Background

The Calcitonin Receptor (CALCR) is a GPCR involved in calcium homeostasis and bone metabolism. Activated by calcitonin, it inhibits osteoclast activity, reducing bone resorption and maintaining bone density, while also regulating blood calcium levels. Dysregulation can lead to osteoporosis and Paget's disease.

CALCR neurons in the brain influence long-term control of food intake and body weight regulation. Activation can reduce food intake and body weight without adverse effects, making CALCR a target for obesity treatment. CALCR signals through the Gs protein, increasing cAMP levels, which is key to its role in bone health, calcium regulation, and obesity.

Eurofins DiscoverX's cAMP Hunter™ CALCR Gs cell line provides a robust tool for studying CALCR-targeting drugs, enabling accurate assessment of ligand-based activation and supporting drug discovery for bone diseases and obesity.

Product Highlights
  • Validated CALCR stable cell line
  • Detects intracellular cAMP levels as a response to CALCR activation
  • Wild-type CALCR
  • Suitable for CALCR drug discovery on small and large molecules
  • Designed to be used with HitHunter cAMP Assay Detection kit

Assay Principle

The cAMP Hunter™ CALCR Gs Cell Line overexpresses CALCR. When used in conjunction with the HitHunter® cAMP Assay Detection Kit, it utilizes the natural coupling status of CALCR to Gαs to monitor receptor activation. When CALCR is activated by Calcitonin, a reference agonist for this receptor, it stimulates adenylate cyclase, which in turn enables the production of cAMP. The resulting increase in cellular cAMP levels is measured using a homogeneous, gain-of-signal competitive immunoassay based on Enzyme Fragment Complementation (EFC) technology.

The signal from the assay is directly proportional to the amount of cellular cAMP in the well; i.e., the higher the CALCR activation, the greater the cellular cAMP levels, and the larger the signal produced in the assay.

cAMP CALCR Gs Cell line Assay Principle