2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor 5-HT Receptor
  4. Spiroxatrine

Spiroxatrine  (Synonyms: R 5188)

目录号: HY-12706 纯度: 99.18%
COA 产品使用指南

摩尔计算器

Spiroxatrine (R 5188) 是一种选择性的 5-HT1α 和 α-肾上腺素能 (α2-adrenergic) 双拮抗剂，对5-HT1α、5-HT1 β 和 5-HT2 的 Ki 值分别为 3.94、224000、118.5 nM。Spiroxatrine (R 5188) 有镇静作用。

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Spiroxatrine Chemical Structure

Spiroxatrine Chemical Structure

CAS No. : 1054-88-2

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5 mg ￥1000
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10 mg ￥1600
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25 mg ￥3200
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50 mg ￥5100
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Customer Review

Spiroxatrine 相关抗体

Top Publications Citing Use of Products

查看 Adrenergic Receptor 亚型特异性产品:

查看所有亚型
α adrenergic receptor β adrenergic receptor

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
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

Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect[1][2][3][4].

IC50 & Target

α2-adrenergic receptor

 

5-HT1A Receptor

3.94 nM (Ki)

5-HT1B/D Receptor

224000 nM (Ki)

5-HT2 Receptor

118.5 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 EC50
20 μM
Compound: Spiroxatrine
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
HepG2 EC50
35.5 μM
Compound: Spiroxatrine
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
[PMID: 20966043]
体外研究
(In Vitro)

Spiroxatrine (0.01-0.1 μM, 15 mins) 使 α2A/D-肾上腺素受体敲除小鼠输精管组织收缩增强[2]。

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

Spiroxatrine 相关抗体:
体内研究
(In Vivo)

Spiroxatrine (1-25 ug, 腹腔注射, 5 天) 增加神经损伤大鼠和 Carrageenan (HY-125474) 诱导的炎症大鼠后爪对热刺激和机械刺激的戒断潜伏期[3]。 Spiroxatrine (4 mg/kg/每天, 腹腔注射, 5 分钟) 增强 Fluoxetine (HY-B0102) 减少选择性繁殖的嗜醇性 P系大鼠自愿口服乙醇摄入的效果[4]。

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

Animal Model: The nerve injury rat model and Carrageenan (HY-125474)-induced rat inflammation model[3]
Dosage: 1, 10, 25 ug, 5 days
Administration: Intraperitoneal injection (i.p.)
Result: Increased hindpaw withdrawal latencies to thermal and mechanical stimulation.
Animal Model: Fluoxetine (HY-B0102) -induced reduction of ethanol Intake by the P Line of rats[4]
Dosage: 4 mg/kg/day, 5 mins
Administration: Intraperitoneal injection (i.p.)
Result: Increased the voluntary oral ethanol intake induced by Fluoxetine (HY-B0102) in the selectively bred alcohol-preferring P line of rats.
分子量

379.45

Formula

C22H25N3O3
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 1.92 mg/mL (5.06 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 2.6354 mL 13.1770 mL 26.3539 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 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。-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
参考文献

Spiroxatrine 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。-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 2.6354 mL 13.1770 mL 26.3539 mL 65.8848 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL 13.1770 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:

Spiroxatrine1054-88-2R 5188R5188R-5188Adrenergic Receptor5-HT ReceptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine Receptornerve injury rat modelCarrageenan-induced rat inflammation modelsedativeinflammationInhibitorinhibitorinhibit

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