Verapamil-hydrochloride-racemic-Verapamil-hydrochlorid-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVerapamil hydrochlorideCat. No.: HY-A0064CAS No.: 152-11-4Synonyms: ()-Verapamil hydrochlorid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 solven

2、t : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 31 mg/mL (63.13 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration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

3、的溶剂配制储备液，并请注意储备液的保存式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.09 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline

4、)Solubility: 2.5 mg/mL (5.09 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.09 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Verapamil hydrochloride钙离通道 (calcium channel) 拮抗剂。IC50 & Target Calcium channel 1体外研究 Verapamil (h

5、ydrochloride) is an L-type calcium channel antagonist. The combination of Bortezomib andVerapamil (70 M) markedly declines the viability of the JK-6L, RPMI 8226, and ARH-77 cell lines after 16hours of culture 1. The enzyme hydrolase activity of recombinant human carboxylesterase (CES2) issubstantial

6、ly inhibited by Verapamil with Ki of 3.840.99M 2.体内研究 Verapamil, a calcium channel antagonist, is injected i.v. into a femoral vein prior to ischemia. Verapamil (1mg/kg) significantly decreases the incidence of ventricular arrhythmias including premature ventricularcontractions (PVC), ventricular ta

7、chycardia (VT) and ventricular fibrillation (VF) for 45-min coronary arteryocclusion. Total arrhythmia scores are significantly increased when the heart is subjected to ischemia (P 3.PROTOCOLCell Assay 1 Cells (1105) are treated with 10 nM Bortezomib and/or 70 M Verapamil for 16 hours and incubated

8、foranother 4 hours with Alamar-Blue. Activity of the mitochondrial dehydrogenase results in conversion of thecoloring, which is followed by measurement of the absorption using a spectrophotometer 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal

9、Rats 3Administration 3 Adult male Sprague-Dawley (SD) rats (250350 g) are used. Verapamil (1 mg/kg) is injected i.v. into afemoral vein 10 min prior to ischemia. A sham group undergoes the same surgical procedures, except thesuture underneath the LAD is left untied. In another series of experiment,

10、arrhythmia is induced by BayK8644, 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. All injections are performed within 30 sec.MCE has not independently confirmed the accuracy of these methods. They are fo

11、r 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. Phytomedicine. 2019 Mar 15;56:175-182. Mol Cell Endocrinol. 2019 Jun 14:110490. Toxicol Appl Pharmacol. 2019 Apr 1;368:18-25.See more customer validations on HYPERLINK / www.MedChemE2/3 Mas

12、ter of Small Molecules 您边的抑制剂师www.MedChemEREFERENCES1. Meister S, et al. Calcium channel blocker Verapamil enhances endoplasmic reticulum stress and cell death induced by proteasomeinhibition in myeloma cells. 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 MetabPharmacokinet. 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 Aug12;8(8):e71567.McePdfHei