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Zotepine

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纯度: 99.78%

货号 T19680Cas号 26615-21-4

别名 佐替平

Zotepine 是一种抗精神病剂,是有效的5-HT2A、5-HT2C、组胺H1、α1-肾上腺素能和多巴胺D2受体拮抗剂,Kd 值分别为 2.6、3.2、3.3、7.3 和 8 nM。它在体内表现出抗抑郁和抗焦虑作用。

Zotepine
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Zotepine

一键复制产品信息
Rating icon 很棒

纯度: 99.78%

货号 T19680 别名 佐替平Cas号 26615-21-4

Zotepine 是一种抗精神病剂,是有效的5-HT2A、5-HT2C、组胺H1、α1-肾上腺素能和多巴胺D2受体拮抗剂,Kd 值分别为 2.6、3.2、3.3、7.3 和 8 nM。它在体内表现出抗抑郁和抗焦虑作用。

规格价格库存数量
1 mg
¥ 388
现货
5 mg
¥ 747
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10 mg
¥ 969
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25 mg
¥ 1,380
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50 mg
¥ 1,980
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100 mg
¥ 3,120
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200 mg
¥ 4,470
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1 mL x 10 mM (in DMSO)
¥ 788
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产品介绍


Zotepine AI Summary
Zotepine exhibits a diverse range of bioactivities and binding affinities towards various human receptors, including dopamine receptors (DRD1, DRD2, DRD3, and DRD4), serotonin receptors (5-HT2A, 5-HT2C, and 5-HT1), alpha adrenergic receptors (alpha-1 and alpha-2), and histamine H1 receptor. It shows very high binding affinity towards human serotonin 5-HT2A receptor (Ki = 0.5 nM) and strong binding affinity to dopamine D2 (Ki = 11.0 nM), D3 (Ki = 6.4 nM), and histamine H1 receptor (Ki = 0.62 nM). It also exhibits moderate binding affinity towards these receptors and others such as D1 (Ki = 29.0 nM), D4 (Ki = 39.0 nM), and alpha-2 adrenergic receptor (Ki = 180.0 nM), but lower binding affinity towards muscarinic receptor. Additionally, Zotepine affects neurotransmission and receptor-mediated activities, as well as demonstrating significant engagement in various biological assays. It has exhibited inhibitory activity against human tyrosyl-DNA phosphodiesterase 1 (TDP1) and demonstrated potential antiviral effects against Lassa Virus, Marburg Virus, Ebola Virus, and SARS-CoV-2, albeit with varying degrees of efficacy. Notably, it displays inhibitory activity against SARS-CoV-2-induced cytotoxicity in Caco-2 and VERO-6 cells, though with limited potency. Zotepine also shows strong inhibition of human HDAC6 enzyme activity, with an IC50 value of 602.4 nM, and possesses moderate liver toxicity as indicated by elevated levels of ALT and AST serum activities in clinical trials. Furthermore, it has been evaluated in numerous receptor, enzyme, and transporter assays, demonstrating a wide range of interactions and activities that may inform its potential therapeutic applications..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic, and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM, and 8 nM, respectively. Zotepine is a second-generation antipsychotic with a primary use as a treatment for schizophrenia, although clinical trials have been conducted into its efficacy as an antimanic agent in patients with acute bipolar mania.
靶点活性
H1 receptor:3.3 nM(Kd), 5-HT2A:2.6 nM(Kd), 5-HT2C:3.2 nM(Kd)
别名佐替平
化学信息
分子量331.86
分子式C18H18ClNOS
CAS No.26615-21-4
SmilesCN(C)CCOC1=Cc2ccccc2Sc2ccc(Cl)cc12
密度1.0675 g/cm3 (Estimated)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 25 mg/mL (75.33 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.03 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.0133 mL15.0666 mL30.1332 mL150.6659 mL
5 mM0.6027 mL3.0133 mL6.0266 mL30.1332 mL
10 mM0.3013 mL1.5067 mL3.0133 mL15.0666 mL
20 mM0.1507 mL0.7533 mL1.5067 mL7.5333 mL
50 mM0.0603 mL0.3013 mL0.6027 mL3.0133 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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