B2 Human Bradykinin GPCR Binding Agonist Radioligand LeadHunter Assay - FR

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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.

Family:

GPCR

Sub Family:

Bradykinin

Class:

Class A

Protein Name:

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

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]bradykinin

Ligand Kd (nM):

0.32

Ligand Concentration:

0.3 nM

Non Specific:

1 µM Bradykinin

Incubation:

60 min at RT

Control Inhibitor:

Npc 567

Test Concentration / Dose:

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

Test Sample Requirements:

Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final 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:

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

119343

Name

Npc 567

Measurement

9.1nM - IC50

PubChem ID

439201

Name

Bradykinin

Measurement

0.41nM - IC50

PubChem ID

Name

[d(CH2)51,Tyr(Me)2]-AVP

Measurement

0.43nM - IC50

PubChem ID

105044

Name

desArg9-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