盐酸维拉帕米作用机制 - Medchemexpress - MCE中国

1、Product Data SheetVerapamil hydrochlorideCat. No.: HY-A0064CAS No.: 152-11-4分式: CHClNO分量: 491.06作靶点: Calcium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 DMSO : 31 mg/mL (63.13 mM

2、)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.0364 mL 10.1821 mL 20.3641 mL5 mM 0.4073 mL 2.0364 mL 4.0728 mL10 mM 0.2036 mL 1.0182 mL 2.0364 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from l

3、ight)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 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 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.0

4、9 mM); Clear solution此案可获得 2.5 mg/mL (5.09 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.09 mM); Clear solution此案可获得 2.5 mg/mL (5.09 mM，饱和度未知)

5、的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合Page 1 of 2 www.MedChemE均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.09 mM); Clear solution此案可获得 2.5 mg/mL (5.09 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合

6、均匀。BIOLOGICAL ACTIVITY物活性 Verapamil hydrochloride ()-Verapamil hydrochloride)钙离通道 (calcium channel) 拮抗剂。IC & Target Calcium channel1体外研究 Verapamil (hydrochloride) is an L-type calcium channel antagonist. The combination of Bortezomib and Verapamil (70M) markedly declines the viability of the JK-6L,

7、RPMI 8226, and ARH-77 cell lines after 16 hours of culture1. Theenzyme hydrolase activity of recombinant human carboxylesterase (CES2) is substantially inhibited by Verapamil withKi of 3.840.99M2.体内研究 Verapamil, a calcium channel antagonist, is injected i.v. into a femoral vein prior to ischemia. Ve

8、rapamil (1 mg/kg)significantly decreases the incidence of ventricular arrhythmias including premature ventricular contractions (PVC),ventricular tachycardia (VT) and ventricular fibrillation (VF) for 45-min coronary artery occlusion. Total arrhythmiascores are significantly increased when the heart

9、is subjected to ischemia (P0.01 vs. sham). Verapamil (1 mg/kg)significantly prevented the enhancement of total arrhythmia scores induced by ischemia (P0.01 vs. ischemia). Resultsindicate that Verapamil exerts an anti-arrhythmic property3.PROTOCOLCell Assay 1 Cells (1105) are treated with 10 nM Borte

10、zomib and/or 70 M Verapamil for 16 hours and incubated for another 4hours with Alamar-Blue. Activity of the mitochondrial dehydrogenase results in conversion of the coloring, which isfollowed by measurement of the absorption using a spectrophotometer1.MCE has not independently confirmed the accuracy

11、 of these methods. They are for reference only.Animal Rats3Administration 3 Adult male Sprague-Dawley (SD) rats (250350 g) are used. Verapamil (1 mg/kg) is injected i.v. into a femoral vein 10min prior to ischemia. A sham group undergoes the same surgical procedures, except the suture underneath the

12、 LADis left untied. In another series of experiment, arrhythmia is induced by Bay K8644, an L-type calcium channel agonist,at a dose of 0.1 mg/kg given i.v. into the FV. Verapamil (1 mg/kg) is administered 10 min prior to Bay K8644. Allinjections are performed within 30 sec.MCE has not independently

13、 confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cancer Cell. 2017 Apr 10;31(4):501-515.e8. Cancer Sci. 2018 Apr;109(4):1135-1146. J Pharm Anal. 2019 Sep.Page 2 of 3 www.MedChemE Phytomedicine. 2019 Mar 15;56:175-182. Cell Calcium. 2020 Feb.See more customer validati

14、ons on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Meister S, et al. Calcium channel blocker Verapamil enhances endoplasmic reticulum stress and cell death induced by proteasome inhibition in myelomacells. Neoplasia. 2010 Jul;12(7):550-61.2. Yanjiao X, et al. Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro. Drug Metab Pharmacokinet.2013;28(6):468-74.3. Zhou P, et al. Anti-arrhythmic effect of Verapamil is accompanied by preservation of cx43 protein in rat heart. PLoS One. 2013 Aug 12;8(8):e71567