Description

Veldoreotide (Somatoprim, DG3173; CAS 252845-37-7) is a novel cyclic somatostatin analogue distinguished by its ability to simultaneously activate somatostatin receptor subtypes SSTR2, SSTR4, and SSTR5. Synthesized under GMP-compliant protocols, this peptide offers high stability and purity. It mimics the inhibitory role of native somatostatin while expanding receptor scope—particularly to SSTR4, where it displays remarkable efficacy and potency.

Pharmacologically, veldoreotide performs as a full agonist at SSTR4 (E??? ~99.5%), significantly outperforming traditional analogues like octreotide and pasireotide, which have limited SSTR4 activity. It also activates SSTR2 and SSTR5 with high efficacy (E??? ~98.4–96.9%). In functional assays, veldoreotide reduces chromogranin A secretion in SSTR4-expressing cells more effectively (65.3% reduction) than via SSTR2 and SSTR5 pathways. It also inhibits proliferation in neuroendocrine BON-1 cells via SSTR4, showing stronger cell growth suppression than native somatostatin.

A key translational advantage is veldoreotide’s capacity to suppress growth hormone (GH) secretion even in Octreotide-nonresponsive pituitary adenomas, positioning it as a compelling alternative in acromegaly research and endocrine therapeutics.

Product Specifications

Mechanism of Action & Research Applications

Veldoreotide functions as a broad-spectrum somatostatin receptor agonist, delivering potent activation of SSTR2, SSTR4, and SSTR5. This unique triple-receptor affinity enables versatile biological responses. As a full agonist at SSTR4, veldoreotide uniquely suppresses chromogranin A secretion and cell proliferation—with superior efficacy over endogenous somatostatin. Via SSTR2 and SSTR5 activation, it effectively diminishes GH secretion, even in pituitary adenomas that fail to respond to octreotide.

Research Applications include:

• Acromegaly and GH Regulation: Evaluate suppression of GH secretion in cell and tissue models, including Octreotide-resistant adenomas.

• Receptor-Specific Signaling: Compare receptor subtype functions—study downstream pathways (cAMP, ERK, cell proliferation) mediated by SSTR2/4/5 activation.

• Neuroendocrine Tumor Biology: Inhibit chromogranin A release and tumor cell proliferation via SSTR4—explore implications in neuroendocrine tumor control.

• Pain Modulation Research: Investigate veldoreotide’s potential in reducing inflammatory or nociceptive responses via SSTR pathways (noted potential, mechanistic studies encouraged).

  

Development & Formulation Notes

Veldoreotide is supplied as lyophilized peptide, optimized for stability. For experimental work:

• Reconstitution: Dissolve in DMSO to prepare concentrated stock solutions (e.g., 1–5 mM). Dilute appropriately in aqueous buffer prior to use.

• Aliquoting: Dispense single-use aliquots and store at –80 °C to preserve activity through repeat experiments.

• Assay Design: Use stepwise receptor assay protocols to distinguish functional engagement of SSTR2, SSTR4, and SSTR5. Include cell-based functional readouts for GH release, chromogranin A assays, or proliferation in BON-1/NEN cell lines.

• Signal Specificity: Employ receptor-selective antagonists to confirm veldoreotide’s receptor-mediated effects.

Keywords

Veldoreotide; Somatoprim; DG3173; somatostatin analogue; SSTR2 agonist; SSTR4 agonist; SSTR5 agonist; GH suppression; acromegaly research; pain modulation peptide; GMP peptide; CAS 252845-37-7; hedge receptor agonist.