Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the G_αi1 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.

Elabela(19-32) (analogue 3) has a K_i of 0.93 nM for binding of radioligand apelin-13[Glp⁶⁵, Nle⁷⁵, Tyr⁷⁷][¹²⁵I].
Elabela(19-32) 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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Elabela(19-32) (analogue 3) is rapidly metabolized in rat plasma (t_1/2<2 min).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Elabela(19-32) (analogue 3) is rapidly metabolized in rat plasma (t_1/2<2 min).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . 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.  [Content Brief]