Product Description

Parathyroid hormone receptor 1 (PTH1R) is the primary class B G protein-coupled receptor mediating the actions of parathyroid hormone, mainly distributed in the kidneys and bones (osteoblasts and osteocytes), serving as the central target for calcium and phosphate metabolism. Its core function, through activation of multiple pathways including Gs/cAMP and Gq/PKC, is to promote calcium reabsorption and inhibit phosphate reabsorption in the kidneys, while dually regulating bone resorption and formation (depending on the mode of action) in bone, thereby jointly maintaining blood calcium homeostasis and bone metabolic balance. Abnormalities in this receptor are directly linked to various bone metabolic disorders (e.g., osteoporosis, hyperparathyroidism) and genetic diseases (e.g., Jansen's metaphyseal chondrodysplasia).

ScreeningBio’s HEK293T/Rat PTH1 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.