APLNR, active

Background Information:

Early Access Product :
The apelin receptor (APLNR) is a class A GPCR activated by the endogenous peptide ligands apelin and Elabela. It plays central roles in cardiovascular regulation, fluid homeostasis, and embryonic development, including vasculogenesis and heart morphogenesis. Upon ligand binding, APLNR predominantly couples to Gi proteins, leading to inhibition of adenylyl cyclase and modulation of cAMP levels, and also signals through β arrestin pathways, which mediate receptor internalization and contribute to cardiovascular effects. While some studies report downstream PLC activation and calcium mobilization, these are not established as primary signaling mechanisms. APLNR is expressed in various tissues, including the cardiovascular system and central nervous system, where it contributes to the regulation of vascular tone, blood pressure, and angiogenesis. Because of its roles in cardiovascular regulation, APLNR has emerged as an important therapeutic target, with active research into its modulation for conditions such as heart failure, hypertension, ischemic injury, and potentially metabolic dysfunction.
Our recombinant full‑length APLNR is produced in a eukaryotic expression system to preserve native folding and essential post‑translational modifications. The purified wild‑type receptor remains structurally and functionally intact, providing a high‑quality reagent for biochemical, structural, and pharmacological studies, including ligand screening, antibody discovery, and mechanistic investigations.

Target Class:

GPCR

Sub Family:

Class A

Protein Name:

APLNR

Protein Aliases:

AGTRL1; APJ

UniProt Number:

P35414

Gene Name:

APLNR

Gene ID:

187

Gene Aliases:

APJ; APJR; HG11; AGTRL1

Target Species:

Human