Product Description

The CRF2 receptor (CRHR2), another subtype of the corticotropin-releasing hormone receptor, exhibits high affinity for the ligands urocortin 1, 2, and 3. Its distribution in the brain differs from CRF1, being concentrated in areas like the lateral septum, hypothalamus, and amygdala; peripherally, it is widely expressed in the heart, skeletal muscle, and gastrointestinal tract. Functionally, the CRF2 receptor is believed to buffer or counteract the excessive stress responses mediated by the CRF1 receptor, contributing to reduced anxiety, suppressed appetite, enhanced cardiac function, and regulated gastrointestinal motility. Consequently, CRF2 receptor agonists are under investigation for treating anxiety disorders and heart failure.

ScreeningBio’s HEK293T/Human CRF2 β-Arrestin cell line is an ideal tool for studying GPCR/β-arrestin interactions. In this system, the GPCR C-terminus is fused to a smallBiT tag, and the β2-arrestin N-terminus is fused to a largeBiT tag. Upon receptor activation, GPCR/β-arrestin interaction brings the two fragments together to reconstitute an active NanoLuc enzyme, which can be quantified using the NanoBiT substrate. This cell line is designed to evaluate a compound’s ability to activate the β-arrestin signaling pathway.