Apelin Receptors

(Glp1)-Apelin-13 is an activator of Apelin Receptor

Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions.

MM 07 is a biased apelin receptor agonist, with a KD of 300 nM in CHO-K1 cells and a KD of 172 nM in human heart.

ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.

CMF019 is a potent and small molecule agonist at Apelin receptor (APJ) with G protein bias.

Azelaprag (Example 263.0) is an apelin receptor agonist drug candidate.

ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways.