1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
    Dopamine Transporter
    Serotonin Transporter
  3. Centanafadine hydrochloride

Centanafadine hydrochloride (Synonyms: EB-1020 hydrochloride)

Cat. No.: HY-16736A Purity: 99.93%
Handling Instructions

Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.

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

Centanafadine hydrochloride Chemical Structure

Centanafadine hydrochloride Chemical Structure

CAS No. : 923981-14-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 226 In-stock
Estimated Time of Arrival: December 31
5 mg USD 205 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
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100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.

IC50 & Target

IC50: 6 nM (human NE), 38 nM (human DA), 83 nM (human serotonin)[1].

In Vitro

Centanafadine (EB-1020) preferentially inhibits monoamine reuptake in cloned cell lines transfected with human transporters with IC50 values of 6 and 38 nM, respectively, for NE and DA transporters, Centanafadine has lesser effects on 5-HT transporter as it inhibits the reuptake of 5-HT with an IC50 value of 83 nM [1].

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

In Vivo

In microdialysis studies, Centanafadine markedly increases NE, and DA concentrations levels in rat prefrontal cortex in vivo with peak increases of 375 and 300%, respectively with the greatest effects on NE, and also increases DA extracellular concentrations in the striatum to 400% of baseline concentrations. Behavioral studies demonstrate that Centanafadine dose-dependently decreases immobility in the mouse tail suspension test of depression to 13% of control levels, and do not stimulate locomotor activity in adult rats in the optimal dose range. Centanafadine dose-dependently inhibits locomotor hyperactivity in juvenile rats lesioned with the neurotoxin 6-hydroxydopamine (100 μg intracisternally) as neonates; a well-established animal model for attention-deficit hyperactivity disorder (ADHD)[1].

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

Clinical Trial
Molecular Weight

245.75

Formula

C₁₅H₁₆ClN

CAS No.

923981-14-0

SMILES

[[email protected]@H]12[[email protected]@](CNC2)(C3=CC(C=CC=C4)=C4C=C3)C1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (508.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0692 mL 20.3459 mL 40.6918 mL
5 mM 0.8138 mL 4.0692 mL 8.1384 mL
10 mM 0.4069 mL 2.0346 mL 4.0692 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: ≥ 2.08 mg/mL (8.46 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (8.46 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (8.46 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

CentanafadineEB-1020EB1020EB 1020Adrenergic ReceptorDopamine TransporterSerotonin TransporterBeta ReceptorDATSLC6A35-HTTSERTSLC6A4Inhibitorinhibitorinhibit

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Product Name:
Centanafadine hydrochloride
Cat. No.:
HY-16736A
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