CCK2 (CCKB) Human Cholecystokinin GPCR Cell Based Agonist & Antagonist IP1 LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
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. CCK₂ receptor agonism may enhance anxiety and gastric acid secretion. CCK₂ receptor antagonism may impair memory.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
CCK2 (CCKB) Human Cholecystokinin GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
309940-0
Protein
CCK2 (CCKB)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CCK2 (CCKB) Human Cholecystokinin GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item
309940-1
Protein
CCK2 (CCKB)
Organism
Human
Assay Sub Type
Cell Based
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:
Full Length, Recombinant
Cell Type:
1321N1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant cholecystokinin CCK₂ receptor-expressing 1321-N1 cells are used. Test compound or vehicle is incubated with the cells in stimulation buffer of IP-One-Gq kit for 30 minutes at 37°C. The reaction is evaluated for IP₁ levels by TR-FRET. Test compound-induced increase of IP₁ production by 50 percent or more (≥50%) relative to the 1 µM Gastrin I response indicates possible CCK₂ receptor agonist activity. Test compound inhibits the 5 nM Gastrin I-induced response in IP₁ levels by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
30 min at 37°C
Control Inhibitor:
L-365260
Control Activator:
Gastrin I
Criteria For Significance:
≥ 50% increase in IP-one relative to Gastrin I response, ≥ 50% inhibition of Gastrin I-induced response
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Adverse / Beneficial Action:
CCK2 receptor agonism may enhance anxiety and gastric acid secretion. CCK2 receptor antagonism may impair memory.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
CCK2 (CCKB) Human Cholecystokinin GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item: 309940-0
CCK2 (CCKB) Human Cholecystokinin GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item: 309940-1
CCK2 (CCKB) Human Cholecystokinin GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item: 218130
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