Description

Product Description

Octreotide Acetate is a chemically synthesized cyclic octapeptide that mimics the natural hormone somatostatin but exhibits a longer duration of action and higher stability. As a potent somatostatin analogue, it plays a vital role in research related to hormonal secretion, tumor proliferation, and neuroendocrine system regulation.

Octreotide Acetate (CAS 79517-01-4) binds selectively to somatostatin receptors (SSTR2 and SSTR5), producing a strong inhibitory effect on growth hormone, insulin, glucagon, and various gastrointestinal peptides. This makes it an essential tool in studying conditions such as acromegaly, insulinoma, gastrinoma, carcinoid syndrome, and other hormone-secreting tumors.

From a biochemical standpoint, Octreotide’s stability and resistance to enzymatic degradation make it suitable for long-term research experiments. Unlike natural somatostatin, which has a plasma half-life of only 1–3 minutes, Octreotide demonstrates an extended duration, remaining active for hours, thus providing consistent experimental data in endocrine and oncology research.

Structure and Chemical Features

• Molecular Formula: C49H66N10O10S2

• Molecular Weight: 1019.25 g/mol

• Sequence: H-D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-ol (cyclic disulfide bridge between Cys2 and Cys7)

• Form: White to off-white powder

• Solubility: Soluble in water, acetic acid, and DMSO

• Stability: Stable under refrigerated conditions (2–8°C); sensitive to light and moisture

Octreotide Acetate’s design incorporates D-amino acid residues that enhance metabolic stability while maintaining high receptor affinity. Its cyclic disulfide bridge confers conformational rigidity, crucial for receptor specificity.

Applications in Research

1. Endocrine Regulation Studies:
   Octreotide is used to study the inhibitory mechanisms of somatostatin on pituitary and pancreatic hormones, providing insights into hormonal feedback loops and secretion control.

2. Tumor and Cancer Research:
   As a somatostatin analogue, Octreotide suppresses the secretion of hormones and growth factors that promote tumor proliferation, particularly in neuroendocrine tumors, carcinoids, and pituitary adenomas.

3. Gastrointestinal Research:
   Octreotide modulates secretion of gastrointestinal peptides, including gastrin, secretin, and vasoactive intestinal peptide (VIP), helping researchers explore its regulatory influence on digestion and intestinal motility.

4. Receptor Pharmacology:
   Octreotide serves as a model ligand for studying somatostatin receptor binding kinetics, internalization, and signaling pathways.

Pharmacological Research Context

Octreotide’s long-acting inhibitory action is particularly significant in understanding chronic hormone dysregulation models. It demonstrates dose-dependent suppression of growth hormone secretion, while simultaneously reducing insulin and glucagon levels, making it a key molecule in research on diabetes, acromegaly, and hormone-secreting neoplasms.

Furthermore, Octreotide’s antiproliferative properties are of growing interest in oncology research. By binding to SSTR-expressing tumor cells, it inhibits angiogenesis and cell proliferation, highlighting its potential as an investigational agent in tumor biology studies.

Product Specifications

Mechanism of Action

Octreotide Acetate acts as a potent agonist for somatostatin receptors, particularly SSTR2 and SSTR5, which are predominantly expressed in endocrine and neuroendocrine cells. Upon receptor binding, Octreotide activates intracellular inhibitory G-proteins (Gi/o), leading to a cascade of downstream effects.

1. Hormone Inhibition Pathway

Octreotide inhibits adenylate cyclase activity, resulting in decreased cyclic AMP (cAMP) levels. This suppression leads to reduced secretion of growth hormone (GH), thyroid-stimulating hormone (TSH), insulin, glucagon, and gastrointestinal peptides such as gastrin and VIP.

2. Ion Channel Modulation

Octreotide reduces calcium influx and increases potassium efflux in endocrine cells, stabilizing the membrane potential and diminishing the stimulus-secretion coupling necessary for hormone release.

3. Antiproliferative and Antiangiogenic Effects

By binding to SSTRs expressed on tumor cells, Octreotide downregulates mitogenic signaling pathways such as PI3K/Akt and MAPK, reducing cell proliferation. It also inhibits vascular endothelial growth factor (VEGF), limiting tumor angiogenesis — a critical aspect of its use in neuroendocrine tumor research.

4. Neuroendocrine Regulation

Octreotide modulates neuronal hormone release, making it valuable in studying central neuropeptide signaling, stress hormone modulation, and the cross-regulation of hypothalamic-pituitary axes.

Side Effects

In laboratory and experimental studies, Octreotide has been observed to cause several dose-related physiological changes:

1. Gastrointestinal Effects:
   Altered gut motility and mild digestive suppression due to inhibition of pancreatic and intestinal hormones.

2. Metabolic Effects:
   Possible fluctuations in glucose metabolism resulting from altered insulin and glucagon levels.

3. Local Reactions:
   Transient irritation at the injection site in animal models, consistent with peptide administration.

4. Gallbladder Function:
   Inhibition of cholecystokinin release may affect bile secretion, offering insights into gastrointestinal hormone regulation models.

5. Endocrine System Adaptation:
   Chronic exposure may lead to compensatory hormonal feedback mechanisms — an area of active research for long-term peptide regulation.

All observed effects are consistent with Octreotide’s known pharmacodynamics and contribute valuable data for understanding peptide-based hormonal control systems.

Keywords

Octreotide Acetate; CAS 79517-01-4; Somatostatin analogue; Growth hormone inhibitor; Endocrine research peptide; Tumor research peptide; Neuroendocrine peptide; High purity peptide; Research peptide manufacturer; OEM peptide production.

Shipping Guarantee

All shipments are handled using validated cold-chain logistics to preserve peptide integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.

Trade Assurance

We ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.

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Disclaimer

This product is intended for laboratory research use only. It is not for human or veterinary use, nor for diagnostic or therapeutic applications. Researchers should handle this compound in accordance with institutional safety procedures and applicable regulations.