1. Neuronal Signaling
  2. Dopamine Transporter Serotonin Transporter
  3. Dasotraline

Dasotraline  (Synonyms: SEP 225289)

目录号: HY-12850
产品使用指南

Dasotraline 是一种三重再摄取抑制剂,阻断多巴胺 (dopamine),去甲肾上腺素 (norepinephrine) 和 5-羟色胺 (5-HT) 转运蛋白,IC50 值分别为 4, 6 和 11 nM。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Dasotraline hydrochloride 通常具有更好的水溶性和稳定性。

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Dasotraline Chemical Structure

Dasotraline Chemical Structure

CAS No. : 675126-05-3

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规格 是否有货
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Dasotraline 的其他形式现货产品:

Customer Review

Other Forms of Dasotraline:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

IC50 & Target

IC50: 4 nM (dopamine transporter), 6 nM (norepinephrine transporter),11 nM (5-HT transporter)[1]

体内研究
(In Vivo)

The present in-vivoelectrophysiological study is undertaken to determine the effects of the triple reuptake inhibitor Dasotraline (SEP-225289) on the neuronal activities of locus coeruleus (LC) NE, ventral tegmental area (VTA) DA and dorsal raphe (DR) 5-HT neurons. Administered acutely, Dasotraline dose-dependently decreases the spontaneous firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of α2, D2 and 5-HT1A autoreceptors, respectively. Dasotraline predominantly inhibits the firing rate of LC NE neurons while producing only a partial decrease in VTA DA and DR 5-HT neuronal discharge. Dasotraline is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery (RT50) of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE. The recovery time (RT), from the suppression of hippocampus pyramidal neuron firing activity following microiontophoresis application of 5-HT and NE, is assessed by determining the RT50 values before and after the acute intravenous administration of cumulative doses of Dasotraline (1–8 mg/kg). Although Dasotraline (1 and 2 mg/kg) does not modify the firing activity of CA3 pyramidal neurons, a significant reduction (∼50%) is detected with the highest dose (8 mg/kg). In rats pre-treated with WAY100635, Dasotraline (0.5-2 mg/kg i.v.) elicits a significant increase in DR 5-HT firing rate. In rats pre-treated with WAY100635, Dasotralinesignificantly increases the number of single spikes and bursts[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

292.20

Formula

C16H15Cl2N

CAS 号
中文名称

达索曲林

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 31 mg/mL (106.09 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4223 mL 17.1116 mL 34.2231 mL
5 mM 0.6845 mL 3.4223 mL 6.8446 mL
查看完整储备液配制表
  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4223 mL 17.1116 mL 34.2231 mL 85.5578 mL
5 mM 0.6845 mL 3.4223 mL 6.8446 mL 17.1116 mL
10 mM 0.3422 mL 1.7112 mL 3.4223 mL 8.5558 mL
15 mM 0.2282 mL 1.1408 mL 2.2815 mL 5.7039 mL
20 mM 0.1711 mL 0.8556 mL 1.7112 mL 4.2779 mL
25 mM 0.1369 mL 0.6845 mL 1.3689 mL 3.4223 mL
30 mM 0.1141 mL 0.5704 mL 1.1408 mL 2.8519 mL
40 mM 0.0856 mL 0.4278 mL 0.8556 mL 2.1389 mL
50 mM 0.0684 mL 0.3422 mL 0.6845 mL 1.7112 mL
60 mM 0.0570 mL 0.2852 mL 0.5704 mL 1.4260 mL
80 mM 0.0428 mL 0.2139 mL 0.4278 mL 1.0695 mL
100 mM 0.0342 mL 0.1711 mL 0.3422 mL 0.8556 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Dasotraline
目录号:
HY-12850
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