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Lidocaine
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很棒纯度: 99.95%
货号 T0468Cas号 137-58-6
别名 利多卡因, Xylocaine, Lignocaine, Alphacaine
Lidocaine (Alphacaine) 是一种酰胺衍生物，抑制涉及复杂电压和依赖性的钠通道，可用于研究室性心律失常。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
一键复制产品信息 很棒纯度: 99.95%
货号 T0468 别名 利多卡因, Xylocaine, Lignocaine, AlphacaineCas号 137-58-6
Lidocaine (Alphacaine) 是一种酰胺衍生物，抑制涉及复杂电压和依赖性的钠通道，可用于研究室性心律失常。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。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 500 mg | ¥ 326 | 现货 | |
| 5 g | ¥ 395 | 现货 | |
| 10 g | ¥ 662 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 395 | 现货 |
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产品介绍
Lidocaine AI Summary
Lidocaine exhibits diverse bioactivities and pharmacokinetic properties indicative of its potential therapeutic applications. It shows significant antiarrhythmic effects, demonstrated by its ability to reduce induced ventricular tachycardia (VT) and prolong the ventricular effective refractory period in various animal models, including dogs and guinea pigs. The compound affects cardiac electrophysiology by modulating the action potential duration and refractory period in canine Purkinje fibers and isolated right atria. Additionally, it impacts mean blood pressure during arrhythmias and has demonstrated local anesthetic activity in multiple assays, including in rat sciatic nerve models.
Pharmacokinetically, Lidocaine has an observed volume of distribution of 1.1 L/kg and an unbound plasma fraction of 0.3, suggesting moderate tissue distribution. It also shows a moderate octanol-water partition coefficient with log P values around 2.26 and variable permeability across different biological membranes, indicating balanced lipophilicity and potential for systemic absorption. The compound demonstrates efficient renal and hepatic clearance, with a total body clearance of 16.0 mL/min/kg.
Notably, Lidocaine exhibits inhibitory activity against several enzymes and receptors, including various voltage-gated sodium channels and calcium channels, which are crucial for its cardiac effects. It also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase at micromolar concentrations. The compound's interaction with neuronal sodium channels and ability to modulate Nav1.4, Nav1.7, and Nav1.3 channels further underscore its broad-spectrum bioactivity.
On the toxicity front, Lidocaine displays CNS toxicity in mice at higher doses, leading to ataxia and convulsions, and has an LD50 of 238.0 mg/kg, suggesting a narrow therapeutic window. However, the compound shows no significant hepatotoxicity, according to DILIps prediction scores. Its aqueous solubility (Log S value of -1.71) and intrinsic solubility of 3130.0 ug/mL imply moderate solubility, which is beneficial for formulation purposes.
Overall, Lidocaine demonstrates a comprehensive bioactivity profile suitable for developing antiarrhythmic and anesthetic therapies, with a need for careful dosing to mitigate potential CNS toxicities and optimize therapeutic efficacy..
Note: Summary generated by AI. Data source: ChEMBL 
生物活性
化学信息
储存&溶解度
| 产品描述 | Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx. |
| 靶点活性 | H1 receptor:>32 μM |
| 别名 | 利多卡因, Xylocaine, Lignocaine, Alphacaine |
| 分子量 | 234.34 |
| 分子式 | C14H22N2O |
| CAS No. | 137-58-6 |
| Smiles | N(C(CN(CC)CC)=O)C1=C(C)C=CC=C1C |
| 密度 | 1.026g/cm3 |
| 存储 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 250 mg/mL (1066.83 mM), Sonication is recommended.  H2O: 21.34 mM, Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (8.53 mM), Sonication is recommended. 请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||||||||||||
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H2O/DMSO
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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：
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 μL， 一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / 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 100 μL DMSO （ 母液浓度为 20 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： 取 100 μL DMSO 母液， 添加 400 μL PEG300 混匀澄清， 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 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。
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