MC3 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
MC3 Human Melanocortin GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
332250-0
Protein
MC3
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
MC3 Human Melanocortin GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
Item
332250-1
Protein
MC3
Organism
Human
Assay Sub Type
Cell Based
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 & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant melanocortin MC₃ receptor expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (1.5 x 10⁵/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 10 μM NDP-α-MSH control response indicates possible receptor agonist activity. Test compound-induced inhibition of the 10 nM NDP-α-MSH induced cAMP response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
20 min at 37°C
Control Inhibitor:
AGRP (83-132)
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 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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MC3 Human Melanocortin GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
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MC3 Human Melanocortin GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
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