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

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

HTRF

Testing Information

Incubation:

10 min at 37°C

Control Activator:

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 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

896

Name

Melatonin

Measurement

0.055nM - EC50

PubChem ID

115348

Name

2-iodomelatonin

Measurement

0.09nM - EC50

PubChem ID

4172142

Name

IIK7

Measurement

0.11nM - EC50

PubChem ID

Name

GR 135531

Measurement

- EC50

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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