盐酸利多卡因 T1144

Product Introduction
Bioactivity


英文名: Lidocaine hydrochloride

描述: Lidocaine hydrochloride (Lignocaine hydrochloride) 抑制涉及复杂电压和依赖性的钠通道。它通过调节 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，是一种研究室性心律失常的药物和有效的肿瘤抑制剂。

细胞实验: Cells at logarithmic phase are treated with lidocaine hydrochloride at concentrations (w/v) from 10 to 0.15625 g/l in step dilutions. HCE cells without lidocaine treatment are used as controls. The morphology and growing status of the cells are monitored every 4 hr.(Only for Reference)

体外活性: Lidocaine 浓度超过1.25 g/l时，可降低HCE细胞的存活率，并以时间和剂量依赖的方式触发凋亡。Lidocaine 诱导的凋亡是依赖于半胱天冬蛋白酶的，并可能与线粒体途径有关[1]。局部或局麻使用时，Lidocaine 在组织浓度水平上亦直接抑制表皮生长因子受体(EGFR)的活性（EGFR是癌细胞增殖的潜在抑制靶点）[3]。

体内活性: 静脉给予局麻药lidocaine多年来已被用于治疗神经病性疼痛，并显著改善由复杂脊柱手术和胆囊切除术后引起的疼痛。Lidocaine作为区域麻醉药，通过抑制电压门控钠（Na+）通道，阻断外周神经的冲动传递已得到确认。静脉注射lidocaine对机械性伤害反应具有镇痛效果，减少由外周夹捏刺激引起的脊髓伤害反应以及自发兴奋性突触后电流(EPSCs)的频率，但不改变其幅度。Lidocaine对自发抑制性突触后电流无影响，并在SG神经元中产生外向电流[2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (184.64 mM)
Ethanol : 54 mg/mL (199.41 mM)


关键字: Extracellular signal regulated kinases | Lidocaine | Mitogen-activated protein kinase kinase | Nuclear factor-kappaB | MEK | inhibit | Na channels | Na+ channels | Lignocaine Hydrochloride | MAPKK | Lignocaine | Nuclear factor-κB | NF-κB | Sodium Channel | Lidocaine hydrochloride | ERK | Inhibitor | MAP2K | Apoptosis | Lidocaine Hydrochloride

相关产品: Scopoletin | Masitinib | 6-Thioguanine | 3BDO | 1-beta-D-Arabinofuranosylthymine | CI-1040 | Voreloxin hydrochloride | ICCB280 | [6]-Gingerol | Enpp/Carbonic anhydrase-IN-2

相关库: Antioxidant Compound Library | Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途