Elabela(19-32)TFA是一种有效的apelin受体(APJ)内源性激动剂，Ki值为0.93nM。Elabela(19-32)TFA激活Gαi1和β-arrestin-2信号通路，EC50分别为8.6nM和166nM。Elabela(19-32)TFA诱导受体内在化，降低动脉压，对心脏产生正性肌力作用。
货号:ajcx30574
CAS:N/A
分子式:C77H120F3N25O19S2
分子量：1821.05
溶解度:DMSO: 100 mg/mL (54.91 mM); H2O: 33.33 mg/mL (18.30 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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

Elabela(19-32) TFA (analogue 3) has an EC50 of 36 nM in HEK293 cells transiently expressing the HA-hAPJ receptor. Elabela(19-32) TFA is slightly less potent than apelin-13 and ELA to elicit receptor internalization[1]. Elabela(19-32) TFA (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) TFA (analogue 3) is rapidly metabolized in rat plasma (t1/2<2 min)[1].

[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.