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

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at 37°C

Control Activator:

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 finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

16220044

Name

Gastrin tetrapeptide

Measurement

208nM - EC50

PubChem ID

Name

CCK-8s

Measurement

1.4nM - EC50

PubChem ID

Name

CCK-8ns

Measurement

30nM - EC50

PubChem ID

Name

gastrin

Measurement

30nM - EC50

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

RELATED SOLUTIONS

Item: 41
Item: 1879
Item: G063
Item: P458-EU
Item: P459-EU
Item: P460-EU