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 CCK1 receptors are found in high concentrations in the gastrointestinal tract and a few discrete brain regions.

Family:

GPCR

Sub Family:

Cholecystokinin

Class:

Class A

Protein Name:

CCK1 (CCKA)

Uniprot Number:

P32238

Protein Aliases:

CCK-AR|Cholecystokinin-1 receptor|CCK1-R

Gene Name:

CCKAR

Gene ID:

886

Accession Number:

NM_000730

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):

0.24

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

1.5nM - IC50

PubChem ID

443375

Name

Devazepide

Measurement

0.39nM - IC50

PubChem ID

4355450

Name

133040-77-4

Measurement

5600nM - IC50

PubChem ID

Name

CCK-8s

Measurement

0.1nM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Adverse / Beneficial Action:

Cholecystokinin CCK1 receptor agonism may decrease symptoms of constipation predominant IBS and functional dyspepsia.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 1876
Item: 1877
Item: G062
Item: P1
Item: P22-p
Item: P270
Item: P3
Item: P342
Item: P9
Item: P411
Item: P448
Item: P456