Veldoreotide TFA

Veldoreotide (DG3173) TFA a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide TFA inhibits growth hormone (GH) secretion in adenomas compared with Octreotide . Veldoreotide has the potential to be used as pain modulating agent

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].

References:
[1]. Dasgupta P, et al. Pharmacological Characterization of Veldoreotide as a Somatostatin Receptor 4 Agonist. Life (Basel). 2021 Oct 12;11(10):1075.
[2]. Plöckinger U, et al. DG3173 (somatoprim), a unique somatostatin receptor subtypes 2-, 4- and 5-selective analogue, effectively reduces GH secretion in human GH-secreting pituitary adenomas even in Octreotide non-responsive tumours. Eur J Endocrinol. 2012 Feb;166(2):223-34.