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

PubChem ID

9832172

Name

WIN64338

Measurement

0.69µM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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