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

Cell Type:

SK-N-MC

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Activator:

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: 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

16178853

Name

143113-45-5

Measurement

- EC50

PubChem ID

44284481

Name

Endothelin-1

Measurement

1nM - EC50

PubChem ID

Name

Endothelin-3

Measurement

- EC50

PubChem ID

Name

Sarafotoxin S6c

Measurement

- EC50

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

RELATED SOLUTIONS

Item: 54
Item: 2257
Item: G067
Item: P347
Item: P458-EU
Item: P460-EU