Product Description

The VPAC1 receptor (vasoactive intestinal peptide receptor 1) is a class B G protein-coupled receptor encoded by the VIPR1 gene, binding with high affinity to both vasoactive intestinal peptide and pituitary adenylate cyclase-activating polypeptide. It is widely distributed in multiple human tissues including the lungs, liver, intestine, pancreatic ductal epithelium, heart, kidneys, as well as lymphocytes and monocytes. Its core function involves activating Gs proteins to stimulate cAMP production, thereby mediating smooth muscle relaxation (e.g., vascular, bronchial, gastrointestinal), promoting glandular secretion, regulating immune and inflammatory responses, and playing roles in cell proliferation and survival. This receptor holds potential therapeutic value in conditions such as asthma, inflammatory bowel disease, and certain cancers.

ScreeningBio’s HEK293T/Human VPAC1 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.