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.
PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.
Family:
GPCR
Sub Family:
Melanocortin
Class:
Class A
Coupling:
Gs
Protein Name:
MC5
Uniprot Number:
P33032
Protein Aliases:
MC-2
Gene Name:
MC5R
Gene ID:
4161
Accession Number:
NM_005913
Organism:
Human
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
β-Arrestin Isoform:
β-Arrestin-2
Testing Information
Control Inhibitor:
HS024
Control Activator:
Melanotan II
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:
Melanocortin MC5 receptor agonism may increase lachrymal and sebaceous gland secretion.
Additional Information
Brand:
LeadHunter
Testing Location:
USA - Fremont, CA