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 tissue and within the central nervous system.

Family:

GPCR

Sub Family:

Bradykinin

Class:

Class A

Protein Name:

B1

Uniprot Number:

P46663

Protein Aliases:

BK-1 receptor

Gene Name:

BDKRB1

Gene ID:

623

Gene Aliases:

BKR1|B1BKR|bradyb1

Accession Number:

NM_000710

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]desArg10-KD

Ligand Kd (nM):

2

Ligand Concentration:

2 nM

Non Specific:

10 µM DesArg9[Leu8]-BK

Incubation:

120 min at RT

Control Inhibitor:

desArg10-KD

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:

2

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

123884

Name

desArg9[Leu8]-BK

Measurement

298nM - IC50

PubChem ID

122227

Name

desArg10-KD

Measurement

0.4nM - IC50

PubChem ID

105044

Name

desArg9-BK

Measurement

471nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

Bradykinin B1 receptor agonism may facilitate cough, algesia, inflammation and vasodilation. Bradykinin B1 receptor antagonism may find therapeutic use in the treatment of chronic pain and inflammation.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 1108
Item: 1109
Item: G055
Item: P9