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Elabela(19-32) TFA 

Cat. No.: HY-P2106A
Handling Instructions

Elabela(19-32) TFA is a potent apelin receptor (APJ) endogenous agonist with a Ki of 0.93 nM. Elabela(19-32) TFA activates the Gαi1 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.

For research use only. We do not sell to patients.

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Elabela(19-32) TFA Chemical Structure

Elabela(19-32) TFA Chemical Structure

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Description

Elabela(19-32) TFA is a potent apelin receptor (APJ) endogenous agonist with a Ki of 0.93 nM. Elabela(19-32) TFA activates the Gαi1 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][2].

IC50 & Target

Ki: 0.93 nM (APJ)[1]
IC50: 8.6 nM (Gαi1) and 166 nM (β-arrestin-2)[1]

In Vitro

Elabela(19-32) TFA (analogue 3) 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].

In Vivo

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

Molecular Weight

1821.05

Formula

C₇₇H₁₂₀F₃N₂₅O₁₉S₂

Sequence

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

Sequence Shortening

{Glp}RRCMPLHSRVPFP

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

Elabela(19-32)OthersapelinreceptorAPJendogenousGαi1β-arrestin-2internalizationarterialpressureinotropicheartInhibitorinhibitorinhibit

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Elabela(19-32) TFA
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HY-P2106A
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