1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Thioperamide maleate

Thioperamide maleate  (Synonyms: MR-12842 maleate)

目录号: HY-12206A 纯度: 98.26%
COA 产品使用指南

Thioperamide maleate (MR-12842 maleate) 是一种有效的,具有口服活性的,可透过血脑屏障的选择性 H3 受体拮抗剂,抑制 [3H] 组胺释放的Ki 为 4.3 nM。Thioperamide maleate 抑制 [3H] 组胺合成的 Ki 为 31 nM 。

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Thioperamide maleate Chemical Structure

Thioperamide maleate Chemical Structure

CAS No. : 148440-81-7

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Other Forms of Thioperamide maleate:

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide maleate inhibits [3H]histamine synthesis with a Ki of 31 nM[1].

IC50 & Target[1]

H3 Receptor

 

体外研究
(In Vitro)

Thioperamide inhibits [3H]-(R)α-MeHA binding rat brain and guinea-pig lung with Kis of 2.1 nM and 2.0 nM, respectively. Thioperamide competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki of 4 nM[1].
Thioperamide (0.01-100 μM; 24 hours) promotes the viability of NE-4C stem cells in a concentration-dependent manner[2].
Thioperamide displays similar potencies at human H4 and H3 receptors (Ki=43 and 60 nM, respectively)[3].

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

Cell Viability Assay[2]

Cell Line: NE-4C stem cells
Concentration: 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 24 hours
Result: The viability of NE-4C stem cells increased significantly to 150.83±6.91% when (1 μM) was administrated, and increased to 145.11±14.52% and 132.02%±25.65% when 10 μM and 100 μM were administrated respectively.
体内研究
(In Vivo)

Thioperamide (5-20 mg/kg; i.p.) is able to facilitate reconsolidation of a contextually-conditioned fear memory in C57BL/6J mice[4].

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

Animal Model: Naive female C57BL/6J mice[4]
Dosage: 5, 10 or 20 mg/kg
Administration: Injections (i.p.)
Result: Facilitated reconsolidation of a contextually-conditioned fear memory.
Formula

C15H24N4S.xC4H4O4

CAS 号
性状

固体

颜色

White to off-white

中文名称

硫丙咪胺马来酸

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: 

H2O 中的溶解度 : 100 mg/mL (超声助溶)

  • 摩尔计算器

  • 稀释计算器

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

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=
浓度
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体积
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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

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每只动物的给药体积

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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
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
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纯度 & 产品资料
参考文献
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:
Thioperamide maleate
目录号:
HY-12206A
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