鹽酸利多卡因作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetLidocaine hydrochlorideCat. No.: HY-B0185ACAS No.: 73-78-9分式: CHClNO分量: 270.8作靶點(diǎn): Sodium Channel; MEK; ERK; NF-B; Apoptosis作通路: Membrane Transporter/Ion Channel; MAPK/ERK Pathway; Stem Cell/Wnt; NF-B;Apoptosis儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (

2、protect from light)溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 100 mg/mL (369.28 mM)DMSO : 100 mg/mL (369.28 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 3.6928 mL 18.4638 mL 36.9276 mL5 mM 0.7386 mL 3.6928 mL 7.3855 mL10 mM 0.3693 mL 1.8464 mL 3.6928 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液

3、；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助

4、溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.23 mM); Clear solution此案可獲得 2.5 mg/mL (9.23 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in sal

5、ine)Solubility: 2.5 mg/mL (9.23 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (9.23 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.23 mM); Clear solution此案可獲得 2.5 mg/mL (9.23 mM，飽和度未知

6、) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Lidocaine hydrochloride (Lignocaine hydrochloride) 抑制涉及復(fù)雜電壓和依賴性的鈉通道 (sodium channels)。Lidocaine hydrochloride 通過(guò)調(diào)節(jié) miR-145 表達(dá)和進(jìn)步抑制 MEK/ERK 和 NF-B 信號(hào)通路來(lái)減少胃癌細(xì)胞的長(zhǎng)，遷移和侵襲。Lidocaine hydrochloride 種

7、酰胺衍物常于局部醉。Lidocaine hydrochloride 種治療室性 律失常的藥物和有效的腫瘤抑制劑。IC & Target MEK ERK NF-B體外研究Lidocaine hydrochloride (Lignocaine hydrochloride) (10 nM; 48 hours) decreases significantly cell proliferation2.Lidocaine hydrochloride (1-10 nM; 24-72 hours) inhibits cell viability and achieves the most suppressin

8、g effects at theconcentration of 10 nM and treatment time 48 hours2.Lidocaine hydrochloride (10 nM; 48 hours) increases significantly the apoptotic cell rate2.Lidocaine hydrochloride (10 nM; 48 hours) down-regulates Cyclin D1 and up-regulates p21 expression significantly2.Cell Proliferation Assay2Ce

9、ll Line: The human gastric cancer cell line MKN45Concentration: 10 nMIncubation Time: 48 hoursResult: Decreased significantly cell proliferation.Cell Viability Assay2Cell Line: The human gastric cancer cell line MKN45Concentration: 1, 5 and 10 nMIncubation Time: 24, 48, 72 hoursResult: Inhibited MKN

10、45 cell viability.Apoptosis Analysis2Cell Line: The human gastric cancer cell line MKN45Concentration: 10 nMIncubation Time: 48 hoursResult: Increased significantly the apoptotic cell rate.Page 2 of 3 www.MedChemEWestern Blot Analysis2Cell Line: The human gastric cancer cell line MKN45Concentration:

11、 10 nMIncubation Time: 48 hoursResult: Down-regulated Cyclin D1 and up-regulated p21 expression significantly.體內(nèi)研究 Lidocaine hydrochloride (Lignocaine hydrochloride) causes completely reversible tail nerve block in rats. Mechanicalnociception block produced by lidocaine has slower onset and faster r

12、ecovery compared with thermal nociception block3.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Neuroinflammation. 2017 Nov 2;14(1):211. J Phys D Appl Phys. 2019 Aug.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Cummins TR, et al. Setting up for the block: the mechanism underlying lidocaines use-d

13、ependent inhibition of sodium channels. J Physiol. 2007 Jul1;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 Mar15;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. 2013Jul;113(1):31-6.McePdfHeightCaution: P