Lidocaine hydrochloride(Synonyms: 盐酸利多卡因; Lignocaine hydrochloride)

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Lidocaine hydrochloride (Synonyms: 盐酸利多卡因; Lignocaine hydrochloride) 纯度: 99.81%

Lidocaine (Lignocaine) hydrochloride 抑制涉及复杂电压和依赖性的钠通道 (sodium channels)。Lidocaine hydrochloride 通过调节 miR-145 表达和进一步抑制 MEK/ERKNF-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。

Lidocaine hydrochloride(Synonyms: 盐酸利多卡因; Lignocaine hydrochloride)

Lidocaine hydrochloride Chemical Structure

CAS No. : 73-78-9

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生物活性

Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a drug to treat ventricular arrhythmia and an effective tumor-inhibitor[2].

IC50 & Target[1,2]

MEK

 

ERK

 

NF-κB

 

体外研究
(In Vitro)

Lidocaine hydrochloride (Lignocaine hydrochloride) (10 nM; 48 hours) decreases significantly cell proliferation[2].
Lidocaine hydrochloride (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 hydrochloride (10 nM; 48 hours) increases significantly the apoptotic cell rate[2].
Lidocaine hydrochloride (10 nM; 48 hours) down-regulates Cyclin D1 and up-regulates p21 expression significantly[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

Lidocaine hydrochloride (Lignocaine hydrochloride) 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

270.80

Formula

C14H23ClN2O

CAS 号

73-78-9

中文名称

盐酸利多卡因

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

H2O : ≥ 100 mg/mL (369.28 mM)

DMSO : ≥ 100 mg/mL (369.28 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6928 mL 18.4638 mL 36.9276 mL
5 mM 0.7386 mL 3.6928 mL 7.3855 mL
10 mM 0.3693 mL 1.8464 mL 3.6928 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 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: 120 mg/mL (443.13 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 (9.23 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.23 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.23 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.23 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.23 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.23 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Cummins TR, et al. Setting up for the block: the mechanism underlying lidocaine’s use-dependent inhibition of sodium channels. J Physiol. 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. 2019 Mar 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 Pharmacol Toxicol. 2013 Jul;113(1):31-6.

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