1. 诱导疾病模型产品 Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  2. 免疫与炎症疾病模型 Na+/K+ ATPase Endogenous Metabolite
  3. 半抗原
  4. Digoxin

Digoxin  (Synonyms: 地高辛; 12β-Hydroxydigitoxin)

目录号: HY-B1049 纯度: 99.71%
COA 产品使用指南

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。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Digoxin Chemical Structure

Digoxin Chemical Structure

CAS No. : 20830-75-5

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
100 mg ¥780
In-stock
500 mg ¥1560
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

Na+/K+ ATPase[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
50 nM
Compound: Digoxin
Cytotoxicity against human A549 cells after 3 days by MTT assay
Cytotoxicity against human A549 cells after 3 days by MTT assay
[PMID: 23706005]
B16-F10 IC50
> 10000 nM
Compound: Digoxin
Cytotoxicity against mouse B16F10 cells after 3 days by MTT assay
Cytotoxicity against mouse B16F10 cells after 3 days by MTT assay
[PMID: 23706005]
BT-549 IC50
0.051 μM
Compound: Digoxin
Cytotoxicity against human BT-549 cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human BT-549 cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
CAL-51 IC50
0.13 μM
Compound: Digoxin
Cytotoxicity against human CAL-51 cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human CAL-51 cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
Cancer cell lines IC50
0.1 μM
Compound: 3
Cytotoxicity against human colon cancer cells after 72 hrs by FMCA method
Cytotoxicity against human colon cancer cells after 72 hrs by FMCA method
[PMID: 19894733]
CT26.WT IC50
> 10000 nM
Compound: Digoxin
Cytotoxicity against mouse CT26.WT cells after 3 days by MTT assay
Cytotoxicity against mouse CT26.WT cells after 3 days by MTT assay
[PMID: 23706005]
D283 Med IC50
10 nM
Compound: Digoxin
Anticancer activity against human D283 Med cells assessed as reduction in cell viability incubated for 72 hrs
Anticancer activity against human D283 Med cells assessed as reduction in cell viability incubated for 72 hrs
[PMID: 33636537]
HCC1806 IC50
0.28 μM
Compound: Digoxin
Cytotoxicity against human HCC1806 cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human HCC1806 cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
HCC1937 IC50
0.55 μM
Compound: Digoxin
Cytotoxicity against human HCC1937 cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human HCC1937 cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
HCC70 IC50
0.64 μM
Compound: Digoxin
Cytotoxicity against human HCC70 cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human HCC70 cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
HCT-116 IC50
0.27 μM
Compound: 3
Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method
Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method
[PMID: 19894733]
HeLa IC50
2.2 μM
Compound: digoxin
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
[PMID: 26122772]
Hs 683 IC50
40 nM
Compound: Digoxin
Cytotoxicity against human Hs683 cells after 3 days by MTT assay
Cytotoxicity against human Hs683 cells after 3 days by MTT assay
[PMID: 23706005]
Hs-578T IC50
0.069 μM
Compound: Digoxin
Cytotoxicity against human Hs-578T cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human Hs-578T cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
Hs-578T IC50
0.251 μM
Compound: digoxin
Cytotoxicity against human Hs578T cells after 72 hrs by CellTiter-Glo assay
Cytotoxicity against human Hs578T cells after 72 hrs by CellTiter-Glo assay
[PMID: 22316168]
Hs-578T IC50
93.5 μM
Compound: digoxin
Cytotoxicity against human Hs578T cells at 40 uM after 72 hrs by CellTiter-Glo assay relative to untreated control
Cytotoxicity against human Hs578T cells at 40 uM after 72 hrs by CellTiter-Glo assay relative to untreated control
[PMID: 22316168]
HT-29 IC50
0.28 μM
