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:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Incubation:
20 min at 37°C
Control Activator:
NDP-alpha-MSH
Criteria For Significance:
≥ 50% increase in cAMP relative to NDP-alpha-MSH response, ≥ 50% Inhibition of NDP-alpha-MSH-induced cAMP response
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 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:
Taiwan - Taipei
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