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| 10mg |
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| 25mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Vortioxetine HBr (formerly AA21004, Lu-AA21004, AA21004; Lu AA21004), the hydrobromide salt of Vortioxetine which is a marketed and atypical antidepressant, is an orally bioactive and multimodal serotonergic agent with potential anti-depressive activity. It has IC50 values of 15 nM, 33 nM, 3.7 nM, 19 nM, and 1.6 nM for 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor, and SERT, respectively. In 2013, the FDA approved the atypical antidepressant vortioxetine for the treatment of major depressive disorder (MDD) in adults. One such "serotonin modulator and stimulator" is vortioxetine.
| Targets |
sPLA2 ( Ki = 15 nM ); 5-HT3A Receptor ( Ki = 3.7 nM ); 5-HT7 Receptor ( Ki = 19 nM ); SERT ( Ki = 1.6 nM )
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| ln Vivo |
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| Enzyme Assay |
Vortioxetine (Compound 5m) is a multimodal serotonergic agent that inhibits SERT with values of 1.6 nM, 33 nM, 3.7 nM, 19 nM, and 5-HT1A, 5-HT1B, and 5-HT7 receptors, respectively. Vortioxetine exhibits strong suppression of SERT as well as antagonistic effects at 5-HT3A and 5-HT7 receptors, partial agonist effects at 5-HT1B receptors, and agonistic effects at 5-HT1A receptors.
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| Cell Assay |
Vortioxetine is a partial h5-HT1B receptor agonist that, in a whole-cell cAMP-based assay, has an EC50 of 460 nM and an intrinsic activity of 22%. In vitro whole-cell cAMP assay, vortioxetine binds to the r5-HT7 receptor with a Kivalue of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM.
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| References |
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| Molecular Formula |
C18H22N2S
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| Molecular Weight |
379.36
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| Exact Mass |
378.08
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| Elemental Analysis |
C, 56.99; H, 6.11; Br, 21.06; N, 7.38; S, 8.45
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| CAS # |
960203-27-4
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| Related CAS # |
Vortioxetine; 508233-74-7; Vortioxetine-d8 hydrobromide
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| Appearance |
White to off-white solid powder
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| SMILES |
CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C.Br
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| InChi Key |
VNGRUFUIHGGOOM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22N2S.BrH/c1-14-7-8-17(15(2)13-14)21-18-6-4-3-5-16(18)20-11-9-19-10-12-20;/h3-8,13,19H,9-12H2,1-2H3;1H
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| Chemical Name |
1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine;hydrobromide
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.59 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 (6.59 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 (6.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 15% Captisol, pH 9: 10 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6360 mL | 13.1801 mL | 26.3602 mL | |
| 5 mM | 0.5272 mL | 2.6360 mL | 5.2720 mL | |
| 10 mM | 0.2636 mL | 1.3180 mL | 2.6360 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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