ETB Human Endothelin GPCR Binding Agonist Radioligand LeadHunter Assay - FR

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Endothelin 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. Endothelin receptors are widely expressed in all tissues, ETA receptors primarily on vascular smooth muscles and ETB receptors primarily on endothelial cells. Receptors are also localized to non-vascular structures such as epithelial cells and in central nervous system glia and neurones.

Family:

GPCR

Sub Family:

Endothelin

Class:

Class A

Protein Name:

ETB

Uniprot Number:

P24530

Protein Aliases:

ET-BR|Endothelin receptor non-selective type

Gene Name:

EDNRB

Gene ID:

1910

Gene Aliases:

ETB

Accession Number:

NM_000115

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]endothelin-1

Ligand Kd (nM):

0.04

Ligand Concentration:

0.03 nM

Non Specific:

0.1 µM Endothelin-1

Incubation:

120 min at 37°C

Control Inhibitor:

endothelin-3

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

44284481

Name

Endothelin-1

Measurement

0.13nM - IC50

PubChem ID

101675604

Name

BQ-788

Measurement

37nM - IC50

PubChem ID

Name

Endothelin-3

Measurement

0.03nM - IC50

PubChem ID

Name

Sarafotoxin S6c

Measurement

0.17nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

ETB receptor agonism may cause initial vasodepression through release of NO, vasoconstriction in some vascular beds, bronchoconstriction and facilitate cell proliferation (e.g., astrocytes).

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault