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GeA-69

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产品编号 T5399Cas号 2143475-98-1

GeA-69 是一种选择性变构 PARP14 大结构域 2 (MD2) 抑制剂,Kd 值为 2.1 µM。

GeA-69
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GeA-69

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纯度: 99.85%
产品编号 T5399Cas号 2143475-98-1

GeA-69 是一种选择性变构 PARP14 大结构域 2 (MD2) 抑制剂,Kd 值为 2.1 µM。

规格价格库存数量
2 mg
¥ 108
现货
5 mg
¥ 173
现货
10 mg
¥ 278
现货
25 mg
¥ 557
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50 mg
¥ 768
现货
100 mg
¥ 1,030
现货
1 mL x 10 mM (in DMSO)
¥ 191
现货
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产品介绍

生物活性
产品描述
GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).
靶点活性
PARP14:0.86 μM (Kd, in ITC assays)
体外活性
The macrodomain recruitment was significantly decreased in cells pre-treated with 50 μM GeA-69 and completely prevented in cells exposed to 250 μM GeA-69.
激酶实验
Binding experiments were carried out on a VP-ITC microcalorimeter. All experiments were performed in 50 mM HEPES (pH 7.4), 300 mM NaCl, 5 % glycerol, 0.5 mM TCEP at 12 °C, a reference power of 12 μCal/sec and a stirring speed of 307 rpm. The titrations were conducted using an initial injection of 2 μL followed by 28 identical injections of 10 μL with duration of 4 sec (per injection) and a spacing of 240 sec between injections. Competition experiments were performed on an iTC200 instrument at 20 °C, a reference power of 12 μCal/sec and a stirring speed of 1000 rpm. Following an initial injection of 0.2 μL, 20 identical injections of 2 μL were run with a duration of 4 sec (per injection) and a spacing of 150 sec between injections. Data analysis was carried out using Origin software with the MicroCal plugin. Thermodynamic parameters were calculated using ΔG = ΔH ? TΔS = ?RTlnKB, where ΔG, ΔH, and ΔS are the changes in free energy, enthalpy, and entropy of binding, respectively. In all cases, a single binding site model was employed.
化学信息
分子量300.35
分子式C20H16N2O
CAS No.2143475-98-1
SmilesCC(=O)Nc1ccccc1-c1cccc2c3ccccc3[nH]c12
密度1.281 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 120 mg/mL (399.53 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.3294 mL16.6472 mL33.2945 mL166.4724 mL
5 mM0.6659 mL3.3294 mL6.6589 mL33.2945 mL
10 mM0.3329 mL1.6647 mL3.3294 mL16.6472 mL
20 mM0.1665 mL0.8324 mL1.6647 mL8.3236 mL
50 mM0.0666 mL0.3329 mL0.6659 mL3.3294 mL
100 mM0.0333 mL0.1665 mL0.3329 mL1.6647 mL

SCI 文献

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 20 g ,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% 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 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 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | 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。

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
%ddH2O

剂量转换

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