin release and unmasks glucagon secretion, leading to increased plasma glucose levels in experimental systems.

Research Implications

• Hypoglycemia Mechanisms: By blocking incretin-driven insulin release, Imapextide models insulin overproduction syndromes.

• Counter-Regulatory Hormones: Demonstrates the role of GLP-1 in glucagon suppression and highlights how antagonism restores glucagon output.

• Drug Testing: Provides a control for incretin-based therapies (GLP-1R agonists, dual GIP/GLP-1R agonists, GLP-1R/GCGR agonists).

• Neuroendocrine Studies: Since GLP-1R is also expressed in the brain, Imapextide supports research into the central regulation of appetite and autonomic glucose sensing.

  

Side Effects

Although Imapextide is used exclusively for research purposes, its pharmacological profile suggests potential side effects in experimental models:

Metabolic Effects

• Hyperglycemia due to reduced insulin secretion.

• Dysregulated glucagon levels, potentially leading to impaired glucose homeostasis.

Gastrointestinal Effects

• Altered gastric motility due to GLP-1 blockade.

• Possible changes in appetite regulation.

CNS-Related Effects

• GLP-1 signaling in the brain is involved in satiety and stress; antagonism may alter feeding behaviors or stress response pathways.

Laboratory Precautions

• Handle with protective equipment in a laboratory setting.

• Avoid contamination, repeated freeze-thaw, or prolonged exposure to room temperature.

Disclaimer

Imapextide is intended for laboratory research use only. It is not for human administration, diagnostic procedures, or therapeutic purposes.

Keywords

Imapextide, CAS 3004569-93-8, GLP-1 receptor antagonist, incretin biology, hypoglycemia research, pancreatic islet regulation, metabolic disorder model, insulin secretion inhibitor, glucagon regulation, peptide antagonist.

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