Elabela(19-32)

• CAT Number: I015137
• CAS Number: 1886973-05-2
• Molecular Formula: C75H119N25O17S2
• Molecular Weight: 1707.03
• Purity: ≥95%

Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). 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].
Elabela(19-32) (analogue 3) has a Ki of 0.93 nM for binding of radioligand apelin-13[Glp65, Nle75, Tyr77][125I][1]. ?
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[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].
Elabela(19-32) (analogue 3) is rapidly metabolized in rat plasma (t1/2<2 min)[1].

Reference

[1]. 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.
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