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:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

HOE140

Control Activator:

bradykinin (0.03 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 70 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

119343

Name

Npc 567

Measurement

23000nM - IC50

PubChem ID

5312119

Name

bradyzide

Measurement

13000nM - IC50

PubChem ID

122130213

Name

HOE140

Measurement

21nM - IC50

PubChem ID

Name

LysdesArg9[Leu8]-BK

Measurement

- IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

Bradykinin B2 receptor agonism may facilitate algesia, cough, bronchoconstriction, inflammation and vasodilation. Bradykinin B2 receptor antagonism may find therapeutic use in the treatment of chronic pain and inflammation.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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