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 Orphan GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. This assay measures intracellular cAMP using TR-FRET technology.

Family:

GPCR

Sub Family:

Melanocortin

Class:

Class A

Coupling:

Gs

Protein Name:

mMC4R

Uniprot Number:

P56450

Protein Aliases:

MC4R|MC4-R

Gene Name:

Mc4r

Gene ID:

17202

Gene Aliases:

FatBoy|Pkcp

Accession Number:

NM_016977.1

Organism:

Mouse

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

β-Arrestin Isoform:

β-Arrestin-2

Testing Information

Control Inhibitor:

 

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 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:

USA - Fremont, CA