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Tolfenamic Acid

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纯度: 99.97%

货号 T0784Cas号 13710-19-5

别名 托灭酸, 托芬那酸, Tolfedine, GEA 6414

Tolfenamic Acid (GEA 6414) 是一种非甾体抗炎剂和抗癌剂,可用于治疗偏头痛的症状。它能选择性地抑制COX-2的活性,在 LPS 诱导的犬 DH82 单核细胞/巨噬细胞中,对COX-2的IC50值为 13.49 μM(3.53 μg/mL)。

Tolfenamic Acid
其他形式的 “Tolfenamic Acid”:

Tolfenamic Acid

一键复制产品信息
Rating icon 很棒

纯度: 99.97%

货号 T0784 别名 托灭酸, 托芬那酸, Tolfedine, GEA 6414Cas号 13710-19-5

Tolfenamic Acid (GEA 6414) 是一种非甾体抗炎剂和抗癌剂,可用于治疗偏头痛的症状。它能选择性地抑制COX-2的活性,在 LPS 诱导的犬 DH82 单核细胞/巨噬细胞中,对COX-2的IC50值为 13.49 μM(3.53 μg/mL)。

规格价格库存数量
500 mg
¥ 326
现货
1 mL x 10 mM (in DMSO)
¥ 395
现货
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产品介绍


Tolfenamic Acid AI Summary
Tolfenamic Acid exhibits a broad range of bioactivities, including significant antiviral, anti-inflammatory, and enzyme inhibitory properties. It demonstrates the ability to undergo in vitro ester hydrolysis in 80% human plasma at 37°C, with distinctly different half-lives for methyl ester (100.0 hours) and N,N-diethylglycolamide ester (0.08333 hours) hydrolysis. Additionally, the compound displays potent anti-inflammatory effects, reducing carrageenan-induced paw edema in rats by 24.0% at specific dosages. Tolfenamic Acid shows marked antiviral activity against JC polyomavirus and modest activity against SARS-CoV-2, although its efficacy for the latter is relatively weak with an inhibition IC50 greater than 19952.62 nM. It also exhibits inhibition of the CYP2C9 enzyme (Ki of 537650433122253.3 nM), COX-2 enzyme (IC50 of 1170.0 nM), and multiple cytochrome P450 enzymes. The compound has demonstrated hepatotoxic and ulcerogenic activities, evidenced by significant toxicity in rats at 760 uM/kg over four days, leading to a 50% mortality rate and substantial body weight reduction. Tolfenamic Acid inhibits various other enzymes and targets, such as SARS-CoV-2 protease, human AKR1C3 (Ki of 8.0 nM), and HDAC6. Its binding affinity to TTR is noted, with distinct IC50 and Kd values. The diverse bioactivities presented indicate potential therapeutic applications but also highlight significant toxicity that needs to be carefully evaluated..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Tolfenamic Acid (GEA 6414) is one of the class of non-steroidal anti-inflammatory drugs (NSAIDs). It is used to treat the symptoms of migraine.
靶点活性
COX-2:0.2 μM
别名托灭酸, 托芬那酸, Tolfedine, GEA 6414
化学信息
分子量261.70
分子式C14H12ClNO2
CAS No.13710-19-5
SmilesN(C1=C(C(O)=O)C=CC=C1)C2=C(C)C(Cl)=CC=C2
密度1.2037 g/cm3 (Estimated)
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
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 49 mg/mL (187.24 mM), Sonication is recommended.
体内实验配方
10% DMSO+90% Corn Oil: 2 mg/mL (7.64 mM), Sonication is recommeded.
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 mM3.8212 mL19.1058 mL38.2117 mL191.0585 mL
5 mM0.7642 mL3.8212 mL7.6423 mL38.2117 mL
10 mM0.3821 mL1.9106 mL3.8212 mL19.1058 mL
20 mM0.1911 mL0.9553 mL1.9106 mL9.5529 mL
50 mM0.0764 mL0.3821 mL0.7642 mL3.8212 mL
100 mM0.0382 mL0.1911 mL0.3821 mL1.9106 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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