Biological Information
Background Information:
Melanocortins 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. 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:
MC4
Uniprot Number:
P32245
Gene Name:
MC4R
Gene ID:
4160
Accession Number:
NM_005912
Organism:
Human
Construct Details:
Recombinant
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):
0.54
Ligand Concentration:
0.05 nM
Non Specific:
1 µM NDP-alpha -MSH
Incubation:
120 min at 37°C
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:
10 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Adverse / Beneficial Action:
Melanocortin MC4 receptor agonism may decrease body fat and attenuate cachexia while receptor antagonism may result in obesity and Type II diabetes.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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