Digoxin-12β-Hydroxydigitoxin-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDigoxinCat. No.: HY-B1049CAS No.: 20830-75-5Synonyms: 12-Hydroxydigitoxin分式: CHO分量: 780.94作靶点: Na+/K+ ATPase作通路: Membrane Transporter/Ion Channel储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fr

2、omlight)溶解性数据体外实验 DMSO : 28 mg/mL (35.85 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.2805 mL 6.4025 mL 12.8051 mL5 mM 0.2561 mL 1.2805 mL 2.5610 mL10 mM 0.1281 mL 0.6403 mL 1.2805 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，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

3、溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清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: 2.08 mg/mL (2.66 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (2.66 mM); Clear so

4、lution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (2.66 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 DigoxinNa+/K+-ATPase 的有效抑制剂，临床上于治疗律失常和衰竭。IC50 & Target Na+/K+ ATPase 1体外研究 Digoxin, a sodium-potassium ATPase inhibitor, has a negative Z s

5、core of 26.67, suggesting a function forthe sodium-potassium ATPase in CHIKV infection. Relative to DMSO-treated cells, treatment of U-2 OS cellswith Digoxin results in a dose-dependent decrease in CHIKV infection with a half-maximal effectiveconcentration (EC50) of 48.8 nM. Digoxin treatment simila

6、rly decreases CHIKV infection of primary humansynovial fibroblasts (HSFs) and Vero African green monkey kidney cells with EC50s of 43.9 nM and 67.3 nM,respectively. Digoxin treatment significantly diminishes CHIKV infection in these cell types, with EC50s of16.2 M in ST2 cells and 23.2 M in C2C12 ce

7、lls, values 330 and 475 times the EC50 of Digoxin in U-2 OScells. Cell viability is only modestly impaired at 24 h posttreatment with 1 M Digoxin, a dose 20 times theDigoxin EC50 for CHIKV antiviral activity in these cells 1.PROTOCOLCell Assay 1 U-2 OS cells seeded in 60-mm-diameter dishes are incub

8、ated with DMSO, 10 M STS as an inducer ofapoptosis, or increasing concentrations of Digoxin at 37C for 6 h. Cells are washed with fluorescence-activated cell sorter (FACS) buffer (PBS with 2% FBS) and stained with PI. Cell staining is quantified using aBD LSRII flow cytometer and FlowJo software. Al

9、ternatively, U-2 OS cells seeded in 96-well plates areincubated with DMSO, STS, or increasing concentrations of Digoxin at 37C for 6 or 24 h. PrestoBluereagent is added to supernatants of compound-treated cells, and cells are incubated at 37C for 30 min.Fluorescence as a surrogate for cell viability

10、 is quantified using a Synergy H1 plate reader 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cancer Biol Ther. 2019;20(1):52-64.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Ashbrook AW, et al. Antagonism of the Sodium-Potassium ATPase Impairs Chikungunya Virus Infection. MBio. 2016 May 24;7(3). pii:e00693-16.McePdfHeight Caution: Product has not been fully