MC4R Assay(s)

Background Information

MC4R (Melanocortin 4 Receptor) is a G protein-coupled receptor (GPCR) in the CNS that regulates appetite and metabolism by responding to hormones like α-MSH and proteins like AgRP, with genetically validated mutations that cause severe obesity. MC4R is also known to complex with inward rectifying potassium channels, whose potentiation plays a key role in neuronal cell excitability and energy homeostasis.

Family: GPCR
Protein Name: Melanocortin 4 Receptor
Gene Name:MC4R

Organism : Human
Therapeutic Area: Metabolism

Assay Information

Validated Assay(s):cAMP, Calcium flux, Ga15/16, Thallium Flux Assay
Assay type: Cell-based
MethodFluorescence

Instrumentation: FLIPR, Panoptic, Flexstation
Plate Format: 96- or 384-well
Expression: Transient
Cell type: HEK293T

Testing Information

Functional Mode(s): Agonist, Antagonist, Allosteric modulators
Reference compound(s): Setmelanotide

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