MT2 Human Melatonin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Melatonin 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. Melatonin, present primarily in the central nervous system, is released following a circadian rhythm with high levels at night.
Family:
GPCR
Sub Family:
Melatonin
Class:
Class A
Protein Name:
MT2
Uniprot Number:
P49286
Protein Aliases:
Mel1b receptor
Gene Name:
MTNR1B
Gene ID:
4544
Accession Number:
XM_017017777
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[125I]2-iodomelatonin
Ligand Kd (nM):
0.085
Ligand Concentration:
0.05 nM
Non Specific:
1 µM Melatonin
Incubation:
120 min at 37°C
Control Inhibitor:
melatonin
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:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Adverse / Beneficial Action:
Melatonin MT2 receptor agonism may result in a phase change in circadian rhythms, cause vasodilation and inhibit pain transmission.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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