Biological Information
Background Information:
Cholecystokinin 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. Cholecystokinin CCK2 receptors are widely distributed in the brain, with highest concentrations in the striatum, cerebral cortex and limbic system, but can also be found in the stomach.
Family:
GPCR
Sub Family:
Cholecystokinin
Class:
Class A
Protein Name:
CCK2 (CCKB)
Uniprot Number:
P32239
Protein Aliases:
CCK-BR|Cholecystokinin-2 receptor|CCK2-R
Gene Name:
CCKBR
Gene ID:
887
Gene Aliases:
CCKRB
Accession Number:
NM_176875
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[125I]CCK-8s
Ligand Kd (nM):
0.054
Ligand Concentration:
0.08 nM
Non Specific:
1 µM CCK-8s
Incubation:
60 min at RT
Control Inhibitor:
CCK-8s
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:
CNS/Addiction/Pain
Adverse / Beneficial Action:
Cholecystokinin CCK2 receptor agonism may enhance anxiety and gastric acid secretion while receptor antagonism may impair memory.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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