Biological Information
Background Information:
Bombesin receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Bombesin receptors are widely distributed in the central nervous system and peripheral tissues. Bombesin BB2 (gastrin-releasing peptide, GRP) receptor agonism may promote gastric emptying, gastrointestinal transit, insulin secretion, inflammation, cell proliferation and tumors. Receptor antagonism may lead to abnormal social behavior.
Family:
GPCR
Sub Family:
Bombesin
Class:
Class A
Protein Name:
BB2
Uniprot Number:
P30550
Protein Aliases:
bombesin receptor 2
Gene Name:
GRPR
Gene ID:
2925
Gene Aliases:
BB2|BB2R
Accession Number:
NM_005314
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[125I][Tyr4]bombesin
Ligand Kd (nM):
0.04
Ligand Concentration:
0.04 nM
Non Specific:
1 µM Bombesin
Incubation:
60 min at RT
Control Inhibitor:
GRP
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:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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