Verapamil-hydrochloride-racemic-Verapamil-hydrochlorid-DataSheet-生命科學(xué)試劑-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作靶點(diǎn): Calcium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲(chǔ)存式: 4C, protect from light* In solven

2、t : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 31 mg/mL (63.13 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適

3、的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。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)娜芙獍福渲魄罢?qǐng)先配制澄的儲(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，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.09 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline

4、)Solubility: 2.5 mg/mL (5.09 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (5.09 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Verapamil hydrochloride鈣離通道 (calcium channel) 拮抗劑。IC50 & Target Calcium channel 1體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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 您邊的抑制劑師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