Biological Information
Background Information:
Melanocortins belong to the superfamily of seven transmembrane G-protein-coupled receptors, which 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. The melanocortin MC1 receptor is made primarily in melanocytes, MC2 in adrenal cortex, MC3 and MC4 almost exclusively neuronal, and MC5 in exocrine gland cells.
Family:
GPCR
Sub Family:
Melanocortin
Class:
Class A
Protein Name:
MC1
Uniprot Number:
Q01726 (human)
Protein Aliases:
alpha melanocyte stimulating hormone receptor
Gene Name:
MC1R
Gene ID:
4157
Gene Aliases:
MSH-R|MSHR
Accession Number:
NM_002386
Organism:
Mouse
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[125I]NDP-alpha -MSH
Ligand Kd (nM):
0.05
Ligand Concentration:
0.05 nM
Non Specific:
1 µM NDP-alpha-MSH
Incubation:
90 min at RT
Control Inhibitor:
NDP-alpha-MSH
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
Therapeutic Area:
Oncology/Immuno-Oncology
Adverse / Beneficial Action:
Melanocortin MC1 receptor agonism may increase the risk of developing melanoma and nonmelanoma skin cancer beyond their effects on pigmentation phenotype.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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