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:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

20 min at 37°C

Control Activator:

NDP-alpha-MSH

Criteria For Significance:

≥ 50% increase in cAMP relative to NDP-alpha-MSH response, ≥ 50% Inhibition of NDP-alpha-MSH-induced cAMP response

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

16

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

16131138

Name

Des-acetyl MSH

Measurement

0.2μM - EC50

PubChem ID

44277697

Name

NDP-alpha-MSH

Measurement

0.001μM - EC50

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:

Taiwan - Taipei

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