Elabela(19-32) TFA 是与 apelin 受体 (APJ) 结合的 ELABELA (ELA) 活性片段。Elabela(19-32) TFA 激活 G_αi1 和 β-arrestin-2 信号通路，EC₅₀ 分别为 8.6 nM 和 166 nM。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。

Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the G αi1 and β-arrestin-2 signaling pathways with EC 50 s 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.

Solid

IC50: 8.6 nM (Gαi1) and 166 nM (β-arrestin-2)

Elabela(19-32) TFA (analogue 3) has a Ki of 0.93 nM for binding of radioligand apelin-13[Glp, Nle, Tyr][I].
Elabela(19-32) TFA 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.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Elabela(19-32) TFA (analogue 3) is rapidly metabolized in rat plasma (t 1/2 <2 min).
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years；-20°C 1 ye

[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.

In Vitro: DMSO : 100 mg/mL (54.91 mM; Need ultrasonic)H₂O : 33.33 mg/mL (18.30 mM; Need ultrasonic)配制储备液