Digoxin(Synonyms: 12β-Hydroxydigitoxin)

天然产物 糖类和糖苷 Saccharides and Glycosides

Digoxin;(Synonyms: 12β-Hydroxydigitoxin) 纯度: 98.92%

Digoxin是 Na+/K+-ATPase 的有效抑制剂,有潜力用于心律失常和心力衰竭的研究。

Digoxin(Synonyms: 12β-Hydroxydigitoxin)

Digoxin Chemical Structure

CAS No. : 20830-75-5

规格 价格 是否有货 数量
100 mg ¥780 In-stock
500 mg ¥1560 In-stock
1 g ; 询价 ;
5 g ; 询价 ;

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生物活性

Digoxin is a potent inhibitor of Na+/K+-ATPase, has the potential for arrhythmia and heart failure treatment.

IC50 Target

Human Endogenous Metabolite

;

体外研究
(In Vitro)

Digoxin, a sodium-potassium ATPase inhibitor, has a negative Z score of −26.67, suggesting a function for the sodium-potassium ATPase in CHIKV infection. Relative to DMSO-treated cells, treatment of U-2 OS cells with Digoxin results in a dose-dependent decrease in CHIKV infection with a half-maximal effective concentration (EC50) of 48.8 nM. Digoxin treatment similarly decreases CHIKV infection of primary human synovial 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 of 16.2 µM in ST2 cells and 23.2 µM in C2C12 cells, values 330 and 475 times the EC50 of Digoxin in U-2 OS cells. Cell viability is only modestly impaired at 24 h posttreatment with 1 µM Digoxin, a dose 20 times the Digoxin EC50 for CHIKV antiviral activity in these cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

780.94

Formula

C41H64O14

CAS 号

20830-75-5

中文名称

地高辛;异羟洋地黄毒苷

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4deg;C, protect from light

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light)

溶解性数据
In Vitro:;

DMSO : 62.5 mg/mL (80.03 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2805 mL 6.4025 mL 12.8051 mL
5 mM 0.2561 mL 1.2805 mL 2.5610 mL
10 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方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,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (2.66 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (2.66 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.66 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.66 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Ashbrook AW, et al. Antagonism of the Sodium-Potassium ATPase Impairs Chikungunya Virus Infection. MBio. 2016 May 24;7(3). pii: e00693-16.

Cell Assay
[1]

U-2 OS cells seeded in 60-mm-diameter dishes are incubated with DMSO, 10 µM STS as an inducer of apoptosis, or increasing concentrations of Digoxin at 37°C 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 a BD LSRII flow cytometer and FlowJo software. Alternatively, U-2 OS cells seeded in 96-well plates are incubated with DMSO, STS, or increasing concentrations of Digoxin at 37°C for 6 or 24 h. PrestoBlue reagent is added to supernatants of compound-treated cells, and cells are incubated at 37°C for 30 min. Fluorescence as a surrogate for cell viability is quantified using a Synergy H1 plate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Ashbrook AW, et al. Antagonism of the Sodium-Potassium ATPase Impairs Chikungunya Virus Infection. MBio. 2016 May 24;7(3). pii: e00693-16.

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