Biological Information

Background Information:

Melanocortins belong to the superfamily of seven transmembrane G-protein-coupled receptors, which 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:

MC1

Uniprot Number:

Q01726 (human)

Protein Aliases:

alpha melanocyte stimulating hormone receptor

Gene Name:

MC1R

Gene ID:

4157

Gene Aliases:

MSH-R|MSHR

Accession Number:

NM_002386

Organism:

Mouse

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):

0.05

Ligand Concentration:

0.05 nM

Non Specific:

1 µM NDP-alpha-MSH

Incubation:

90 min at RT

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:

15 Business Days

Reference Compound Data

PubChem ID

92432

Name

Melanotan II

Measurement

0.2nM - IC50

PubChem ID

16131138

Name

Des-acetyl MSH

Measurement

1.4nM - IC50

PubChem ID

16132265

Name

Corticotropin

Measurement

0.96nM - IC50

PubChem ID

44277697

Name

NDP-alpha-MSH

Measurement

0.18nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Melanocortin MC1 receptor agonism may increase the risk of developing melanoma and nonmelanoma skin cancer beyond their effects on pigmentation phenotype.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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