[CAS NO. ] Elabela(19-32) TFA

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PRODUCTS SPECIFICATIONS

Catalog

HY-P2106A

Brand

MCE

CAS

-

DESCRIPTION

Overview

MDL	-
Molecular Weight	1821.05
Molecular Formula	C77H120F3N25O19S2
SMILES	-

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

3 Publications Citing Use of MCE

Summary

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 EC ₅₀ s 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 & Target

IC50: 8.6 nM (G _αi1 ) and 166 nM (β-arrestin-2) ^[1]

In Vitro

Elabela(19-32) TFA (analogue 3) has a K _i of 0.93 nM for binding of radioligand apelin-13[Glp ⁶⁵ , Nle ⁷⁵ , Tyr ⁷⁷ ][ ¹²⁵ I] ^[1] .
Elabela(19-32) TFA has an EC ₅₀ 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 EC ₅₀ 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.

In Vivo

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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light, under nitrogen

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, under nitrogen)

Solvent & Solubility

In Vitro:

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

H ₂ O : 33.33 mg/mL ( 18.30 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (1.37 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (1.37 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.

References

[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.