| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
IC50: 8.6 nM (Gαi1) and 166 nM (β-arrestin-2)[1]
Apelin receptor (APJ/APLNR); a Class A GPCR; functions as an endogenous agonist, activating Galphai1 and beta-arrestin-2 signaling pathways. |
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| 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].
Elabela(19-32) TFA is a potent APJ endogenous agonist with a Ki of 0.93 nM. It activates Galphai1 (EC50=8.6 nM) and beta-arrestin-2 (EC50=166 nM). It induces receptor internalization, reduces arterial pressure, and exerts positive inotropic effects on the heart. |
| ln Vivo |
In rat plasma, elasta(19–32) TFA (analogue 3) is quickly digested (t1/2<2 min)[1].
Elabela(19-32) TFA (0.001-0.3 nM) induces changes in left ventricular developed pressure (LVDP) on the Langendorff perfused isolated rat heart with an EC50 of 1.5 pM. It rapidly reduces arterial blood pressure and has positive inotropic effects when administered intravenously in rats. |
| Enzyme Assay |
APJ receptor binding affinity (Ki=0.93 nM) is assessed by competitive radioligand binding assays using [125I]-apelin-13 and membranes from HEK293 cells expressing human APJ; unlabeled Elabela(19-32) TFA competes for binding; non-specific binding is determined with excess unlabeled peptide.
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| Cell Assay |
HEK293 cells transiently expressing HA-hAPJ receptor are treated with Elabela(19-32) TFA (1 pM-1 microM); Galphai1 activation is measured by GTPgammaS binding or BRET; beta-arrestin-2 recruitment is measured by BRET; receptor internalization is assessed by confocal microscopy of fluorescently tagged APJ.
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| Animal Protocol |
Sprague-Dawley rats: Elabela(19-32) TFA is administered intravenously (0.1-10 nmol/kg); blood pressure is measured via carotid artery catheter; cardiac function (LVDP) is assessed in Langendorff isolated perfused heart preparation. Alternatively, rats are dosed for pharmacokinetic studies (t1/2 <2 min in rat plasma).
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| ADME/Pharmacokinetics |
Elabela(19-32) TFA is rapidly metabolized in rat plasma with a half-life of less than 2 minutes, indicating very short systemic exposure. Rapid clearance is typical for small peptides due to proteolytic degradation.
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| Toxicity/Toxicokinetics |
No dedicated toxicity studies available; as a 14-amino acid peptide, Elabela(19-32) TFA is expected to have low toxicity at physiological doses. For research use only, not intended for human administration.
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| References | |
| Additional Infomation |
Elabela(19-32) TFA is a research-grade peptide tool for studying APJ receptor biology, cardiovascular function, and hypertension. It has no clinical trial status or marketing approval as a therapeutic agent. For research use only.
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| Molecular Formula |
C77H120F3N25O19S2
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|---|---|
| Molecular Weight |
1821.05
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| Related CAS # |
Elabela(19-32);1886973-05-2
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~54.91 mM)
H2O :~33.33 mg/mL (~18.30 mM) |
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| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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