Description

1. Product Description 

Ilatreotide (CAS 119719-11-8), also known as SDZ CO61, is a glycated derivative of somatostatin, engineered to improve pharmacokinetic stability and oral activity while retaining high receptor affinity. Somatostatin is a peptide hormone that inhibits the secretion of multiple endocrine and exocrine hormones, including growth hormone (GH), insulin, glucagon, and gastrointestinal hormones. Glycation enhances its resistance to enzymatic degradation, allowing extended activity in gastrointestinal and pancreatic research models.

Background

Somatostatin analogues have become important tools in both basic research and preclinical oncology, particularly for the study of gastroenteropancreatic neuroendocrine tumors (GEP-NETs). Ilatreotide demonstrates superior potency over native somatostatin and earlier analogs by combining:

• Extended half-life due to glycation.

• Improved oral bioavailability, enabling convenient experimental administration.

• Selective hormone suppression, providing a controlled research environment.

Scientific Relevance

• Endocrine Research: Study of fasting and postprandial hormone regulation.

• Tumor Biology: Research on GEP tumors, including mechanisms of hormone-secreting neoplasms.

• Pharmacological Modeling: Provides a platform for evaluating somatostatin analog pharmacokinetics and dynamics.

• Comparative Analysis: Allows direct comparison with other somatostatin analogues (e.g., octreotide, lanreotide).

Advantages in Research

• High potency glycated analogue with enhanced receptor binding.

• Improved stability and oral activity allow for reproducible dosing in animal models.

• Facilitates exploration of postprandial hormone secretion patterns and feedback regulation.

• GMP-grade quality ensures consistent experimental outcomes.

2. Product Specifications 

3. Mechanism of Action & Research Applications 

Mechanism of Action

Ilatreotide exerts its effects via binding to somatostatin receptors (SSTR1-5) expressed in the gastrointestinal tract, pancreas, and endocrine tissues:

1. Receptor Binding

   • High-affinity binding to SSTR2 and SSTR5.

   • Modulates adenylate cyclase activity, reducing intracellular cAMP.

2. Hormone Suppression

   • Inhibits secretion of gastrin, insulin, glucagon, pancreatic polypeptide, and other gut hormones.

   • Controls both fasting baseline secretion and postprandial hormone release.

3. Signal Modulation

   • Activates inhibitory G-proteins, downregulating hormone exocytosis and cell proliferation pathways in neuroendocrine cells.

Research Applications

1. Gastroenteropancreatic Tumor Models

   • Evaluates inhibitory effects on hormone-producing tumors.

   • Supports pharmacodynamic studies of somatostatin analogues in GEP-NET preclinical models.

2. Endocrine Regulation Studies

   • Investigates feedback loops between gastrointestinal hormones, pancreatic islets, and the hypothalamic-pituitary axis.

   • Assesses postprandial hormonal dynamics in controlled experimental systems.

3. Pharmacokinetic and Pharmacodynamic Research

   • Glycation improves oral absorption and systemic stability, enabling dose-response analysis.

4. Comparative Analogue Studies

   • Comparison with octreotide, lanreotide, and native somatostatin provides insights into receptor selectivity and efficacy.

5. Translational Relevance

   • Provides preclinical data for development of orally active somatostatin analogues for endocrine tumor therapies.

   • Supports research into hormone hypersecretion syndromes, including gastrinoma and insulinoma models.

     

4. Side Effects (Research Reference) 

Experimental observations in preclinical models indicate:

• Endocrine Modulation: Dose-dependent suppression of insulin and glucagon.

• Gastrointestinal Effects: Altered motility and secretion due to somatostatin receptor activation.

• Cardiovascular Influence: Mild bradycardia observed in high-dose rodent studies.

• Metabolic Changes: Potential shifts in glucose homeostasis due to hormone suppression.

• Stability Considerations: Proper lyophilized storage essential to maintain activity.

These findings are strictly for laboratory research reference. Ilatreotide is not approved for human or veterinary use.

5. Disclaimer

For laboratory research use only. Not for human or veterinary use.

6. Keywords

• Ilatreotide

• Ilatreotide CAS 119719-11-8

• SDZ CO61 peptide

• Glycated somatostatin analog

• Gastroenteropancreatic tumor research peptide

• Endocrine regulation research peptide

• GMP supplier Ilatreotide

• Somatostatin receptor agonist peptide

• Oral-active somatostatin analogue

• Laboratory use GEP tumor peptide