Elabela(19-32)

Elabela(19-32); 纯度: 98.10%

Elabela(19-32) 是与 apelin 受体 (APJ) 结合的 ELABELA (ELA) 活性片段。Elabela(19-32) 激活 Gαi1β-arrestin-2 信号通路,EC50 分别为 8.6 nM 和 166 nM。Elabela(19-32) 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)amp;;

Elabela(19-32) Chemical Structure

CAS No. : 1886973-05-2

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Elabela(19-32) 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

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].

IC50 Target

IC50: 8.6 nM (Gαi1) and 166 nM (β-arrestin-2)[1]

体外研究
(In Vitro)

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].

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

体内研究
(In Vivo)

Elabela(19-32) (analogue 3) is rapidly metabolized in rat plasma (t1/2<2 min)[1].

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

分子量

1707.03

Formula

C75H119N25O17S2

CAS 号

1886973-05-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : 100 mg/mL (58.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5858 mL 2.9291 mL 5.8581 mL
5 mM 0.1172 mL 0.5858 mL 1.1716 mL
10 mM 0.0586 mL 0.2929 mL 0.5858 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [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.