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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $54 | In Stock | |
5 mg | $128 | In Stock | |
10 mg | $213 | In Stock | |
25 mg | $428 | In Stock | |
50 mg | $688 | In Stock | |
100 mg | $1,080 | In Stock | |
200 mg | $1,450 | In Stock | |
500 mg | $2,160 | In Stock | |
1 mL x 10 mM (in DMSO) | $143 | 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). |
In vitro | Centanafadine (EB-1020) preferentially inhibits monoamine reuptake in cloned cell lines transfected with human transporters (IC50s: 6 and 38 nM), for NE and DA transporters, Centanafadine has lesser effects on 5-HT transporter as it inhibits the reuptake of 5-HT (IC50: 83 nM). |
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. 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 intracisternal) as neonates. |
Alias | EB-1020 hydrochloride |
Molecular Weight | 245.75 |
Formula | C15H16ClN |
Cas No. | 923981-14-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 125 mg/mL (508.65 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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