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:
MC3
Uniprot Number:
P41968
Gene Name:
MC3R
Gene ID:
4159
Gene Aliases:
MC3
Accession Number:
NM_019888
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 MC3 receptor agonism may be anti-inflammatory while receptor antagonism may enhance disease-associated cachexia.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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