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顶部相关产品产品介绍化学信息储存和溶解信息计算器

Pimethixene

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纯度: 97.50%

货号 T12489Cas号 314-03-4

别名 匹美噻吨, Pimetixene, Calmixen

Pimethixene (Calmixen) 是抗组胺和抗血清素剂，用作抗偏头疼剂。它是高效多靶点拮抗剂。

Pimethixene
其他形式的 “Pimethixene”:
Pimethixene maleateT12489L13187-06-9
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Pimethixene

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Rating icon 很棒

纯度: 97.50%

货号 T12489 别名 匹美噻吨, Pimetixene, CalmixenCas号 314-03-4

Pimethixene (Calmixen) 是抗组胺和抗血清素剂，用作抗偏头疼剂。它是高效多靶点拮抗剂。

规格价格库存数量
1 mg
¥ 198
现货
5 mg
¥ 413
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10 mg
¥ 593
现货
25 mg
¥ 987
现货
50 mg
¥ 1,530
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100 mg
¥ 2,290
待询
200 mg
¥ 3,290
待询
1 mL x 10 mM (in DMSO)
¥ 358
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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。
实验操作小课堂
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选择批次:
纯度: 97.50%
颜色: 白色
性状: Solid
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资源下载:
COA HNMR HPLC LCMS产品操作手册

产品介绍

Pimethixene AI Summary
Pimethixene is a molecule that exhibits a diverse range of bioactivities across various biological pathways. It has a high binding affinity for the 5-hydroxytryptamine 2A receptor from rat forebrain with a Ki value of 2.5 nM, suggesting potential effects on serotonin signaling pathways. In human H4 cells, it inhibits acid sphingomyelinase (ASM) with 32.0% residual activity at a concentration of 10 μM. Additionally, it inhibits LuxR-dependent quorum sensing in Vibrio fischeri with an IC50 of 56000.0 nM by reducing the bioluminescence intensity induced by 3-oxo-C6-HSL. Pimethixene also demonstrates inhibition of recombinant SET7/9 with an IC50 of 4300.0 nM and the internalization of Anthrax Lethal Toxin with a potency of 10000.0 nM. It acts as both an inhibitor and a substrate for Cytochrome P450 enzymes 2C19 and 2D6 with potencies of 15848.9 nM and 3981.1 nM respectively. Furthermore, it shows inhibitory activity against USP1/UAF1 (IC50 35481.3 nM) and the Marburg Virus (IC50 8912.5 nM). In the context of antiviral activity, Pimethixene exhibits low activity against SARS-CoV-2 in HRCE cells, and has a high IC50 value (> 100000.0 nM) for inhibiting VERO-6 cell cytotoxicity induced by the virus. It also shows cytotoxicity in VERO-E6 cells with a CC50 value of 25700.0 nM. Notably, Pimethixene inhibits human HDAC6 enzyme activity with 47.37% inhibition observed in one enzyme assay, compared to 2.75% in another, indicating potential selectivity for HDAC6. Finally, it interacts with various other receptors and enzymes, displaying bioactivity across a broad spectrum of targets including DRD1, SLC6A2, ADRA2A, HTR1A, DRD3, CHRM2, and TBXA2R, with agonistic activity towards TBXA2R and antagonistic activity towards CHRM1 and ADRA1A, though showing no significant activity against some targets like ESR1 and MAOA within tested concentration ranges..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).
靶点活性
5-HT2C receptor:8.42 (pki), M2 mAChR:9.38 (pki), D2 receptor:8.19 (pki), 5-HT1A receptor:7.63 (pki), DD4.4 receptor:7.54 (pki), 5-HT2A receptor:10.22 (pki), M1 mAChR:8.61 (pki), H1 receptor:10.14 (pki), 5-HT2B receptor:10.44 (pki)
别名匹美噻吨, Pimetixene, Calmixen
化学信息
分子量293.43
分子式C19H19NS
CAS No.314-03-4
SmilesCN1CCC(CC1)=C1c2ccccc2Sc2ccccc12
密度1.192g/cm3
储存&溶解度
存储In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 18.33 mg/mL (62.47 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.4080 mL17.0398 mL34.0797 mL170.3984 mL
5 mM0.6816 mL3.4080 mL6.8159 mL34.0797 mL
10 mM0.3408 mL1.7040 mL3.4080 mL17.0398 mL
20 mM0.1704 mL0.8520 mL1.7040 mL8.5199 mL
50 mM0.0682 mL0.3408 mL0.6816 mL3.4080 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：
比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL， 一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O， 那么您的工作液浓度为2 mg/mL。
母液配置方法：2 mg 药物溶于 100 μL DMSO （ 母液浓度为 20 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： 取 100 μL DMSO 母液， 添加 400 μL PEG300 混匀澄清， 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 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： DMSO， PEG300， PEG400， Tween 80， SBE-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

关键词

Serotonin ReceptorPimethixeneM2 receptorM2 mAChRM1 receptorM1 mAChRInhibitorinhibitHistamineReceptorHistamine ReceptorH1 receptorDopamineReceptorDopamine ReceptorDD4.4 receptorD4.4 receptorD2 receptorD25-hydroxytryptamine Receptor5HTReceptor5-HT2C Receptor5-HT2C5-HT2B Receptor5-HT2B5-HT2A Receptor5-HT2A5-HT1A Receptor5-HT1A5-HT Receptor5HT Receptor
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