| Field | Specification |
|---|---|
| Alternative names | EB-1020 hydrochloride |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C15H16ClN |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Centanafadine hydrochloride is a dual inhibitor of the norepinephrine (NE) and dopamine (DA) transporters that also inhibits the serotonin transporter, with IC50 values of 6 nM, 38 nM and 83 nM at the human NE, DA and serotonin transporter, respectively. Also known as EB-1020 hydrochloride, it is supplied as a white to off-white solid (C15H16ClN, MW 245.75) at 99.55% purity.
Physical & Chemical Properties
| CAS Number | 923981-14-0 |
|---|---|
| Molecular Formula | C15H16ClN |
| Molecular Weight | 245.75 g/mol |
| Purity | 99.55% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | [C@@H]12[C@@](CNC2)(C3=CC(C=CC=C4)=C4C=C3)C1.Cl |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Solubility | In Vitro: DMSO: 125 mg/mL (508.65 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 6 nM (human NE), 38 nM (human DA), 83 nM (human serotonin)[1].
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 125 mg/mL (508.65 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (8.46 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (8.46 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (8.46 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Centanafadine (EB-1020) preferentially blocks monoamine reuptake in human transporter-transfected cloned cell lines, with IC50 values of 6 and 38 nM for the NE and DA transporters, respectively. Its effect on the 5-HT transporter is smaller, with 5-HT reuptake inhibited at an IC50 value of 83 nM[1].
In Vivo
Microdialysis studies show that Centanafadine markedly raises NE and DA concentrations in vivo in the rat prefrontal cortex, peaking at increases of 375 and 300%, respectively, with NE showing the largest effect. It also raises extracellular DA concentrations in the striatum to 400% of baseline. In behavioral studies, Centanafadine reduces immobility to 13% of control levels in a dose-dependent manner in the mouse tail suspension test of depression, and does not stimulate locomotor activity in adult rats within the optimal dose range. Centanafadine also inhibits locomotor hyperactivity dose-dependently in juvenile rats lesioned as neonates with the neurotoxin 6-hydroxydopamine (100 μg intracisternally), a well-established animal model for attention-deficit hyperactivity disorder (ADHD)[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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