Biological Information | |
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Background Information: | The PathHunter® CALCR-RAMP2(AMY2) eXpress kit provides an easy-to-use cell based assay to study drug candidates (small molecules or biologics) targeting GPCRs. This kit assesses ligand (e.g. calcitonin, amylin) based activation of CALCR GPCR activity via detection of β-arrestin recruitment. This product uses EFC technology. The cells included overexpress PK-tagged CALCR and EA-tagged β-Arrestin-2, along with untagged modulating protein RAMP2. Activation of CALCR stimulates the recruitment of β-Arrestin-2 and produces EFC signal. eXpress kits are a convenient, ready-to-use format which contains all materials needed to run the assay, including single-use vials of cryopreserved cells, cell plating media, detection reagent, and assay plates.
Both calcitonin and amylin activate amylin receptors (AMY1, AMY2, AMY3). Amylin, a 37-amino acid peptide hormone, is primarily synthesized in pancreatic beta cells and co-secreted with insulin in response to ingested nutrients. Amylin receptors are GPCRs composed of two units: a core unit formed by the calcitonin receptor (a 7-transmembrane receptor) and one of three receptor activity-modifying proteins (RAMP1-3). Dual amylin and calcitonin receptor agonists have shown significant efficacy in promoting body weight loss, enhancing glucose tolerance, and reducing fat accumulation in liver tissue. Moreover, Amylin and GLP-1R agonists are believed to function via comparable yet distinct mechanisms, particularly in regulating appetite. Consequently, Amylin-based therapeutics exhibit promising potential in combating obesity. |
Target Class: | GPCR |
Family: | Calcitonin Receptor |
Sub Family: | Class B |
Coupling: | Gs |
Accession Number: | NM_001742.2 |
Target Name: | CALCR-RAMP2(AMY2) |
Target Aliases: | Calcitonin receptor, CRT, CT-R, CTR, CTR1, Amylin receptor 2, AMY2 |
Target Species: | Human |
Cell Background: | CHO-K1 |
Usage | |
Product Type: | eXpress Assay Kits |
Application: | Drug Discovery & Development |
Storage Conditions: | Store in vapor phase of liquid nitrogen. |
Usage Disclaimer: | Ready-to-use eXpress assay kits are intended for in vitro research purposes only. These kits are not suitable for lot release applications. Refer to the ready-to-use bioassay kit format for potency testing in lot release for biologic therapeutics. These products may be covered by issued US and/or foreign patents, patent applications and subject to a Limited Use Label License. Please visit discoverx.com/license for a list of products that are governed by limited use label license terms and relevant patent and trademark information. |
Assay Information | |
Assay Type: | Functional |
β-Arrestin isoform: | β-Arrestin-2 |
Assay Measures: | β-Arrestin Recruitment |
Detection Method: | Chemiluminescence |
Additional Information | |
Brand: | PathHunter® |
PathHunter® eXpress CALCR-RAMP2 (AMY2) CHO-K1 β-Arrestin GPCR Assay
User Manuals & Protocols
70-255 PathHunter B Arrestin eXpress GPCR Assay REV4 User Manual
View DocumentDatasheets
93-0267E2_PathHunter_eXpress CALCR-RAMP2 CHO-K1 beta-Arrestin GPCR Assay
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