Veldoreotide

Veldoreotide (DG3173) a somatostatin analogue, that can bind to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent[1]

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor

Research Areas >> Endocrinology

SSTR2:37.6 ± 4.5 nM (EC50)

SSTR3:31.3 ± 14. nM (EC50)

SSTR4:10.5 ± 3.4 nM (EC50)

Veldoreotide stimulates the SST2, SST4, and SST5 receptors with high potency and efficacy in the HEK293 cells, co-expressing these receptors with the GIRK2 channels; EC50s of 37.6 ± 4.5 nM, 31.3 ± 14.4 nM and 10.5 ± 3.4 nM for GIRK2-SST2, GIRK2-SST4 and GIRK2-SST5, respectively[1]. Veldoreotide (10 μM; 24 h) inhibits SST4-expressing BON-1 cells[1]. Veldoreotide (DG3173) (100 nM or 1 μM; 6 h) inhibits GH secreation in adenomas with an IC50 of 0.49 nM[2]. Cell Proliferation Assay[1] Cell Line: SST4-expressing BON-1 cells Concentration: 10 μM Incubation Time: 24 h Result: Inhibited SST4-expressing BON-1 cells, while did not significantly inhibited wild type BON-1 cells.