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.
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:
Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Incubation:
30 min at 37°C
Control Inhibitor:
WIN 64338
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
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