Vortioxetine是一种多模式抗抑郁药，对重组人5-HT1A（Ki=15nM）、5-HT1B（Ki=33nM）、5-HT3A（Ki=3.7nM）、5-HT7（Ki=19nM）、noradrenergic β1 receptor（Ki=46nM）以及SERT（Ki=1.6nM）具有高亲和力。
Cas No.:508233-74-7
Sample solution is provided at 25 µL, 10mM.
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Vortioxetine is a multimodal antidepressant, with high affinity for recombinant human 5-HT1A (Ki=15nM), 5-HT1B (Ki=33nM), 5-HT3A (Ki=3.7nM), 5-HT7 (Ki=19nM), and noradrenergic β1 receptor (Ki=46nM), and SERT (Ki=1.6nM)[1]. Vortioxetine exerts the antidepressant effect by regulating the activity of 5-hydroxytryptamine receptors and inhibiting the 5-hydroxytryptamine transporter [2]. Vortioxetine has been widely used in various animal models to improve cognitive abilities and the ability to recognize new objects[3].
In vitro, Vortioxetine treatment for 24 hours significantly inhibited the growth of AGS cells with an IC50 value of 25.1µM [4]. Treatment of A172 cells with 4μM Vortioxetine for 48h decreased the migration ability of A172 cells, decreased the expression levels of N-cadherin and Slug, and increased the expression levels of E-cadherin[5].
In vivo, Vortioxetine, administered orally at a dose of 10mg/kg daily for 3 weeks, improved context discrimination (CD) in GFAP-TK+ mouse models[6]. Daily intraperitoneal injection of Vortioxetine at a dose of 10mg/kg/day for 4 weeks reversed the reduction in anxiety-like behavior and ameliorated impairments in recognition and spatial reference memory in 5×FAD mice[7]. Daily subcutaneous injection of Vortioxetine at a dose of 10mg/kg for two weeks significantly improved levodopa-induced dyskinesia in mice[8].
References:
[1] Bang-Andersen B, Ruhland T, Jørgensen M, et al. Discovery of 1-[2-(2, 4-dimethylphenylsulfanyl) phenyl] piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder[J]. Journal of medicinal chemistry, 2011, 54(9): 3206-3221.
[2] Chen G, Højer A M, Areberg J, et al. Vortioxetine: clinical pharmacokinetics and drug interactions[J]. Clinical Pharmacokinetics, 2018, 57(6): 673-686.
[3] Sanchez C, Asin K E, Artigas F. Vortioxetine, a novel antidepressant with multimodal activity: review of preclinical and clinical data[J]. Pharmacology & therapeutics, 2015, 145: 43-57.
[4] Lv G B, Wang T T, Zhu H L, et al. Vortioxetine induces apoptosis and autophagy of gastric cancer AGS cells via the PI3K/AKT pathway[J]. FEBS open bio, 2020, 10(10): 2157-2165.
[5] Zhang H, Zhang D, Huang Z, et al. Vortioxetine exhibits anti-glioblastoma activity via the PI3K-Akt signaling pathway[J]. Iranian Journal of Basic Medical Sciences, 2025, 28(4): 401.
[6] Felice D, Guilloux J P, Pehrson A, et al. Vortioxetine improves context discrimination in mice through a neurogenesis independent mechanism[J]. Frontiers in pharmacology, 2018, 9: 204.
[7] Jiang L X, Huang G D, Su F, et al. Vortioxetine administration attenuates cognitive and synaptic deficits in 5× FAD mice[J]. Psychopharmacology, 2020, 237(4): 1233-1243.
[8] Budrow C, Elder K, Coyle M, et al. Broad serotonergic actions of vortioxetine as a promising avenue for the treatment of L-DOPA-induced dyskinesia[J]. Cells, 2023, 12(6): 837.
Vortioxetine是一种多模式抗抑郁药，对重组人5-HT1A（Ki=15nM）、5-HT1B（Ki=33nM）、5-HT3A（Ki=3.7nM）、5-HT7（Ki=19nM）、noradrenergic β1 receptor（Ki=46nM）以及SERT（Ki=1.6nM）具有高亲和力[1]。Vortioxetine通过调节5-羟色胺受体活性和抑制5-羟色胺转运体来发挥抗抑郁作用[2]。Vortioxetine已被广泛用于多种动物模型，以改善认知能力和新物体识别能力[3]。
在体外，Vortioxetine处理24小时显著抑制了AGS细胞的生长，IC50值为25.1µM[4]。用4µM的Vortioxetine处理A172细胞48小时，降低了A172细胞的迁移能力，减少了N-钙黏蛋白和Slug的表达水平，并提高了E-钙黏蛋白的表达水平[6]。
在体内，每日口服10mg/kg剂量的Vortioxetine，持续3周，改善了GFAP-TK+小鼠模型的情境辨别（CD）能力[6]。每日腹腔注射10mg/kg/day剂量的Vortioxetine，持续4周，逆转了5×FAD小鼠焦虑样行为的减少，并改善了识别和空间参考记忆的损伤[7]。每日皮下注射10mg/kg剂量的Vortioxetine，持续两周，显著改善了左旋多巴诱导的小鼠运动障碍[8]。
| Cell experiment [1]: | |
Cell lines | A172 cells |
Preparation Method | A172 cells were cultured in high-glucose DMEM medium supplemented with 10% fetal bovine serum (FBS), 100U/ml penicillin, and 100μg/ml streptomycin in a humidified incubator at 37℃ with 5% CO2. Cells were seeded in 96-well plates at a density of 4×103 cells per well and allowed to adhere overnight before being treated with various concentrations of Vortioxetine (0, 2, 4, 6, 8, and 10µM) for 72h and cell viability was analyzed. |
Reaction Conditions | 0, 2, 4, 6, 8, and 10µM; 72h |
Applications | Vortioxetine treatment reduced the cell viability of A172 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | 5×FAD mice |
Preparation Method | 5×FAD mice were maintained in a temperature and relative humidity-controlled environment (22±2°C, 40 to 70%) with a light/dark cycle of 12h/12h. Food and water were available ad libitum. The mice were divided into two groups: the experimental group was treated with Vortioxetine at a dose of 10mg/kg daily intraperitoneally for 4 weeks; the control group received normal saline without Vortioxetine. After 4 weeks of administration, behavioral tests were performed. |
Dosage form | 10mg/kg/day for 4 weeks; i.p. |
Applications | Vortioxetine treatment improved the impairment in recognition memory function in the 5×FAD mice. |
References: | |
| Cas No. | 508233-74-7 | SDF | |
| 别名 | 沃替西汀; Lu AA 21004 | ||
| 化学名 | 1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine | ||
| Canonical SMILES | CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C | ||
| 分子式 | C18H22N2S | 分子量 | 298.45 |
| 溶解度 | ≥ 14.9 mg/mL in DMSO, ≥ 4.31 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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