Melanocortin 4 Receptor (MC4R) ACTOne Stable Cell Line
|
Catalog Number:
CL-01-MC4R
|
|
In Stock
|
Price: Please inquire order@eEnzyme.com
Detailed Description
|
CL-01-MC4R
|
|
Name
|
Melanocortin 4 Receptor (MC4R) ACTOneTM Stable Cell Line
|
|
Description
|
This cell line is a HEK-293-CNG cell line that expresses a recombinant human MC4R. HEK-293-CNG cells express a modified CNG (Cyclic Nucleotide Gated) channel that opens in response to elevated intracellular cAMP levels and consequently result in ion flux and cell membrane depolarization. The assay allows both end-point and kinetic measurement of intracellular cAMP changes with a FLIPR or a fluorescence microplate reader.<
|
|
Application
|
cAMP dependent human MC4R cell-based assay;
cell-based high-throughput screening of human MC4R agonists/antagonists.
|
|
Size
|
1x 106 cells
|
|
Detection
|
FlexStation or Microplate reader
|
|
For Downloading
|
==>> DATA SHEET ==>> MSDS
|
Selected Citation:
Hammad,et al. MC4R Variant rs17782313 Associates With Increased Levels of DNAJC27, Ghrelin, and Visfatin and Correlates With Obesity and Hypertension in a Kuwaiti Cohort. Front. Endocrinol., 07 July 2020
Synonym: Melanocortin 4 Receptor, Melanocortin Receptor 4, MC4-R, Mutant Melanocortin-4 Receptor, BMIQ20
About MC4R and Applications of the ACTOne MC4R Stable Cell Line
Melanocortin 4 Receptor (MC4R) is a Class A G protein-coupled receptor that plays a critical role in regulating appetite, energy expenditure, body weight, and metabolic homeostasis. MC4R is highly expressed in the hypothalamus and serves as a key component of the leptin-melanocortin signaling pathway, which controls food intake and energy balance. Genetic mutations in MC4R represent one of the most common causes of monogenic obesity, making the receptor an important therapeutic target for obesity and metabolic disease research.
Activation of MC4R by endogenous melanocortin peptides, including α-melanocyte-stimulating hormone (α-MSH), stimulates Gs-mediated signaling pathways that increase intracellular cAMP levels. This signaling cascade suppresses appetite and promotes energy expenditure. Because of its central role in body weight regulation, MC4R has become a major target for the development of anti-obesity therapies and metabolic disease treatments.
eEnzyme's ACTOne Human MC4R Stable Cell Line provides a reliable and reproducible platform for MC4R-targeted drug discovery, receptor pharmacology studies, and GPCR screening applications. The cell line enables the evaluation of agonists, antagonists, inverse agonists, and allosteric modulators, supporting receptor characterization, potency determination, lead optimization, and high-throughput compound screening.
The ACTOne MC4R Stable Cell Line is optimized for functional GPCR assays and screening workflows. Its stable receptor expression and robust assay performance make it an ideal tool for studying appetite regulation pathways, obesity-associated signaling mechanisms, and next-generation therapeutics targeting metabolic disorders.
Advantages of eEnzyme's ACTOne MC4R Stable Cell Line
• Stable recombinant human MC4R expression
• Optimized for ACTOne membrane potential assays
• Suitable for agonist and antagonist screening
• Supports high-throughput screening workflows
• Ideal for obesity and metabolic disease drug discovery
• Consistent and reproducible assay performance
MC4R Signaling Pathway
Upon ligand binding, MC4R activates Gs proteins and stimulates adenylate cyclase activity, resulting in elevated intracellular cAMP levels. Increased cAMP signaling contributes to appetite suppression, energy expenditure, and regulation of body weight. Dysregulation of MC4R signaling has been associated with obesity, metabolic syndrome, and rare genetic disorders affecting energy homeostasis, making MC4R an important target for therapeutic development and pharmacological research.
|
|
|