ELA-14 (human) TFA

Modify Date: 2024-01-14 17:10:12

ELA-14 (human) TFA structure	Common Name	ELA-14 (human) TFA
	CAS Number	1886973-05-2	Molecular Weight	1707.03
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₇₅H₁₁₉N₂₅O₁₇S₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of ELA-14 (human) TFA

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].

Name	Elabela(19-32)

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.