Elabela(19-32) TFA is the active fragment of ELABELA (ELA) that binds to the apelin receptor (APJ). Elabela(19-32) TFA activates Gαi1 and β-arrestin-2 signaling pathways with EC50 of 8.6 nM and 166 nM respectively. Elabela(19-32) TFA induces receptor internalization, reduces arterial pressure, and produces positive inotropic effects on the heart.

Physicochemical Properties

Molecular Formula	C77H120F3N25O19S2
Molecular Weight	1821.05
Related CAS #	Elabela(19-32);1886973-05-2
Appearance	White to off-white solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	IC50: 8.6 nM (Gαi1) and 166 nM (β-arrestin-2)[1]
ln Vitro	Elabela (ages 19–32) TFA (analogue 3) binds radioligand apelin-13 [Glp65, Nle75, Tyr77] with a Ki of 0.93 nM.[125I][1]. When HA-hAPJ receptor is transiently expressed in HEK293 cells, Elabela(19-32) TFA exhibits an EC50 of 36 nM. In comparison to apelin-13 and ELA, eabela(19-32) TFA has a marginally lower potency to induce receptor internalization[1]. Inducing variations in left ventricular developed pressure (LVDP) on the Langendorff perfused isolated rat heart, Elabela (19-32) TFA (0.001 to 0.3 nM) has an EC50 of 1.5 pM[1].
ln Vivo	In rat plasma, elasta(19–32) TFA (analogue 3) is quickly digested (t1/2<2 min)[1].
References	[1]. 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.

Solubility Data

Solubility (In Vitro)

DMSO :~100 mg/mL (~54.91 mM) H2O :~33.33 mg/mL (~18.30 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (1.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (1.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.5491 mL	2.7457 mL	5.4913 mL
	5 mM	0.1098 mL	0.5491 mL	1.0983 mL
	10 mM	0.0549 mL	0.2746 mL	0.5491 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.