ETA 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:

ETA

Uniprot Number:

P25101

Protein Aliases:

ET-A|ET-AR

Gene Name:

EDNRA

Gene ID:

1909

Accession Number:

NM_001957

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):

0.03

Ligand Concentration:

0.03 nM

Non Specific:

100 nM Endothelin-1

Incubation:

120 min at 37°C

Control Inhibitor:

Endothelin-1

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

0.038nM - IC50

PubChem ID

101675604

Name

BQ-788

Measurement

10350nM - IC50

PubChem ID

Name

Endothelin-3

Measurement

6nM - IC50

PubChem ID

Name

Sarafotoxin S6c

Measurement

462nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

ETA receptor agonism may cause vasoconstriction, positive inotropy and facilitate cell proliferation (e.g., smooth muscle, mesangial cells).

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault