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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $32 | In Stock | In Stock | |
| 5 mg | $77 | In Stock | In Stock | |
| 10 mg | $128 | In Stock | In Stock | |
| 25 mg | $257 | In Stock | In Stock | |
| 50 mg | $413 | In Stock | In Stock | |
| 100 mg | $648 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $86 | In Stock | In Stock |
| 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. |
| Synonyms | EB-1020 hydrochloride |
| Molecular Weight | 245.75 |
| Formula | C15H16ClN |
| Cas No. | 923981-14-0 |
| Smiles | Cl.C1[C@@H]2CNC[C@]12c1ccc2ccccc2c1 |
| Relative Density. | no data available |
| Storage | Powder: -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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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