Reboxetine mesylate
Based on 2 publication(s) in Google Scholar
Reboxetine mesylate (FCE20124 mesylate) is a potent, selective, and specific noradrenaline reuptake inhibitor (NARI) for the research of depression. Reboxetine mesylate inhibits the uptake of norepinephrine, with a Ki of 8 nM.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 98769-84-7
- Formula: C20H27NO6S
- Molecular Weight:409.50
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Reboxetine mesylate
MoreAll Adrenergic Receptor Isoforms
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Biological Activity
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α adrenergic receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.005 μM
Compound: Reboxetine
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Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586
Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586
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[PMID: 34112854] |
Reboxetine mesylate has weak affinity for muscarinic, histaminergic H1, adrenergic α1, and dopaminergic D2 receptors[1].
Reboxetine mesylate preventes the Dexamethasone-induced decreases in cell viability and proliferation rate[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells
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Concentration:0.1 μM, 1 μM, 5 μM
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Incubation Time:24 hours
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Result:Prevented the Dexamethasone-induced decreases in cell viability and proliferation rate.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Harlan-bred, male CF-1 mice (18-20 g), depression models[1]
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Dosage:3 mg/kg, 30 mg/kg
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Administration:Intraperitoneal injection
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Result:Significantly decreased the immobility time in the mouse tail suspension test at the dose of 30 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 98769-84-7
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Appearance Solid
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Molecular Weight 409.50
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Formula C20H27NO6S
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Color White to off-white
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SMILES
CS(=O)(O)=O.CCOC1=C(O[C@]([H])(C2=CC=CC=C2)[C@]3(CNCCO3)[H])C=CC=C1
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Synonyms
FCE20124 mesylate; PNU155950E mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Med
2019 Sep;25(9):1428-1441. PMID: 31501614 -
Behav Brain Res
Manipulation of vocal communication and anxiety through pharmacologic modulation of norepinephrine in the Pink1-/- rat model of Parkinson disease. [Abstract]2022 Feb 10:418:113642. PMID: 34755639
Solvent & Solubility
DMSO : 100 mg/mL (244.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (122.10 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (12.21 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (12.21 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 110 mg/mL (268.62 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Wong, E.H., et al., Reboxetine: a pharmacologically potent, selective, and specific norepinephrine reuptake inhibitor. Biol Psychiatry, 2000. 47(9): p. 818-29. [Content Brief]
[2]. Versiani, M., et al., Reboxetine, a unique selective NRI, prevents relapse and recurrence in long-term treatment of major depressive disorder. J Clin Psychiatry, 1999. 60(6): p. 400-6. [Content Brief]
[3]. M Leskiewicz, et al. Antidepressants attenuate the dexamethasone-induced decrease in viability and proliferation of human neuroblastoma SH-SY5Y cells: a involvement of extracellular regulated kinase (ERK1/2). Neurochem Int. 2013 Nov;63(5):354-62. [Content Brief]
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.4420 mL | 12.2100 mL | 24.4200 mL | 61.0501 mL |
| 5 mM | 0.4884 mL | 2.4420 mL | 4.8840 mL | 12.2100 mL | |
| 10 mM | 0.2442 mL | 1.2210 mL | 2.4420 mL | 6.1050 mL | |
| 15 mM | 0.1628 mL | 0.8140 mL | 1.6280 mL | 4.0700 mL | |
| 20 mM | 0.1221 mL | 0.6105 mL | 1.2210 mL | 3.0525 mL | |
| 25 mM | 0.0977 mL | 0.4884 mL | 0.9768 mL | 2.4420 mL | |
| 30 mM | 0.0814 mL | 0.4070 mL | 0.8140 mL | 2.0350 mL | |
| 40 mM | 0.0611 mL | 0.3053 mL | 0.6105 mL | 1.5263 mL | |
| 50 mM | 0.0488 mL | 0.2442 mL | 0.4884 mL | 1.2210 mL | |
| 60 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0175 mL | |
| 80 mM | 0.0305 mL | 0.1526 mL | 0.3053 mL | 0.7631 mL | |
| 100 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6105 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.