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Vortioxetine (Lu AA21004) HBr Sale

(Synonyms: 盐酸沃替西汀; Lu AA21004 hydrobromide) 目录号 : GC14437

A multimodal serotonergic agent

Vortioxetine (Lu AA21004) HBr Chemical Structure

Cas No.:960203-27-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥117.00
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5mg
¥107.00
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25mg
¥416.00
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100mg
¥1,350.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Vortioxetine (Lu AA21004) HBr (vortioxetine) is an antidepressant, [1] [2] and a serotonin (5-HT) receptor modulator [1] [3] with Ki values of 3.7 nM, 19 nM, 200 nM, 33 nM, 15 nM, and 1.6 nM, to human (h) 5-HT3A receptor, h5-HT7 receptor, rat (r) 5-HT7 receptor, h5-HT1B receptor, h5-HT1A receptor and h5-HT transporter (hSERT), respectively, with an IC50 value of 2080 nM to r5-HT7 receptor, and with an EC50 value of 460 nM to h5-HT1B receptor [3].

5-HT is important in brain, acting as a neurotransmitter in neuromodulation [4].

In HELA cells expressing h5-HT1B receptors stably, Lu AA21004 displayed a partial agonistic response with an EC50 value of 460±110 nM and an IA of 22%. In a polyclonal HEK-293 cell line expressing the r5-HT7 receptor, Lu AA21004 bound to the r5-HT7 receptor with a Ki value of 200±27 nM and was a functional antagonist at the r5-HT7 receptor with an IC50 value of 2080±18 nM [3].

In rats, subcutaneous (sc) administration of Lu AA21004 resulted in ED50 values of 0.4 mg/kg and 3.2 mg/kg to the rSERT and the r5-HT1B receptor, respectively. Lu AA21004 acted as an antagonist of 5-HT3 receptor with an ED50 value of 0.11 mg/kg sc [3]. Treatment with vortioxetine at doses of 2.5 and 5 mg/kg prior to the acquisition of novel objects made rats show 29 and 33 s, respectively, as average exploration values [5].

References:
[1].  Connie Sanchez, Karen E. Asin, Francesc Artigas, et al. Vortioxetine, a novel antidepressant with multimodal activity: Review of preclinical and clinical data. Pharmacology & Therapeutics, 2015, 145:43-57.
[2].  Er-min Gu, Chengke Huang, Bingqing Liang, et al. An UPLC–MS/MS method for the quantitation of vortioxetine in rat plasma: Application to a pharmacokinetic study. J. Chromatogr. B, 2015, 997:70-74.
[3].  A. Mørk, A. Pehrson, L.T. Brennum, S. Møller Nielsen, et al. Pharmacological effects of Lu AA21004: a novel multimodal compound for the treatment of major depressive disorder. J. Pharmacol. Exp. Ther., 2012, 340:666-675.
[4].  David M. Lovinger. Serotonin’s Role in Alcohol’s Effects on the Brain. Alcohol Health & Research World, 1997, 21(2):114-120.
[5].  Arne Mørk, Liliana P. Montezinho, Silke Miller, et al. Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats. Pharmacology, Biochemistry and Behavior, 2013, 105:41-50.

Chemical Properties

Cas No. 960203-27-4 SDF
别名 盐酸沃替西汀; Lu AA21004 hydrobromide
化学名 1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine;hydrobromide
Canonical SMILES CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C.Br
分子式 C18H22N2S.HBr 分子量 379.36
溶解度 ≥ 18.968mg/mL in DMSO 储存条件 Store at 2-8°C
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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。
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。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.636 mL 13.1801 mL 26.3602 mL
5 mM 0.5272 mL 2.636 mL 5.272 mL
10 mM 0.2636 mL 1.318 mL 2.636 mL
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