1. Veldoreotide

Veldoreotide (DG3173) a somatostatin analogue, binds 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

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Veldoreotide Chemical Structure

Veldoreotide Chemical Structure

CAS No. : 252845-37-7

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Description

Veldoreotide (DG3173) a somatostatin analogue, binds 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]

IC50 & Target

EC50: 37.6 ± 4.5 nM (GIRK2-SST2); 31.3 ± 14.4 nM (GIRK2-SST4), 10.5 ± 3.4 nM (GIRK2-SST5)[1] IC50: 0.49 nM (GH)[2]

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

1123.30

Formula

C60H74N12O10

CAS No.
SMILES

O=C(N[C@@H](C(N[C@H](C(N[C@@](C(N[C@H](C1=O)CC2=CC=CC=C2)=O)([H])[C@H](O)C)=O)CCCCN)=O)CC3=CNC4=CC=CC=C34)[C@@H](NC([C@@H](NC(CCCNC(CCCN1CC(N)=O)=O)=O)CC5=CC=CC=C5)=O)CC6=CNC7=CC=CC=C67

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Product Name:
Veldoreotide
Cat. No.:
HY-P0024
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