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

PubChem ID

16130995

Name

4-Tyr-Bombesin

Measurement

0.68nM - IC50

PubChem ID

53481579

Name

Neuromedin B

Measurement

140nM - IC50

PubChem ID

Name

GRP

Measurement

0.041nM - IC50

PubChem ID

10056636

Name

ICI 216,140

Measurement

50nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 1915
Item: 1916
Item: G053