Melanocortin 2 (MC2R, ACTHR) Receptor Reporter Assay System

INDIGO’s Melanocortin 2 (MC2R, ACTHR) receptor assay utilizes proprietary human cells that have been engineered to provide constitutive expression of the Human Melanocortin type 2 Receptor (MC2R, ACTHR). In addition to MC2R Reporter Cells, this kit provides two optimized media for use during cell culture and in diluting the user’s test samples, a reference agonist, Luciferase Detection Reagent, and a cell culture-ready assay plate.

The melanocortin type 2 receptor (MC2R) is one of five members of the Melanocortin receptors (MCR). Unlike other types of MCR, MC2R, also known as the Adrenocorticotropin Hormone Receptor (ACTHR), exclusively binds ACTH and mediates its function in steroidogenesis and the release of cortisol. The melanocortin association protein (MRAP) is required for the transport of MC2R to the cell membrane and for binding ACTH and mediating its response. Familial glucocorticoid deficiency, Cushing’s syndrome and Addison disease are examples of diseases linked to mutations in MC2R or the accessory protein MRAP leading to imbalance in the blood levels of ACTH and cortisol . MC2R is predominantly expressed in the adrenal cortex, but can also be expressed in adipocytes, immune cells and kidneys .

Upon binding of ACTH, MC2R undergoes a conformational change that triggers the activation of stimulatory G (G_s) proteins via an exchange of GDP with GTP, followed by the activation of Protein kinase A and adenylate cyclase, and the production of the second messenger cAMP . Because of the significant role of MC2R in the regulation of cortisol and ACTH, there is an interest in developing therapeutics that modulate this receptor.

Human MC2R Reporter Cells are prepared using INDIGO’s proprietary CryoMite™ process. This cryo-preservation method yields high cell viability post-thaw, and provides the convenience of immediately dispensing healthy, division-competent reporter cells into assay plates. There is no need for intermediate spin-and-wash steps, viability determinations, or cell titer adjustments. [INDIGO Catalog Nos. IB41001]

WARNING This product is not for human or veterinary use.