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:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

20 min at 37°C

Control Inhibitor:

SHU 9119

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

70691332

Name

SHU 9119

Measurement

0.7nM - 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:

Taiwan - Taipei

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