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 central nervous system, is released following a circadian rhythm with high levels at night.. It is also a highly potent antioxidative substance, reducing the damage caused by free radicals generated by light and beta-amyloid peptide.
cAMP Hunter™ Gi cell lines overexpress naturally Gi coupled, wild type GPCRs and are designed to detect inhibition of intracellular cAMP production in response to agonist stimulation of the receptor. These cell lines are designed to be used in conjunction with the HitHunter® cAMP Assay Detection Kit.
Family:
GPCR
Sub Family:
Melatonin
Class:
Class A
Coupling:
Gi/Go
Protein Name:
MT1
Uniprot Number:
P48039
Protein Aliases:
Mel1a receptor
Gene Name:
MTNR1A
Gene ID:
4543
Gene Aliases:
MEL-1A-R
Accession Number:
NM_005958
Organism:
Human
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
Testing Information
Control Activator:
2-iodomelatonin
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 10 concentrations are selected
Test Sample Requirements:
40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)
Minimum Order Quantity:
20
Turnaround Time
Standard:
15 Business Days
Clinical Relevance
Adverse / Beneficial Action:
Melatonin MT1 receptor agonist is of potential therapeutic interest for the treatment of insomnia and circadian rhythm disruption and may be of benefit for the treatment on Alzheimers disease.
Additional Information
Brand:
LeadHunter
Testing Location:
USA - Fremont, CA