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

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at 37°C

Control Inhibitor:

SHU 9119

Control Activator:

NDP-alpha -MSH (1 nM)

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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

70691332

Name

SHU 9119

Measurement

0.5nM - IC50

PubChem ID

Name

AGRP (83-132)

Measurement

1.8nM - IC50

PubChem ID

Name

HBS024

Measurement

1.1nM - IC50

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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