| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Targets |
Centanafadine targets the norepinephrine transporter (NET), dopamine transporter (DAT), and serotonin transporter (SERT). It acts as a reuptake inhibitor, blocking the transport of these monoamines from the synaptic cleft back into presynaptic neurons. By increasing the extracellular concentrations of NE, DA, and serotonin, Centanafadine modulates neurotransmission in brain regions involved in attention, motivation, and mood regulation.
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| ln Vitro |
Centanafadine (EB-1020) has IC50 values of 6 and 38 nM for NE and DA transporters, respectively, and preferentially inhibits monoamine reuptake in clonal cell lines transfected with human transporters. For 5-HT transporters, centanafadine has a less significant effect. Due to its ability to prevent monoamine reuptake, it is small. In 5-HT, 83 nM is the IC50 value [1].
In vitro, Centanafadine preferentially inhibits monoamine reuptake in cloned cell lines transfected with human transporters. It exhibits IC50 values of 6 nM for NE transporter, 38 nM for DA transporter, and 83 nM for serotonin transporter. The compound shows lesser effects on the serotonin transporter compared to NE and DA transporters. These in vitro studies characterize the compound's potency and selectivity profile for monoamine transporters. |
| ln Vivo |
Centanafadine dramatically raised the levels of NE and DA concentration in the rat prefrontal cortex in vivo in microdialysis tests. The highest effect was seen for NE, with peak increases of 375% and 300%, respectively. Additionally, centanafadine enhanced the extracellular levels of DA in the striatum. To 400% of the baseline, the concentration was raised. Based on behavioral tests, centanafadine does not promote locomotor activity in adult rats within the optimal dose range, and it dose-dependently reduces immobility in mice to 13% of control levels in the depressed tail-suspension test. In neonatal rats harmed by the neurotoxin 6-hydroxydopamine (100 μg intracisternally), centanafadine dose-dependently decreases locomotor hyperactivity; this is a well-established animal model of attention deficit hyperactivity disorder (ADHD) [1].
In vivo, microdialysis studies in rats demonstrate that Centanafadine markedly increases NE and DA concentrations in the rat prefrontal cortex, with peak increases of 375% and 300%, respectively. It also increases DA extracellular concentrations in the striatum to 400% of baseline levels. Behavioral studies show that Centanafadine dose-dependently decreases immobility in the mouse tail suspension test of depression, suggesting antidepressant-like activity. |
| Enzyme Assay |
In vitro receptor binding assays for Centanafadine are performed using cloned cell lines transfected with human NET, DAT, and SERT. The compound's ability to inhibit [3H]-monoamine uptake is measured, and IC50 values are calculated from concentration-response curves. These cell-free (or cell-based) assays provide quantitative data on the compound's potency and selectivity for each transporter target.
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| Cell Assay |
In vitro cellular assays for Centanafadine involve measuring monoamine reuptake inhibition in cloned cell lines expressing human transporters. Cells are incubated with the compound and a radiolabeled monoamine (e.g., [3H]-NE, [3H]-DA, or [3H]-serotonin), and the amount of radioactivity taken up into cells is quantified. The IC50 values are determined from inhibition curves, providing a measure of the compound's potency at each transporter.
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| Animal Protocol |
In vivo animal experiments for Centanafadine are conducted in rats and mice. In microdialysis studies, rats are administered the compound and extracellular monoamine concentrations in the prefrontal cortex and striatum are measured. In behavioral studies, mice are subjected to the tail suspension test, and immobility time is recorded as a measure of antidepressant-like activity. These experiments characterize the compound's in vivo neurochemical and behavioral effects.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Centanafadine have been characterized in preclinical studies. The compound has a molecular weight of 209.29 and molecular formula C15H15N. It is supplied as a free base. Further PK studies would be needed to fully characterize its absorption, distribution, metabolism, and excretion profile in vivo.
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| Toxicity/Toxicokinetics |
Toxicological data for Centanafadine have been evaluated in preclinical studies to support its development for ADHD. As a monoamine reuptake inhibitor, its toxicity profile is likely to include effects on the cardiovascular and central nervous systems. Formal toxicology studies have been conducted to assess its safety. The compound is for research use only and is not approved for clinical use.
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| References | |
| Additional Infomation |
Centanafadine is being investigated in clinical trial NCT02827513 (a phase 1 study investigating the safety, tolerability, food effects, pharmacokinetics, and pharmacodynamics of single and multiple doses of a sustained-release formulation of centanafadine (CTN) in young, healthy subjects).
Centanafadine (EB-1020) is a dual norepinephrine/dopamine transporter inhibitor with additional serotonin transporter activity. It has been investigated as a potential treatment for ADHD. The compound has IC50 values of 6 nM (NE), 38 nM (DA), and 83 nM (serotonin). It is supplied as a research compound with CAS number 924012-43-1, molecular formula C15H15N, and molecular weight 209.29. |
| Molecular Formula |
C₁₅H₁₅N
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|---|---|
| Molecular Weight |
209.29
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| Exact Mass |
209.12
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| CAS # |
924012-43-1
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| Related CAS # |
Centanafadine hydrochloride;923981-14-0
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| PubChem CID |
16095349
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
363.5±11.0 °C at 760 mmHg
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| Flash Point |
187.3±14.7 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.679
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| LogP |
2.74
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
287
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@H]2[C@@]1(CNC2)C3=CC4=CC=CC=C4C=C3
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| InChi Key |
HKHCSWPSUSWGLI-CABCVRRESA-N
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| InChi Code |
InChI=1S/C15H15N/c1-2-4-12-7-13(6-5-11(12)3-1)15-8-14(15)9-16-10-15/h1-7,14,16H,8-10H2/t14-,15+/m1/s1
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| Chemical Name |
(1R,5S)-1-naphthalen-2-yl-3-azabicyclo[3.1.0]hexane
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| Synonyms |
EB-1020 EB 1020 EB1020
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | 2.3890 mL | 4.7781 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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