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Procaine

产品编号 T0029Cas号 59-46-1
别名 Duracaine, Spinocaine, Novocaine, Vitamin H3, 奴夫卡因, 普鲁卡因

Procaine (Vitamin H3) 是DNA 脱甲基剂,是一种酯类局部麻醉剂。它起效缓慢,作用持续时间短,主要用于浸润麻醉、周围神经阻滞和脊髓阻滞。

Procaine

Procaine

纯度: 99.55%
产品编号 T0029 别名 Duracaine, Spinocaine, Novocaine, Vitamin H3, 奴夫卡因, 普鲁卡因Cas号 59-46-1

Procaine (Vitamin H3) 是DNA 脱甲基剂,是一种酯类局部麻醉剂。它起效缓慢,作用持续时间短,主要用于浸润麻醉、周围神经阻滞和脊髓阻滞。

规格价格库存数量
100 mg¥ 152现货
500 mg¥ 333现货
1 g¥ 418现货
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纯度:99.55%
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产品介绍

生物活性
产品描述
Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.
体外活性
Procaine显著降低了HLE、HuH7和HuH6细胞的活性。Procaine在对HLE细胞实验时观察到S/G2/M周期转换受阻、形态学变化如空泡化,但凋亡率并未增加。Procaine处理后因DNA过度甲基化而转录抑制的基因被去甲基化并重新激活。Procaine对人类肝癌细胞具有生长抑制和去甲基化作用[2]。
体内活性
Procaine 在体内对异种移植瘤具有生长抑制和脱甲基作用[2]。
激酶实验
Biochemical Assays: Compound potency is also assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, PRC2 containing either EZH1 (160 pM), wt EZH2 (40 pM), or Y641N mutant EZH2 (80 pM, both EZH2 prepared in-house) is pre-incubated with 3H-SAM (0.9 μM), 2 μM H3K27me3 activating peptide (H2N-RKQLATKAAR(Kme3)SAPATGGVKKP-amide) and compounds (as 10 point duplicate dose response titrations) for 120 min in a buffer consisting of 50 mM Tris (pH 8.5), 1 mM DTT, 0.07 mM Brij-35, 0.1% BSA, and 0.8% DMSO in a total volume of 12.5 μl in a black 384 well plate. Reaction is initiated with biotinylated H3 substrate peptides (H3K27me1 for wt EZH2, H3K27me2 for Y641N mutant EZH2; H2N-RKQLATKAAR(Kmen)SAPATGGVKKP-NTPEGBiot) as a 2 μM stock in 12.5 μL and allowed to react at room temperature for 5 h. Quenching is accomplished by addition of 20 μl of STOP solution (50 mM Tris (pH 8.5), 200 mM EDTA, 2 mM SAH). 35 μL of the quenched solution is transferred to Streptavidin Flashplates, incubated overnight, washed, and read in a TopCount Reader. For titrations all compound dilutions are in DMSO, final DMSO concentrations are 0.8% (v/v), and turnover is kept to less than < 5%. IC50s are calculated using non-linear least square four parameter fits (GraphPad 6.0).
细胞实验
For apoptosis analysis, the TUNEL assay is performed on HLE cells treated with no drug(control), or 1 μM of DAC(5-aza-2'-deoxycytidine), or 1 mM of PCA(procaine), or 1 mM of PCAA(procainamide) for 96 h. The proportion of TUNEL-positive cells was calculated by counting at least 500 cells randomly. All assays were carried out in triplicate. (Only for Reference)
别名Duracaine, Spinocaine, Novocaine, Vitamin H3, 奴夫卡因, 普鲁卡因
化学信息
分子量236.31
分子式C13H20N2O2
CAS No.59-46-1
储存&溶解度
存储store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 47 mg/mL (198.89 mM)
Ethanol: 43 mg/mL (182 mM)
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM4.2317 mL21.1586 mL42.3173 mL211.5865 mL
5 mM0.8463 mL4.2317 mL8.4635 mL42.3173 mL
10 mM0.4232 mL2.1159 mL4.2317 mL21.1586 mL
20 mM0.2116 mL1.0579 mL2.1159 mL10.5793 mL
50 mM0.0846 mL0.4232 mL0.8463 mL4.2317 mL
100 mM0.0423 mL0.2116 mL0.4232 mL2.1159 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 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

对于不同动物的给药剂量换算,您也可以参考 更多

关键词

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