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

Centanafadine 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.

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Centanafadine

Centanafadine Estructura química

No. CAS : 924012-43-1

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solid
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Descripciòn

Centanafadine 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].

MedChemExpress (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].

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

Ensayo clínico
Peso molecular

209.29

Fòrmula

C15H15N

No. CAS
Appearance

Solid

Color

White to off-white

SMILES

[C@@H]12[C@@](CNC2)(C3=CC(C=CC=C4)=C4C=C3)C1

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvente y solubilidad
In Vitro: 

DMSO : 125 mg/mL (597.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.7781 mL 23.8903 mL 47.7806 mL
5 mM 0.9556 mL 4.7781 mL 9.5561 mL
View the Complete Stock Solution Preparation Table

* 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculadora de molaridad

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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Referencias

Complete Stock Solution Preparation Table

* 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 (protect from light). 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 4.7781 mL 23.8903 mL 47.7806 mL 119.4515 mL
5 mM 0.9556 mL 4.7781 mL 9.5561 mL 23.8903 mL
10 mM 0.4778 mL 2.3890 mL 4.7781 mL 11.9451 mL
15 mM 0.3185 mL 1.5927 mL 3.1854 mL 7.9634 mL
20 mM 0.2389 mL 1.1945 mL 2.3890 mL 5.9726 mL
25 mM 0.1911 mL 0.9556 mL 1.9112 mL 4.7781 mL
30 mM 0.1593 mL 0.7963 mL 1.5927 mL 3.9817 mL
40 mM 0.1195 mL 0.5973 mL 1.1945 mL 2.9863 mL
50 mM 0.0956 mL 0.4778 mL 0.9556 mL 2.3890 mL
60 mM 0.0796 mL 0.3982 mL 0.7963 mL 1.9909 mL
80 mM 0.0597 mL 0.2986 mL 0.5973 mL 1.4931 mL
100 mM 0.0478 mL 0.2389 mL 0.4778 mL 1.1945 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
Centanafadine
Cat. No.:
HY-16736
Cantidad:
MCE Japan Authorized Agent: