Lidocaine-Lignocaine-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELidocaineCat. No.: HY-B0185CAS No.: 137-58-6Synonyms: Lignocaine分式: CHNO分量: 234.34作靶点: Sodium Channel; MEK; ERK; NF-B作通路: Membrane Transporter/Ion Channel; MAPK/ERK Pathway;Stem Cell/Wnt; NF-B储存式: 4C, protect from light* In solv

2、ent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 100 mg/mL (426.73 mM)H2O : 5 mg/mL (21.34 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.2673 mL 21.3365 mL 42.6730 mL5 mM 0.8535 mL 4.2673 mL 8.5346 mL10 mM 0.4267 mL 2.1337 mL 4

3、.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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.67 mM); Clear solution2. 请依序添加每种溶剂： 10%

4、 DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (10.67 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (10.67 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Lidocaine (Lignocaine) 抑制涉及复杂电压和依赖性的钠通道 (sodium channels)。Lidocai

5、ne 通过调节 miR-145 表达和进步抑制 MEK/ERK 和 NF-B 信号通路来减少胃癌细胞的长，迁移和侵袭。Lidocaine 种常的酰胺衍物局部醉剂，种治疗室性律失常的药物和有效的肿瘤抑制剂。IC50 & Target MEK ERK NF-B体外研究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 sup

6、pressing effects at theconcentration of 10nM and treatment time 48hours 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 2Cell Line: The human

7、gastric cancer cell line MKN45Concentration: 10nMIncubation Time: 48 hoursResult: Decreased significantly cell proliferation.Cell Viability Assay 2Cell Line: The human gastric cancer cell line MKN45Concentration: 1, 5 and 10nMIncubation Time: 24, 48, 72 hoursResult: Inhibited MKN45 cell viability.Ap

8、optosis Analysis 2Cell Line: The human gastric cancer cell line MKN45Concentration: 10nMIncubation Time: 48 hoursResult: Increased significantly the apoptotic cell rate.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEWestern Blot Analysis 2Cell Line: The human gastric cancer cell line MKN45Concentr

9、ation: 10nMIncubation Time: 48 hoursResult: Down-regulated Cyclin D1 and up-regulated p21 expression significantly.体内研究 Lidocaine (Lignocaine) causes completely reversible tail nerve block in rats. Mechanical nociception blockproduced by lidocaine has slower onset and faster recovery compared with t

10、hermal nociception block 3.户使本产品发表的科研献 J Neuroinflammation. 2017 Nov 2;14(1):211. J Phys D Appl Phys. 2019 Aug.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Cummins TR, et al. Setting up for the block: the mechanism underlying lidocaines use-dependent inhibition of sodium cha

11、nnels. JPhysiol. 2007 Jul 1;582(Pt 1):11.2. Sui H, et al. Lidocaine inhibits growth, migration and invasion of gastric carcinoma cells by up-regulation of miR-145. BMC Cancer. 2019Mar 15;19(1):233.3. Li Z, et al. Evaluation of the antinociceptive effects of lidocaine and bupivacaine on the tail nerves of healthy rats. Basic Clin PharmacolToxicol. 2013 Jul;113(1):31-6.McePdfHeightCaution: Product has