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- CAS号：
59-46-1
- 规格：
1g/100mg/500mg
| 规格： | 1g | 产品价格： | ￥334.0 |
|---|---|---|---|
| 规格： | 100mg | 产品价格： | ￥137.0 |
| 规格： | 500mg | 产品价格： | ￥282.0 |
Product Introduction
Bioactivity
| 名称 | Procaine |
| 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. |
| 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) |
| 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). |
| 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]。 |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 252.5 mg/mL (1068.51 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (8.46 mM), Sonication is recommended. Ethanol : 43 mg/mL (181.96 mM), Sonication is recommended. 10% DMSO+90% Saline : 10 mg/mL (42.32 mM), Solution. |
| 关键字 | targets | SodiumChannel | Sodium Channel | RNASynthesis | RNA Synthesis | Procaine | onset | multiple | Inhibitor | inhibit | HistoneDemethylase | Histone Demethylase | duration | DNASynthesis | DNA/RNA Synthesis | DNA Synthesis |
| 相关产品 | Guanidine hydrochloride | Levulinic acid | Doxycycline | Neomycin sulfate | Terbinafine hydrochloride | Dimethyl sulfoxide | Sodium bicarbonate | Hyaluronic acid sodium (MW 20 kDa) | Thymidine | Sodium diacetate | Sulfamethoxazole sodium | D(+)-Raffinose pentahydrate |
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文献和实验抗心律失常药可通过不同作用机制，改变心肌细胞的自律性、传导性、动作电位时程、有效不应期等电生理特性，用于治疗各种心律失常。显然，药物所致上述心肌电生理特性过度改变，将导致新的心律紊乱，因此这类药大多安全范围狭窄。由于心肌血液供应丰富，该类药血清浓度较能反映靶位浓度，并大多与治疗作用和毒性反应，特别是心脏毒性相关。用本类药物治疗的疾病，往往存在循环、肝、肾功能改变，将对该类药的体内过程产生影响。而本类药中普鲁卡因胺、利多卡因等的代谢物仍有药理活性，此外本类中某些药物代谢上存在强、医学|教育
刘连璞，单春文，肖焕才，杨淑琴，乔东访，安连兵.普鲁卡因胺抑制兔血小板聚集的电镜观察［J］.武汉大学学报，Sup.2P125-126. ［12］ 单春文，刘连璞，林继红，杨淑琴.普鲁卡因胺对血小板及其开放管道系统形态结构改变的影响［J］.中国医学物理学杂志1999，16：56-59. ［13］ Lin JH,Shan CW,Yang SQ,Liu PL.Effects of procainamide on morphological parameter of dense
55 - 1.2 0.59 6.0 多巴酚丁胺 dobutamine - - - 59 0.2 2.4 阿霉素 doxorublicin 5
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