Vortioxetine|508233-74-7|(沃替西汀; Lu AA 21004)-陌孚医药/Medlife

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Vortioxetine (Synonyms: 沃替西汀; Lu AA 21004)

目录号: PL04426 纯度: ≥99%

Vortioxetine 是 5-HT1A，5-HT1B，5-HT3A，5-HT7 受体和 5-羟色胺转运体 (SERT) 的抑制剂，其 Ki 值分别为 15 nM，33 nM，3.7 nM，19 nM 和 1.6 nM。

CAS No. :508233-74-7

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中文名称	Vortioxetine
中文别名	米氮平杂质D;沃替丁汀;沃替西汀碱;沃替西汀对照品;1-[2-(2,4-甲基苯硫基)苯基]哌嗪;沃替西汀;1-(2-((2,4-二甲基苯基)硫代)苯基)哌嗪;米氮平杂质;沃替西汀标准品;沃替西汀杂质;沃替西汀杂质对照品
英文名称	Vortioxetine
英文别名	Vortioxetine;Trintellix (vortioxetine);Vortioxetine(Lu AA21004);1-(2-((2,4-DIMETHYLPHENYL)THIO)PHENYL)PIPERAZINE-HCL;Vortioxetin;1-[2-(2,4-Dimethylphenylsulfanyl)phenyl]piperazine;Lu AA 21004;Vortioxetine 1-(2-((2,4-Dimethylphenyl)thio)phenyl)piperazine;1-(2-((2,4-Dimethylphenyl)thio)phenyl)piperazine;1-(2-(2,4-dimethylphenylthio)phenyl)piperazine （Vortioxetine）;[14C]-Vortioxetine;1-(2-((2,4-Dimethylphenyl)sulfanyl)phenyl}piperazine;1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine;1-{2-[(2,4-dimethylphenyl)sulfanyl]phenyl}piperazine;CHEBI:76016;Piperazine, 1-(2-((2,4-dimethylphenyl)thio)phenyl)-;UNII-3O2K1S3WQV;Vortioxetine (USAN);Vortioxetine [USAN];Vortioxetine iMpurity;Brintellix;Lu AA21004;3O2K1S3WQV;Trintellix;1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine;Piperazine, 1-[2-[(2,4-dimethylphenyl)thio]phenyl]-;Brintellix (TN);1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine;1-[2-[(2,4-Dimethylphenyl)thio]phenyl]piperazine;1-(2-((2,4-Dim
Cas No.	508233-74-7
分子式	C₁₈H₂₂N₂S
分子量	298.45
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Vortioxetine 是 5-HT_1A，5-HT_1B，5-HT_3A，5-HT₇ 受体和 5-羟色胺转运体 (SERT) 的抑制剂，其 K_i 值分别为 15 nM，33 nM，3.7 nM，19 nM 和 1.6 nM。

生物活性

Vortioxetine is a inhibitor of 5-HT 1A , 5-HT 1B , 5-HT 3A , 5-HT 7 receptor and SERT, with K i values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

性状

Solid

IC50 & Target[1][2]

sPLA2 15 nM (Ki) 5-HT3A Receptor 3.7 nM (K

体外研究(In Vitro)

Vortioxetine (Compound 5m) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Vortioxetine displays 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]. Vortioxetine is a partial h5-HT 1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Vortioxetine binds to the r5-HT 7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay

体内研究(In Vivo)

Vortioxetine (Lu AA21004) occupies the r5-HT 1B receptor and rSERT (ED 50 = 3.2 and 0.4 mg/kg, respectively) after subcutaneous administration and is a 5-HT 3 receptor antagonist [6] . Vortioxetine significantly increases cell proliferation and cell survival and stimulates maturation of immature granule cells in the sub granular zone of the dentate gyrus of the hippocampus after 21 days of treatment [3] . Vortioxetine does not cause cognitive or psychomotor impairment [4] . has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Bang-Andersen B, Ruhland T, J?rgensen M, 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 May 12;54(9):3206-21.
[2]. Guilloux JP, Mendez-David I, Pehrson A, Antidepressant and anxiolytic potential of the multimodal antidepressant vortioxetine (Lu AA21004) assessed by behavioural and neurogenesis outcomes in mice. Neuropharmacology. 2013 May 28;73C:147-159.

溶解度数据	In Vitro: DMSO : 50 mg/mL (167.53 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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