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

PubChem ID

122077

Name

Lintitript

Measurement

103nM - IC50

PubChem ID

443375

Name

Devazepide

Measurement

190nM - IC50

PubChem ID

4355450

Name

133040-77-4

Measurement

24nM - IC50

PubChem ID

Name

CCK-8s

Measurement

0.098nM - IC50

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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