MC4 Human Melanocortin GPCR Cell Based Agonist & Antagonist cAMP LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
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.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
MC4 Human Melanocortin GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
332270-0
Protein
MC4
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
MC4 Human Melanocortin GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
Item
332270-1
Protein
MC4
Organism
Human
Assay Sub Type
Cell Based
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:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant melanocortin MC4 receptor expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (2.5 x 10^5/ml) in modified HBSS pH 7.4 buffer at 37°C for 20 minutes. The reaction is evaluated for cAMP levels by TR-FRET. Test compound-induced cAMP increase by 50 percent or more (≥50%) relative to the 3 μM NDP-a-MSH control response indicates possible receptor agonist activity. Test compound-induced inhibition of the 10 nM NDP-a-MSH induced cAMP response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
20 min at 37°C
Control Inhibitor:
SHU 9119
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
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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MC4 Human Melanocortin GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
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MC4 Human Melanocortin GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
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