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
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
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