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Ketotifen fumarate

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纯度: 99.73%

货号 T0994Cas号 34580-14-8

别名 富马酸酮替芬, HC 20511 fumarate

Ketotifen fumarate (HC 20511 fumarate) 是组胺 H1 受体和炎症介质释放的环七噻吩阻滞剂。

Ketotifen fumarate
其他形式的 “Ketotifen fumarate”:

Ketotifen fumarate

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Rating icon 很棒

纯度: 99.73%

货号 T0994 别名 富马酸酮替芬, HC 20511 fumarateCas号 34580-14-8

Ketotifen fumarate (HC 20511 fumarate) 是组胺 H1 受体和炎症介质释放的环七噻吩阻滞剂。

规格价格库存数量
50 mg
¥ 178
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100 mg
¥ 247
现货
500 mg
¥ 455
现货
1 g
¥ 587
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2 g
¥ 859
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1 mL x 10 mM (in DMSO)
¥ 272
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产品介绍


Ketotifen fumarate AI Summary
Ketotifen fumarate demonstrates a broad spectrum of bioactivities, positioning it as a multifaceted compound with potential applications across various biological systems. It significantly inhibits degranulation in anti-DNP IgE sensitized rat RBL2H3 cells by reducing beta-hexosaminidase release after 10 minutes, exhibiting IC50 values of 220,000 nM and 158,000 nM. Additionally, it shows strong inhibitory activity at histamine H1 receptors in ddY mice, reducing histamine-induced skin vascular permeability by 98.0% at 3 mg/kg, and displays anti-inflammatory effects in BALB/c mice by inhibiting ovalbumin-induced ear swelling. Ketotifen fumarate also exhibits substantial antiplasmodial activity against Plasmodium falciparum, with IC50 values ranging from 794.33 nM to 10000.0 nM, and differential potency in various qHTS assays for inhibitors of proliferation of multiple Plasmodium falciparum lines. In terms of transport proteins, Ketotifen fumarate has high inhibitory activity in OATP1B1 and OATP1B3 transfected CHO cells. It shows antianaphylactic activity, inhibiting antigen-induced histamine release and slow-reacting substance of anaphylaxis in ovalbumin-sensitized guinea pig lung. Furthermore, it displays inhibition activity against SARS-CoV-2 by inhibiting viral-induced cytotoxicity in Vero E6 and Caco-2 cells and inhibiting 3CL-Pro protease by 17.19% at 20 µM concentration. Antifungal and antibacterial assays reveal limited inhibition against Candida albicans, Cryptococcus neoformans, and various bacterial strains, with percentages ranging from minimal to 11.46%. Additionally, it affects protein domain stability and GPCR beta-arrestin recruitment assays, displaying both inhibitory and stimulating effects on multiple receptors, signifying a complex pharmacological profile. Overall, Ketotifen fumarate is a compound of significant interest due to its wide-ranging bioactivities, implicating its potential in antiallergic, anti-inflammatory, antiplasmodial, antiviral, and possibly antifungal and antibacterial therapeutics..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Ketotifen fumarate (HC 20511 fumarate) is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.
别名富马酸酮替芬, HC 20511 fumarate
化学信息
分子量425.50
分子式C23H23NO5S
CAS No.34580-14-8
SmilesOC(=O)\C=C\C(O)=O.CN1CC\C(CC1)=C1/c2ccsc2C(=O)Cc2ccccc12
密度1.236g/cm3
颜色White
物理性状Solid
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
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 55 mg/mL (129.26 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.7 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 mM2.3502 mL11.7509 mL23.5018 mL117.5088 mL
5 mM0.4700 mL2.3502 mL4.7004 mL23.5018 mL
10 mM0.2350 mL1.1751 mL2.3502 mL11.7509 mL
20 mM0.1175 mL0.5875 mL1.1751 mL5.8754 mL
50 mM0.0470 mL0.2350 mL0.4700 mL2.3502 mL
100 mM0.0235 mL0.1175 mL0.2350 mL1.1751 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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