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.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
ETB Human Endothelin GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
1762
Protein
ETB
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
ETB Human Endothelin GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
1763
Protein
ETB
Organism
Human
Assay Sub Type
Cell Based
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
Organism:
Human
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist & Antagonist
Detection Method:
Fluorimetry
Measured Response:
Fluorescence
Testing Information
Incubation:
RT
Control Activator:
endothelin-1 (1 nM)
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
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
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