Lidocaine (Lignocaine) 抑制涉及复杂电压和依赖性的钠通道 (sodium channels)。Lidocaine 通过调节 miR-145 表达和进一步抑制MEK/ERK和NF-κB信号通路来减少胃癌细胞的生长,迁移和侵袭。Lidocaine 是一种酰胺衍生物,可用于研究室性心律失常。
生物活性 | Lidocaine (Lignocaine) inhibitssodium channelsinvolving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation ofMEK/ERKandNF-κBsignaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2]. |
IC50& Target[1,2] | |
体外研究 (In Vitro) | Lidocaine (Lignocaine) (10 nM; 48 hours) decreases significantly cell proliferation[2]. Lidocaine (1-10 nM; 24-72 hours) inhibits cell viability and achieves the most suppressing effects at the concentration of 10 nM and treatment time 48 hours[2]. Lidocaine (10 nM; 48 hours) increases significantly the apoptotic cell rate[2]. Lidocaine (10 nM; 48 hours) down-regulates Cyclin D1 and up-regulates p21 expression significantly[2].
Cell Proliferation Assay[2] Cell Line: | The human gastric cancer cell line MKN45 | Concentration: | 10 nM | Incubation Time: | 48 hours | Result: | Decreased significantly cell proliferation. |
Cell Viability Assay[2] Cell Line: | The human gastric cancer cell line MKN45 | Concentration: | 1, 5 and 10 nM | Incubation Time: | 24, 48, 72 hours | Result: | Inhibited MKN45 cell viability. |
Apoptosis Analysis[2] Cell Line: | The human gastric cancer cell line MKN45 | Concentration: | 10 nM | Incubation Time: | 48 hours | Result: | Increased significantly the apoptotic cell rate. |
Western Blot Analysis[2] Cell Line: | The human gastric cancer cell line MKN45 | Concentration: | 10 nM | Incubation Time: | 48 hours | Result: | Down-regulated Cyclin D1 and up-regulated p21 expression significantly. |
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体内研究 (In Vivo) | Lidocaine (Lignocaine) causes completely reversible tail nerve block in rats. Mechanical nociception block produced by lidocaine has slower onset and faster recovery compared with thermal nociception block[3].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(426.73 mM) H2O : ≥ 5 mg/mL(21.34 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 4.2673 mL | 21.3365 mL | 42.6730 mL | 5 mM | 0.8535 mL | 4.2673 mL | 8.5346 mL | 10 mM | 0.4267 mL | 2.1337 mL | 4.2673 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 4.35 mg/mL (18.56 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.67 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.67 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.67 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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