sst4 Human Somatostatin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Somatostatin (SS) is a neurotransmitter/hormone with a wide range of biological actions. Somatostatin mediates its diverse physiological effects through a family of five G-protein-coupled receptors (sst1-sst5). A reduction in cortical SS levels has been reported in Alzheimer’s and Parkinson’s diseases.
Family:
GPCR
Sub Family:
Somatostatin
Class:
Class A
Protein Name:
sst4
Uniprot Number:
P31391
Protein Aliases:
SS4-R|SS4R
Gene Name:
SSTR4
Gene ID:
6754
Accession Number:
NM_001052
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[125I]Tyr11-somatostatin-14
Ligand Kd (nM):
5.9
Ligand Concentration:
0.1 nM
Non Specific:
1 µM Somatostatin-14
Incubation:
120 min at RT
Control Inhibitor:
Somatostatin-14
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 µl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
2
Turnaround Time
Standard:
10 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Gastroenterology
Adverse / Beneficial Action:
A reduction in cortical SS levels has been reported in Alzheimers and Parkinsons diseases. The SS analog, octreotide (SMS 201995), is used clinically in the treatment of certain tumors, carcinoid syndrome, and glucagonoma. Somatostatin inhibits cell proliferation and growth hormone secretion. Somatostatin released from capsaicin-sensitive afferents exerts systemic anti-nociceptive actions, presumably via somatostatin receptor subtype 4 (sst4).
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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