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 withOctreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent
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- No. CAS: 252845-37-7
- Fòrmula: C60H74N12O10
- Peso molecular:1123.30
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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SSTR2 37.6 nM (EC50) |
SSTR3 31.3 nM (EC50) |
SSTR4 10.5 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SST4-expressing BON-1 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Inhibited SST4-expressing BON-1 cells, while did not significantly inhibited wild type BON-1 cells.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 252845-37-7
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Peso molecular 1123.30
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Fòrmula C60H74N12O10
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Synonyms
DG3173; PTR-3173
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Dasgupta P, et al. Pharmacological Characterization of Veldoreotide as a Somatostatin Receptor 4 Agonist. Life (Basel). 2021 Oct 12;11(10):1075. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Veldoreotide Related Classifications
HY-P0024 Related Classifications
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