Vortioxetine |
| Catalog No.GC16312 |
A multimodal serotonergic agent
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 508233-74-7
Sample solution is provided at 25 µL, 10mM.
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Vortioxetine is a novel multimodal antidepressant currently under development for the treatment of MDD. The serotonergic system plays an important role in cognitive functions via various 5-HT receptors.
In vitro: Vortioxetine (Lu AA21004) was the lead compound, displaying high affinity for recombinant human 5-HT1A (Ki = 15 nM), 5-HT1B (Ki = 33 nM), 5-HT3A (Ki = 3.7 nM), 5-HT7 (Ki = 19 nM), and noradrenergic β1 (Ki = 46 nM) receptors, and SERT (Ki = 1.6 nM). Vortioxetine displayed antagonistic properties at 5-HT3A and 5-HT7 receptors, partial agonist properties at 5-HT1B receptors, agonistic properties at 5-HT1A receptors, and potent inhibition of SERT [1].
In vivo: In conscious rats, vortioxetine significantly increased extracellular 5-HT levels in the brain after acute and 3 days of treatment. Following the 3-day treatment (5 or 10 mg/kg/day) SERT occupancies were only 43% and 57%, respectively [1].
Clinical trial: Drugs were administered in the evening of 15 consecutive days. Vortioxetine did not cause cognitive or psychomotor impairment. However, mirtazapine impaired cognitive and psychomotor performance on day 2. Most of these effects disappeared after multiple doses of mirtazapine [2].
References:
[1] Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A, Stensbøl TB. Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem. 2011;54(9):3206-21.
[2] Theunissen EL, Street D, Højer AM, Vermeeren A, van Oers A, Ramaekers JG. A randomized trial on the acute and steady-state effects of a new antidepressant, vortioxetine (Lu AA21004), on actual driving and cognition. Clin Pharmacol Ther. 2013;93(6):493-501.
| Cas No. | 508233-74-7 | SDF | |
| Chemical Name | 1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine | ||
| Canonical SMILES | CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C | ||
| Formula | C18H22N2S | M.Wt | 298.45 |
| Solubility | ≥ 14.9 mg/mL in DMSO, ≥ 4.31 mg/mL in EtOH with ultrasonic | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3506 mL | 16.7532 mL | 33.5064 mL |
| 5 mM | 670.1 μL | 3.3506 mL | 6.7013 mL |
| 10 mM | 335.1 μL | 1.6753 mL | 3.3506 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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