Lidocaine
(Synonyms: 利多卡因; Lignocaine) 目录号 : GC17608
An Analytical Reference Standard
Cas No.:137-58-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Lidocaine (Lignocaine) inhibits sodium channels involving 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 of MEK/ERK and NF-κB signaling pathways. Lidocaine is a commonly used local anesthetics of amide derivative, a drug to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
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].
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].
References:
[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.
| Cell experiment [1,2]: | |
|
Cell lines |
Fresh bovine articular chondrocytes, sarcoplasmic reticulum |
|
Preparation method |
The solubility of this compound in DMSO is >11.7 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1% or 2% lidocaine, 30 minutes |
|
Applications |
Lidocaine (1%, 15-minute) decreased chondrocyte viability. Longer exposures to 1% and 2% lidocaine further reduced chondrocyte viability. Lidocaine (40 μM) showed reverse frequency-dependent depression of myocardial contractility. Lidocaine(40 μM, 100 μM) caused a marked depression of the late-peaking contractile responses, attributed to Ca2+ release from the sarcoplasmic reticulum. |
| Animal experiment [3]: | |
|
Animal models |
Dogs with 2-hour-old myocardial infarctions |
|
Dosage form |
Intravenous bolus injection, 2-8 μg/ml |
|
Application |
Lidocaine prolonged the Q-EG intervals in the infarcted zones of the heart 17-26% at peak effect, but it had no effect on the Q-EG intervals in the normal zone except for a slight (1.5%) prolongation shortly after the initial intravenous bolus injection. Lidocaine prolonged the effective refractory period of the infarcted zone 23% at peak effect but had no effect on the effective refractory period of the normal zone. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Karpie J C, Chu C R. Lidocaine exhibits dose-and time-dependent cytotoxic effects on bovine articular chondrocytes in vitro[J]. The American journal of sports medicine, 2007, 35(10): 1622-1627. [2]. Lynch III C. Depression of myocardial contractility in vitro by bupivacaine, etidocaine, and lidocaine[J]. Anesthesia & Analgesia, 1986, 65(6): 551-559. [3]. Kupersmith J, Antman E M, Hoffman B F. In vivo electrophysiological effects of lidocaine in canine acute myocardial infarction[J]. Circulation research, 1975, 36(1): 84-91. | |
| Cas No. | 137-58-6 | SDF | |
| 别名 | 利多卡因; Lignocaine | ||
| 化学名 | 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide | ||
| Canonical SMILES | CCN(CC)CC(=O)NC1=C(C=CC=C1C)C | ||
| 分子式 | C14H22N2O | 分子量 | 234.34 |
| 溶解度 | ≥ 11.7mg/mL in DMSO, ≥ 227.27mg/mL in EtOH | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.2673 mL | 21.3365 mL | 42.673 mL |
| 5 mM | 0.8535 mL | 4.2673 mL | 8.5346 mL |
| 10 mM | 0.4267 mL | 2.1337 mL | 4.2673 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet