Bioactivity | 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 (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent[1] |
Invitro | 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Veldoreotide TFA 相关抗体: Cell Viability Assay[1] Cell Line: |
CAS | 2126831-23-8 |
Formula | C62H75F3N12O12 |
Molar Mass | 1237.33 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |