ELA-14 (human) TFA

Names

[ Name ]:
ELA-14 (human) TFA

Biological Activity

[Description]:

Elabela(19-32) is a potent apelin receptor (APJ) endogenous agonist with a Ki of 0.93 nM. Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

[Target]

Ki: 0.93 nM (APJ)[1] IC50: 8.6 nM (Gαi1) and 166 nM (β-arrestin-2)[1]

[In Vitro]

Elabela(19-32) (analogue 3) has an EC50 of 36 nM in HEK293 cells transiently expressing the HA-hAPJ receptor. Elabela(19-32) is slightly less potent than apelin-13 and ELA to elicit receptor internalization[1]. Elabela(19-32) (0.001 to 0.3 nM) has an EC50 of 1.5 pM in inducing changes in left ventricular developed pressure (LVDP) on the Langendorff perfused isolated rat heart[1].

[In Vivo]

Elabela(19-32) (analogue 3) is rapidly metabolized in rat plasma (t1/2<2 min)[1].

[References]

[1]. Peiran Yang, et al. Elabela/Toddler Is an Endogenous Agonist of the Apelin APJ Receptor in the Adult Cardiovascular System, and Exogenous Administration of the Peptide Compensates for the Downregulation of Its Expression in Pulmonary Arterial Hypertension. Circulation. 2017 Mar 21;135(12):1160-1173.

[2]. Alexandre Murza, et al. Discovery and Structure-Activity Relationship of a Bioactive Fragment of ELABELA That Modulates Vascular and Cardiac Functions. J Med Chem. 2016 Apr 14;59(7):2962-72.

Chemical & Physical Properties

[ Molecular Formula ]:
C₇₅H₁₁₉N₂₅O₁₇S₂

[ Molecular Weight ]:
1707.03