1. GPCR/G Protein
  2. Arrestin Apelin Receptor (APJ)
  3. Elabela(19-32)

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.

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Elabela(19-32)

Elabela(19-32) Estructura química

No. CAS : 1886973-05-2

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Revisión del cliente

Based on 6 publication(s) in Google Scholar

Other Forms of Elabela(19-32):

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Descripciòn

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]

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].

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

In Vivo

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

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

Peso molecular

1707.03

Fòrmula

C75H119N25O17S2

No. CAS
Appearance

Solid

Color

White to off-white

Sequence

{Glp}-Arg-Arg-Cys-Met-Pro-Leu-His-Ser-Arg-Val-Pro-Phe-Pro

Sequence Shortening

{Glp}-RRCMPLHSRVPFP

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

Solvente y solubilidad
In Vitro: 

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

DMSO : 25 mg/mL (14.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (29.29 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Pureza y Documentación
Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 0.5858 mL 2.9291 mL 5.8581 mL 14.6453 mL
5 mM 0.1172 mL 0.5858 mL 1.1716 mL 2.9291 mL
10 mM 0.0586 mL 0.2929 mL 0.5858 mL 1.4645 mL
H2O 15 mM 0.0391 mL 0.1953 mL 0.3905 mL 0.9764 mL
20 mM 0.0293 mL 0.1465 mL 0.2929 mL 0.7323 mL
25 mM 0.0234 mL 0.1172 mL 0.2343 mL 0.5858 mL
30 mM 0.0195 mL 0.0976 mL 0.1953 mL 0.4882 mL
40 mM 0.0146 mL 0.0732 mL 0.1465 mL 0.3661 mL
50 mM 0.0117 mL 0.0586 mL 0.1172 mL 0.2929 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Inquiry Information

Nombre del producto:
Elabela(19-32)
Cat. No.:
HY-P2106
Cantidad:
MCE Japan Authorized Agent: