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 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].

IC50: 8.6 nM (G_αi1) and 166 nM (β-arrestin-2)^[1]

Elabela(19-32) TFA (analogue 3) has a K_i of 0.93 nM for binding of radioligand apelin-13[Glp⁶⁵, Nle⁷⁵, Tyr⁷⁷][¹²⁵I]^[1].
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^[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].

MCE 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)^[1].

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

1821.05

C₇₇H₁₂₀F₃N₂₅O₁₉S₂

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

In Vitro: 

DMSO : 100 mg/mL (54.91 mM; Need ultrasonic)

H₂O : 33.33 mg/mL (18.30 mM; Need ultrasonic)

*

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 (sealed storage, away from moisture and light)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (1.37 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (1.37 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (1.37 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (1.37 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (1.37 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (1.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.