Cat. No.: HY-A0144

Etilefrine

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Etilefrine is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output.

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Pureté: 97.03%
CAS No.: 709-55-7
Formule: C₁₀H₁₅NO₂
Masse moléculaire:181.23

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Etilefrine Chemical Structure

CAS No.: 709-55-7

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

AMPK

Voir tous les produits spécifiques à Isoform Adrenergic Receptor :

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform AMPK :

In Vitro

Etilefrine (10 μM; 1-2 h) significantly activates AMPKα (Thr172) phosphorylation and inhibits Akt (Ser473) phosphorylation in PC-3 and 293T cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

PC-3 (human prostate cancer), 293T (human embryonic kidney)
Concentration:

5, 10, 50 μM
Incubation Time:

1 h or 2 h
Result:

Increased phosphorylated AMPKα (Thr172) by 1.5-2.0 fold and decreased phosphorylated Akt (Ser473) by 0.2-0.4 fold compared to controls, indicating AMPK activation and Akt inhibition in both cell lines.

In Vivo

Etilefrine (0.1 mg/kg; intravenous injection; single dose) causes an increase in blood pressure and heart rate in anesthetized mongrel dog models, which may be related to the constriction of resistance vessels and the increase in cardiac contractility and heart rate^[2].
Etilefrine (50 μg/kg, 200 μg/kg; intravenous injection; single dose) can increase cardiac output, right heart filling pressure and blood pressure at rest and reduce total peripheral resistance in New Zealand white rabbit experimental models. Total peripheral resistance increased at a dose of 200 μg/kg^[3].

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

Animal Model:

New Zealand white rabbits (male, 3.0-4.1 kg), resting cardiovascular function model^[3]
Dosage:

50 μg/kg, 200 μg/kg Etilefrine
Administration:

Intravenous injection, single dose, acute experiment
Result:

At 50 μg/kg, increased right heart filling pressure (RHFP), cardiac output (CO), and blood pressure (BP), reduced total peripheral resistance (TPR), and caused bradycardia.
At 200 μg/kg, it increased RHFP, BP, and TPR, while CO showed a minor decrease, indicating mixed α and β adrenoceptor-mediated effects.

Animal Model:

Anesthetized mongrel dogs (8.5-14 kg), postural hypotension model induced by hexamethonium and 30° tilt^[2]
Dosage:

0.1 mg/kg Etilefrine
Administration:

Intravenous injection, single dose, acute experiment
Result:

Significantly increased basal blood pressure (BP) and heart rate (HR). During tilt, it did not attenuate the decrease in systolic, diastolic, or mean BP, but tended to increase cardiac output (CO) without significant attenuation of tilt-induced CO reduction.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 709-55-7
Appearance Solid
Masse moléculaire 181.23
Formule C₁₀H₁₅NO₂
Color Off-white to pink
SMILES

OC(CNCC)C1=CC=CC(O)=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 40 mg/mL (220.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

5.5179 mL

27.5893 mL

55.1785 mL

5 mM

1.1036 mL

5.5179 mL

11.0357 mL

10 mM

0.5518 mL

2.7589 mL

5.5179 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 4 mg/mL (22.07 mM); Clear solution

This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 4 mg/mL (22.07 mM); Clear solution

This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Chi Xu, et al. Accurate Drug Repositioning through Non-tissue-Specific Core Signatures from Cancer Transcriptomes. Cell Rep. 2018 Oct 9;25(2):523-535.e5. [Content Brief]

[2]. R Yamazaki, et al. Effects of dihydroergotamine and Etilefrine on experimentally-induced postural hypotension in dogs. J Pharmacobiodyn. 1990 Sep;13(9):519-24. [Content Brief]

[3]. Adigun SA, et al. A comparison of the effects of salbutamol, etilefrine and dextran during hypotension and low cardiac output states in rabbit. Clin Exp Pharmacol Physiol. 1984 Nov-Dec;11(6):627-43. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1 mM	5.5179 mL	27.5893 mL	55.1785 mL	137.9463 mL
	5 mM	1.1036 mL	5.5179 mL	11.0357 mL	27.5893 mL
	10 mM	0.5518 mL	2.7589 mL	5.5179 mL	13.7946 mL
	15 mM	0.3679 mL	1.8393 mL	3.6786 mL	9.1964 mL
	20 mM	0.2759 mL	1.3795 mL	2.7589 mL	6.8973 mL
	25 mM	0.2207 mL	1.1036 mL	2.2071 mL	5.5179 mL
	30 mM	0.1839 mL	0.9196 mL	1.8393 mL	4.5982 mL
	40 mM	0.1379 mL	0.6897 mL	1.3795 mL	3.4487 mL
	50 mM	0.1104 mL	0.5518 mL	1.1036 mL	2.7589 mL
	60 mM	0.0920 mL	0.4598 mL	0.9196 mL	2.2991 mL
	80 mM	0.0690 mL	0.3449 mL	0.6897 mL	1.7243 mL
	100 mM	0.0552 mL	0.2759 mL	0.5518 mL	1.3795 mL

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Etilefrine

Epigenetics Compound Library

GPCR/G Protein Compound Library

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FDA Kinase Inhibitor Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform Adrenergic Receptor

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform AMPK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Etilefrine Related Classifications

HY-A0144 Related Classifications