| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Tedatioxetine targets the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) as a triple reuptake inhibitor. It preferentially inhibits serotonin and norepinephrine reuptake. Additionally, it acts as an antagonist at 5-HT₂A, 5-HT₂C, 5-HT₃, and α₁A-adrenergic receptors. This multimodal mechanism is designed to enhance monoaminergic neurotransmission in depression.
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| ln Vitro |
One antidepressant is tetraacetine. It functions as an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors in addition to being a triple reuptake inhibitor [1].
In vitro, Tedatioxetine functions as a triple reuptake inhibitor favoring serotonin and norepinephrine. It acts as an antagonist of 5-HT₂A, 5-HT₂C, 5-HT₃, and α₁A-adrenergic receptors. The compound's activity is assessed in receptor binding and reuptake inhibition assays using cell lines expressing human transporters and receptors. |
| ln Vivo |
In vivo activity data for Tedatioxetine are limited in the published literature. As of 2009, it was in Phase II clinical trials for major depressive disorder. Its multimodal mechanism, combining reuptake inhibition with receptor antagonism, is designed to provide antidepressant efficacy with a favorable side effect profile. Further clinical data are needed to confirm its efficacy.
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| Enzyme Assay |
In vitro receptor binding assays for Tedatioxetine are performed using membrane preparations expressing human 5-HT₂A, 5-HT₂C, 5-HT₃, and α₁A-adrenergic receptors. Radioligand competition binding assays are used to measure the compound's affinity for these receptors. Reuptake inhibition assays are performed using cells expressing human SERT, NET, and DAT to measure inhibition of [³H]-monoamine uptake.
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| Cell Assay |
In vitro cellular assays for Tedatioxetine are performed using cell lines expressing serotonin, norepinephrine, and dopamine transporters. Cells are treated with the compound, and monoamine reuptake is measured using radiolabeled substrates. Receptor antagonist activity is assessed by measuring the compound's ability to inhibit agonist-induced intracellular signaling, such as calcium mobilization or cAMP accumulation.
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| Animal Protocol |
In vivo animal experimental protocols for Tedatioxetine are not extensively documented. As an antidepressant candidate, preclinical studies would typically involve administration to rodent models of depression, such as the forced swim test or tail suspension test. Efficacy would be assessed by measuring immobility time, and pharmacokinetic parameters would be determined from plasma samples.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tedatioxetine hydrobromide have been characterized in preclinical studies. The compound has a molecular weight of 364.34 and molecular formula C₁₈H₂₂BrNS. It is soluble in DMSO (~100 mg/mL). In vivo formulation is soluble at ≥2.5 mg/mL in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline. The compound should be stored as a powder at -20°C for up to 3 years.
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| Toxicity/Toxicokinetics |
Toxicological data for Tedatioxetine hydrobromide are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive toxicology studies. The compound is intended for research purposes only and is not approved for clinical use. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
Tedatioxetine hydrobromide (Lu AA24530) is a multimodal antidepressant with CAS number 960151-65-9, molecular formula C₁₈H₂₂BrNS, and molecular weight 364.34. It acts as a triple reuptake inhibitor (serotonin, norepinephrine, dopamine) and an antagonist of 5-HT₂A, 5-HT₂C, 5-HT₃, and α₁A-adrenergic receptors. It was investigated for major depressive disorder. This product is for research use only.
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| Molecular Formula |
C18H22BRNS
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|---|---|
| Molecular Weight |
364.3430
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| Exact Mass |
363.066
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| CAS # |
960151-65-9
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| PubChem CID |
24751582
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| Appearance |
White to off-white solid powder
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| LogP |
5.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
279
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Br.S(C1C(C2CCNCC2)=CC=CC=1)C1C=CC(C)=CC=1
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| InChi Key |
OJVYWXLMPZJYGV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21NS.BrH/c1-14-6-8-16(9-7-14)20-18-5-3-2-4-17(18)15-10-12-19-13-11-15;/h2-9,15,19H,10-13H2,1H3;1H
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| Chemical Name |
4-[2-(4-methylphenyl)sulfanylphenyl]piperidine;hydrobromide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~100 mg/mL (~274.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7447 mL | 13.7234 mL | 27.4469 mL | |
| 5 mM | 0.5489 mL | 2.7447 mL | 5.4894 mL | |
| 10 mM | 0.2745 mL | 1.3723 mL | 2.7447 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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