Centanafadine (EB-1020) |
| Catalog No.GC31283 |
La centanafadine (EB-1020) est un double inhibiteur du transporteur de la noradrénaline (NE)/dopamine (DA), inhibe également le transporteur de la sérotonine, avec des IC50 de 6 nM, 38 nM et 83 nM pour le NE humain, le DA et le transporteur de la sérotonine, respectivement.
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Cas No.: 924012-43-1
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
[1]. Bymaster FP, et al. Pharmacological characterization of the norepinephrine and dopamine reuptake inhibitor EB-1020: implications for treatment of attention-deficit hyperactivity disorder. Synapse. 2012 Jun;66(6):522-32.
| Cas No. | 924012-43-1 | SDF | |
| Canonical SMILES | [C@@H]12[C@@](CNC2)(C3=CC(C=CC=C4)=C4C=C3)C1 | ||
| Formula | C15H15N | M.Wt | 209.29 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
| 10 mM | 0.4778 mL | 2.389 mL | 4.7781 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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