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Centanafadine hydrochloride

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Catalog No. T10758LCas No. 923981-14-0
Alias EB-1020 hydrochloride

Centanafadine hydrochloride (EB-1020 hydrochloride) is a dual inhibitor of norepinephrine (NE)/dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter).

Centanafadine hydrochloride

Centanafadine hydrochloride

🥰Excellent
Purity: 99.65%
Catalog No. T10758LAlias EB-1020 hydrochlorideCas No. 923981-14-0
Centanafadine hydrochloride (EB-1020 hydrochloride) is a dual inhibitor of norepinephrine (NE)/dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$32In StockIn Stock
5 mg$77In StockIn Stock
10 mg$128In StockIn Stock
25 mg$257In StockIn Stock
50 mg$413In StockIn Stock
100 mg$648In StockIn Stock
1 mL x 10 mM (in DMSO)$86In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.65%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Centanafadine hydrochloride (EB-1020 hydrochloride) is a dual inhibitor of norepinephrine (NE)/dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter).
Targets&IC50
5-HT:83 nM(human), Norepinephrine:6 nM (human), Dopamine:38 nM (human)
In vitro
Centanafadine (EB-1020) preferentially inhibits monoamine reuptake in cloned cell lines transfected with human transporters, with IC50 values of 6 nM for NE and 38 nM for DA transporters. It has a lesser effect on the 5-HT transporter, inhibiting 5-HT reuptake with an IC50 of 83 nM.
In vivo
In microdialysis studies, Centanafadine significantly increases NE and DA concentrations in the rat prefrontal cortex in vivo, with peak increases of 375% and 300%, respectively, showing the greatest effects on NE. It also raises DA extracellular concentrations in the striatum to 400% of baseline levels. Centanafadine dose-dependently reduces immobility in the mouse tail suspension test of depression to 13% of control levels without stimulating locomotor activity in adult rats at the optimal dose range. Additionally, it dose-dependently inhibits locomotor hyperactivity in juvenile rats lesioned with the neurotoxin 6-hydroxydopamine (100 μg intracisternal) as neonates.
SynonymsEB-1020 hydrochloride
Chemical Properties
Molecular Weight245.75
FormulaC15H16ClN
Cas No.923981-14-0
SmilesCl.C1[C@@H]2CNC[C@]12c1ccc2ccccc2c1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 125 mg/mL (508.65 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (16.28 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM4.0692 mL20.3459 mL40.6918 mL203.4588 mL
5 mM0.8138 mL4.0692 mL8.1384 mL40.6918 mL
10 mM0.4069 mL2.0346 mL4.0692 mL20.3459 mL
20 mM0.2035 mL1.0173 mL2.0346 mL10.1729 mL
50 mM0.0814 mL0.4069 mL0.8138 mL4.0692 mL
100 mM0.0407 mL0.2035 mL0.4069 mL2.0346 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
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Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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