2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Autophagy
  3. 5-HT Receptor Potassium Channel Autophagy
  4. Ketanserin

Ketanserin  (Synonyms: 酮色林; R41468)

目录号: HY-10562 纯度: 99.89%
COA 产品使用指南

摩尔计算器

Ketanserin 是一种选择性的 5-HT2 receptor 拮抗剂。Ketanserin 也抑制 hERG 电流 (IhERG)，IC50 为 0.11 μM，这种作用具有浓度依赖性。

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Ketanserin Chemical Structure

Ketanserin Chemical Structure

CAS No. : 74050-98-9

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规格 价格 是否有货 数量
25 mg ￥349
In-stock
50 mg ￥500
In-stock
100 mg ￥700
In-stock
200 mg ￥1045
In-stock
500 mg ￥1775
In-stock
1 g   询价  
5 g   询价  

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Customer Review

Other Forms of Ketanserin:

Ketanserin 相关抗体

Top Publications Citing Use of Products

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

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).

IC50 & Target

5-HT2 Receptor

 

hERG current

0.11 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
260 nM
Compound: Ketanserin
Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
[PMID: 9357514]
CHO IC50
6500 nM
Compound: Ketanserin
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
[PMID: 9357514]
CHO-K1 IC50
0.29 μM
Compound: ketanserin
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
[PMID: 23403082]
CHO-K1 IC50
11 nM
Compound: Ketanserin
Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
[PMID: 25557493]
CHO-K1 IC50
32 nM
Compound: Ketanserin
Antagonist activity at human 5HT2A receptor expressed in EC80 serotonin-stimulated CHOK1 cells by calcium mobilization assay
Antagonist activity at human 5HT2A receptor expressed in EC80 serotonin-stimulated CHOK1 cells by calcium mobilization assay
[PMID: 19328689]
CHO-K1 IC50
80 nM
Compound: Ketanserin
Antagonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay
Antagonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay
[PMID: 23675993]
HEK293 IC50
0.52 nM
Compound: Ketanserin
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor in HEK293 cells after 60 mins by scintillation counting
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor in HEK293 cells after 60 mins by scintillation counting
[PMID: 27997171]
HEK293 EC50
1.04 nM
Compound: Ketanserin
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
[PMID: 23537943]
HEK293 IC50
3.5 x 10-10 M
Compound: Ketanserin
Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
体外研究
(In Vitro)

0.3 μM Ketanserin 抑制 hERG 通道的电压依赖性阶跃电流 (IhERG.step) 和尾电流 (IhERG.tail)，暴露时间为 5 分钟[1]。
观察到的 AA 与 5-HT 的协同作用也被 5-HT 受体阻滞剂赛庚啶 (IC50=22.0±7 μM)、Ketanserin (IC50=152±23 μM)。Ketanserin (50-350 μM) 通过以剂量依赖的方式阻断受体来抑制协同作用。Cyproheptadine 的 IC50 值为 22±7 μM，Ketanserin 为 152±23 μM[2]。
Ketanserin 抑制血小板聚集，IC50 为 240 (169-339) nM[3]。

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

Ketanserin 相关抗体:
体内研究
(In Vivo)

Ketanserin 是一种 5-HT2A 受体拮抗剂。Ketanserin 显著降低许多大脑区域 (海马体的 CA1 和 CA3、前额叶皮层、中央杏仁核、下丘脑背内侧核、齿状回、伏核壳和中脑导水管周围灰质) 中的 BDNF 蛋白水平。5-HT2A拮抗剂 Ketanserin 可显著降低各脑区BDNF mRNA水平[4]。

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

395.43

Formula

C22H22FN3O3
CAS 号
性状

固体

颜色

White to off-white

中文名称

酮色林；凯坦色林；凯他色林；酮舍林；氟哌喹酮
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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 16.67 mg/mL (42.16 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)

DMF 中的溶解度 : 5 mg/mL (12.64 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5289 mL 12.6445 mL 25.2889 mL
5 mM 0.5058 mL 2.5289 mL 5.0578 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.67 mg/mL (4.22 mM); 澄清溶液

    此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.67 mg/mL (4.22 mM); 澄清溶液

    此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂： 50% PEG300    50% Saline

    Solubility: 6.25 mg/mL (15.81 mM); 悬浊液; 超声助溶

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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.89%

COA (190 KB) HNMR (263 KB) LCMS (93 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

The established HEK 293 cell line stably expressing hERG channels is cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% foetal bovine serum, 400 μg/mL G418. The HEK 293 cell line stably expressing recombinant human cardiac KCNQ1/KCNE1 channel current (IKs) is maintained in DMEM containing 10% foetal bovine serum and 100 μg/mL hygromycin. Cells used for electrophysiology are seeded on a glass coverslip. The mutant hERG channels are constructed, and are transiently expressed in HEK 293 cells using 10 μL of Lipofectamine 2000 with 4 μg of hERG mutant cDNA in pCDNA3 vector[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

Rat[4]
A total of 155 specific-pathogen-free 2-month-old male Sprague-Dawley rats, weighing 180-220 g, are used. The rats are randomly divided into the following six groups: 5-HT1A receptor agonist (8-OH-DPAT) PS group (DPAT-PS group, n=30); 5-HT1A receptor antagonist (MDL73005) PS group (MDL-PS group, n=30); 5-HT2A receptor agonist (DOI) PS group (DOI-PS group, n=30); 5-HT2A receptor antagonist (Ketanserin) PS group (Ketan-PS group, n=30); the solvent control no-stress group (0.9% physiological saline group, CON group); and the PS only group (PS group, n=30). The DPAT-PS, MDL-PS, DOI-PS, Ketan-PS and PS groups are further divided into six subgroups (n=5 each) according to the time between the stress and analysis; immediately after stress, and 0.5, 1, 2, 6 and 24 hours after stress. The CON group (n=5) receive normal feed. For the Ketan-PS group, Ketanserin, dissolved in 0.9% physiological saline, is injected intraperitoneally at 5 mg/kg at 1 hour before each stress exposure.

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

Ketanserin 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMF / DMSO 1 mM 2.5289 mL 12.6445 mL 25.2889 mL 63.2223 mL
5 mM 0.5058 mL 2.5289 mL 5.0578 mL 12.6445 mL
10 mM 0.2529 mL 1.2644 mL 2.5289 mL 6.3222 mL
DMSO 15 mM 0.1686 mL 0.8430 mL 1.6859 mL 4.2148 mL
20 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1611 mL
25 mM 0.1012 mL 0.5058 mL 1.0116 mL 2.5289 mL
30 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1074 mL
40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5806 mL
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  • 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:

Ketanserin74050-98-9R41468酮色林凯坦色林凯他色林酮舍林氟哌喹酮R 41468R-414685-HT ReceptorPotassium ChannelAutophagySerotonin Receptor5-hydroxytryptamine ReceptorKcsAInhibitorinhibitorinhibit

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