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:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]NDP-alpha -MSH

Ligand Kd (nM):

0.4

Ligand Concentration:

0.075 nM

Non Specific:

1 µM NDP-alpha-MSH

Incubation:

60 min at 37°C

Control Inhibitor:

NDP-alpha-MSH

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:

2

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

92432

Name

Melanotan II

Measurement

3.9nM - IC50

PubChem ID

16131138

Name

Des-acetyl MSH

Measurement

8.8nM - IC50

PubChem ID

44277697

Name

NDP-alpha-MSH

Measurement

0.23nM - IC50

PubChem ID

70691332

Name

SHU 9119

Measurement

0.62nM - IC50

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:

France - Celle L'Evescault

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