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Request The Product List ofApelin Receptor (APLNR) Apelin Receptor (APLNR)

Apelin is an endogenous ligand of G protein-coupled receptor APJ. Apelin/APJ system is widely expressed in abundant tissues, especially bone, joint and muscle tissue.
Apelin and apelin receptors are expressed in many tissues and organ to regulate their physiological functions. Studies have shown that Apelin/apelin-receptor also expressed in ovary such as follicles, granulosa cells. Furthermore, Apelin/apelin-receptor play roles in vascular establishment and hormone metabolism in ovary.
The apelin receptor (APJ) is a member of the family A of G-protein-coupled receptors (GPCRs) and is involved in range of physiological and pathological functions, including fluid homeostasis, anxiety, and depression, as well as cardiovascular and metabolic disorders.
Therefore, drugs targeting apelin/APJ system undoubtedly provide more therapeutic options, ProbecChem prvided chemical tools for signaling pathways associated with apelin/APJ system. 


1, Nigel A. Chapman, et al. Biochem Cell Biol. 2014 Dec; 92(6): 431-440.
2, Gonghui Hu, et al. Front Physiol. 2021 Feb 10;12:632886.


Cat. No. Product Name Information

APJ agonist 47

Apelin receptor agonist

APJ agonist 47 is a potent and selective, orally active apelin receptor (APJ) agonist EC50 of 6.5 nM.


APLNR agonist

CMF-019 (CMF019) is the first G protein biased small molecule Apelin receptor (APJ, APLNR) agonist, potent benzimidazole-derived apelin peptidomimetic, binds to APLNR with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse APLNR, respectively.


Apelin receptor agonist

BMS-986224 (BMS986224) is a novel potent, selective, orally bioavailable agonist of Apelin receptor (APJ, APLNR) with Ki of 0.074 nM (human APJ).


Apelin receptor agonist

AM-8123 (AM8123) is a small-molecule agonist of Apelin receptor (APJ, APLNR), inhibits forskolin-stimulated cAMP production (pEC50=9.44) and promoted Gα protein activation (pEC50=8.95)..

AMG 986

Apelin receptor agonist

AMG 986 (Azelaprag, AMG986) is a small-molecule agonist of Apelin receptor (APJ, APLNR), inhibits forskolin-stimulated cAMP production (pEC50=9.64) and promoted Gα protein activation (pEC50=9.54).


Apelin receptor antagonist

ML221 is a potent, selective, functional antagonist of apelin receptor (APJ) with IC50 of 1.75 uM in the β-arrestin assay, >37-fold selective over the closely related AT1 receptor.


Apelin receptor agonist

WN561 (WN-561) a potent, selective non-hypertrophic and fully G-protein-biased apelin receptor (APLNR, APJ) agonist, exhibits cardioprotective functions with reduced cardiac hypertrophy.

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