1. Neuronal Signaling
  2. Serotonin Transporter
  3. Ampreloxetine hydrochloride

Ampreloxetine hydrochloride  (Synonyms: TD-9855 hydrochloride)

目录号: HY-107128 纯度: 99.47%
COA 产品使用指南

Ampreloxetine (TD-9855) hydrochloride 是一种具有口服活性和 CNS 渗透性的去甲肾上腺素转运体 (NET) 和羟色胺 5-HT 摄取转运体 (SERT) 抑制剂,但不是多巴胺转运蛋白 (DAT)。Ampreloxetine hydrochloride结合去 NET 和 SERT,在血浆中的 EC50 值分别为 11.7 ng/mL 和 50.8 ng/mL。

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Ampreloxetine hydrochloride Chemical Structure

Ampreloxetine hydrochloride Chemical Structure

CAS No. : 1227056-87-2

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Customer Review

Other Forms of Ampreloxetine hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma[1].

IC50 & Target[1]

human Norepinephrine transporter

8.0 (pIC50)

human Serotonin transporter

8.6 (pIC50)

rat Norepinephrine transporter

7.9 (pIC50)

rat Serotonin transporter

8.9 (pIC50)

体内研究
(In Vivo)

Ampreloxetine hydrochloride (0.3- 60mg /kg;口服;单剂量) 在大鼠模型中,其血浆浓度和剂量水平无关[1]

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

Animal Model: Rat[1]
Dosage: 0.3, 1, 5, 10, 30, and 60mg/kg
Administration: PO; euthanized by decapitation at 0.5, 2, 4, 6, and 8 hr for 5mg/ kg dose level; 2 hr for 0.3, 1, 10, 30, and 60mg/kg dose levels
Result: In the effect compartment PK/PD analysis for NET and SERT occupancy, the estimated EC50 for occupancy was 11.7ng/mL for NET and 50.8ng/mL for SERT in rat spinal cords, and the projected human plasma EC50 values were 5.5ng/mL for NET and 23.9ng/mL for SERT.
Clinical Trial
分子量

357.80

Formula

C18H19ClF3NO

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (279.49 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7949 mL 13.9743 mL 27.9486 mL
5 mM 0.5590 mL 2.7949 mL 5.5897 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

  • 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

Ampreloxetine hydrochloride 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7949 mL 13.9743 mL 27.9486 mL 69.8714 mL
5 mM 0.5590 mL 2.7949 mL 5.5897 mL 13.9743 mL
10 mM 0.2795 mL 1.3974 mL 2.7949 mL 6.9871 mL
15 mM 0.1863 mL 0.9316 mL 1.8632 mL 4.6581 mL
20 mM 0.1397 mL 0.6987 mL 1.3974 mL 3.4936 mL
25 mM 0.1118 mL 0.5590 mL 1.1179 mL 2.7949 mL
30 mM 0.0932 mL 0.4658 mL 0.9316 mL 2.3290 mL
40 mM 0.0699 mL 0.3494 mL 0.6987 mL 1.7468 mL
50 mM 0.0559 mL 0.2795 mL 0.5590 mL 1.3974 mL
60 mM 0.0466 mL 0.2329 mL 0.4658 mL 1.1645 mL
80 mM 0.0349 mL 0.1747 mL 0.3494 mL 0.8734 mL
100 mM 0.0279 mL 0.1397 mL 0.2795 mL 0.6987 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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产品名称:
Ampreloxetine hydrochloride
目录号:
HY-107128
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