B2 Human Bradykinin GPCR Cell Based Agonist & Antagonist IP1 LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Bradykinin 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. Bradykinin receptors are found in most peripheral tissues and within the central nervous system. Bradykinin B2 receptor agonism may promote algesia, cough, bronchoconstriction, inflammation and vasodilation. Bradykinin B2 receptor antagonism may find therapeutic use in the treatment of chronic pain and inflammation.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
B2 Human Bradykinin GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
305610-0
Protein
B2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
B2 Human Bradykinin GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item
305610-1
Protein
B2
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Sub Family:
Bradykinin
Class:
Class A
Protein Name:
B2
Uniprot Number:
P30411
Protein Aliases:
BK-2 receptor
Gene Name:
BDKRB2
Gene ID:
624
Gene Aliases:
BK-2|BKR2
Accession Number:
NM_000623
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
Chem-1
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 bradykinin B2 receptors expressed in Chem-1 cells are used. Test compound and/or vehicle is incubated with the cells (7.5 x 10^5 /ml) in the stimulation buffer from the IP1 Tb kit for 30 minutes at 37°C. A test compound-induced increase of fluorescence by 50 percent or more (≥50%) relative to the 10 μM bradykinin response indicates possible bradykinin B2 receptor agonist activity. A test compound-induced inhibition of the 2 nM bradykinin-induced increase of fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
30 min at 37ºC
Control Inhibitor:
WIN 64338
Control Activator:
Bradykinin
Criteria For Significance:
≥ 50% increase in IP-one relative to bradykinin response, ≥ 50% Inhibition of bradykinin-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:
Inflammation/Allergy
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
B2 Human Bradykinin GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item: 305610-0
B2 Human Bradykinin GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item: 305610-1
B2 Human Bradykinin GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item: 212620
Questions? Contact Us
You can easily get in touch with a Eurofins Discovery Expert or get help from our Customer Service team. Reach out with questions, or to discuss your specific discovery challenges.
