2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Eplivanserin hemifumarate

Eplivanserin hemifumarate  (Synonyms: SR-46349 hemifumarate; SR 46349B)

目录号: HY-110129 纯度: 98.07%
COA 产品使用指南

摩尔计算器

Eplivanserin (SR-46349) hemifumarate 是一种有效的，选择性的，具有口服活性的 5-HT2 receptor 拮抗剂，在大鼠皮层膜中，IC50 值为 5.8 nM，同时对 5-HT2 receptor 的 Kd 值为 1.14 nM。Eplivanserin hemifumarate 对 5-HT2A 的选择性比对 5-HT2B 和 5-HT2C 高 20 倍以上。

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Eplivanserin hemifumarate Chemical Structure

Eplivanserin hemifumarate Chemical Structure

CAS No. : 130580-02-8

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规格 价格 是否有货 数量
5 mg ￥3100
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Customer Review

Other Forms of Eplivanserin hemifumarate:

Eplivanserin hemifumarate 相关抗体

Top Publications Citing Use of Products

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C[1][2].

IC50 & Target[1][2]

5-HT2A Receptor

5.8 nM (IC50)

5-HT2C Receptor

120 nM (IC50)

体外研究
(In Vitro)

Eplivanserin hemifumarate (SR 46349B) shows weak inhibition on other 5-HT kinases, with IC50s of 0.12 μM (Pig cortex 5-HT1C), 14 μM (Rat hippocampus 5-HT1A), and 16 μM (Rat stnatum 5-HT1B, Ox caudate nucleus 5-HT1D). Eplivanserin also has inhibitory effects on rat cortex adrenergic α1 and α2, rat whole brain histammine H1, Na+ channel, and rat striatum dopamine D1 and D2, with IC50s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively[1].

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

Eplivanserin hemifumarate 相关抗体:
体内研究
(In Vivo)

Eplivanserin hemifumarate (SR 46349B) inhibits 5-HT2 receptor binding of [3H]ketanserin with an ED50 of 0.087 mg/kg after i.p. injection, and 0.097 mg/kg after p.o administration in mice[1].
SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment in rats[2].

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

386.43

Formula

C19H21FN2O2.1/2C4H4O4
CAS 号
性状

固体

颜色

White to off-white

中文名称

富马酸依利色林
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 : 25 mg/mL (64.69 mM; 超声助溶 (<60°C); 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 2.5878 mL 12.9390 mL 25.8779 mL
5 mM 0.5176 mL 2.5878 mL 5.1756 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

只
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

纯度: 98.07%

COA (267 KB) RP-HPLC (239 KB)

产品使用指南 (1538 KB)
参考文献

Eplivanserin hemifumarate 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 2.5878 mL 12.9390 mL 25.8779 mL 64.6948 mL
5 mM 0.5176 mL 2.5878 mL 5.1756 mL 12.9390 mL
10 mM 0.2588 mL 1.2939 mL 2.5878 mL 6.4695 mL
15 mM 0.1725 mL 0.8626 mL 1.7252 mL 4.3130 mL
20 mM 0.1294 mL 0.6469 mL 1.2939 mL 3.2347 mL
25 mM 0.1035 mL 0.5176 mL 1.0351 mL 2.5878 mL
30 mM 0.0863 mL 0.4313 mL 0.8626 mL 2.1565 mL
40 mM 0.0647 mL 0.3235 mL 0.6469 mL 1.6174 mL
50 mM 0.0518 mL 0.2588 mL 0.5176 mL 1.2939 mL
60 mM 0.0431 mL 0.2156 mL 0.4313 mL 1.0782 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.

Keywords:

Eplivanserin hemifumarate130580-02-8SR-46349 hemifumarate SR 46349B富马酸依利色林5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2AoraldopaminereleaseInhibitorinhibitorinhibit

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