Compound: 1
Cytotoxicity against human HT-29 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
Cytotoxicity against human HT-29 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
[PMID: 32096998]
HT-29 IC50
1.4 μM
Compound: 3
Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method
Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method
[PMID: 19894733]
HT-29 IC50
380 nM
Compound: Digoxin
Cytotoxicity against human HT-29 cells incubated for 72 hrs by SRB assay
Cytotoxicity against human HT-29 cells incubated for 72 hrs by SRB assay
[PMID: 27983842]
K562 IC50
28.2 nM
Compound: 3
Cytotoxicity against human K562 cells by XTT assay
Cytotoxicity against human K562 cells by XTT assay
[PMID: 16309315]
Kasumi 1 IC50
93 nM
Compound: Digoxin
Cytotoxicity against human Kasumi-1 cells incubated for 48 hrs by MTS assay
Cytotoxicity against human Kasumi-1 cells incubated for 48 hrs by MTS assay
[PMID: 27983842]
LLC-PK1 IC50
> 50 μM
Compound: Digoxin
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
> 50 μM
Compound: Digoxin
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
> 50 μM
Compound: Digoxin
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
MCF7 IC50
24.1 nM
Compound: 3
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
[PMID: 16309315]
MCF7 IC50
4.7 μM
Compound: digoxin
Cytotoxicity against human MCF7 cells after 72 hrs by CellTiter-Glo assay
Cytotoxicity against human MCF7 cells after 72 hrs by CellTiter-Glo assay
[PMID: 22316168]
MCF7 IC50
426 nM
Compound: Digoxin
Cytotoxicity against human MCF7 cells after 3 days by MTT assay
Cytotoxicity against human MCF7 cells after 3 days by MTT assay
[PMID: 23706005]
MDA-MB-231 IC50
0.31 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
[PMID: 32096998]
MDA-MB-231 IC50
0.48 μM
Compound: Digoxin
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
MDA-MB-435 IC50
0.17 μM
Compound: 1
Cytotoxicity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
Cytotoxicity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
[PMID: 32096998]
MDA-MB-453 IC50
0.23 μM
Compound: Digoxin
Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
MDA-MB-468 IC50
0.23 μM
Compound: Digoxin
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
MV4-11 IC50
111 nM
Compound: Digoxin
Cytotoxicity against human MV4-11 cells incubated for 48 hrs by MTS assay
Cytotoxicity against human MV4-11 cells incubated for 48 hrs by MTS assay
[PMID: 27983842]
NCI-H1299 IC50
0.46 μM
Compound: 1
Cytotoxicity against human NCI-H1299 cells after 24 hrs by MTT assay
Cytotoxicity against human NCI-H1299 cells after 24 hrs by MTT assay
[PMID: 32096998]
NCI-H1299 IC50
460 nM
Compound: Digoxin
Cytotoxicity against human H1299 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human H1299 cells incubated for 24 hrs by MTT assay
[PMID: 27983842]
OVCAR-3 IC50
0.1 μM
Compound: 1
Cytotoxicity against human OVCAR3 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
Cytotoxicity against human OVCAR3 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
[PMID: 32096998]
PBMC IC50
> 20 μM
Compound: Digoxin
Cytotoxicity against human PBMC incubated for 48 hrs by MTS assay
Cytotoxicity against human PBMC incubated for 48 hrs by MTS assay
[PMID: 27983842]
PC-3 IC50
75 nM
Compound: Digoxin
Cytotoxicity against human PC3 cells after 3 days by MTT assay
Cytotoxicity against human PC3 cells after 3 days by MTT assay
[PMID: 23706005]
S2 IC50
2 μM
Compound: Digoxin
Inhibition of mouse Gal4 DNA binding domain-fused ROR gamma expressed in Drosophila S2 cells assessed as inhibition of transcriptional activity by luciferase reporter assay
Inhibition of mouse Gal4 DNA binding domain-fused ROR gamma expressed in Drosophila S2 cells assessed as inhibition of transcriptional activity by luciferase reporter assay
10.1039/C3MD00005B
SK-BR-3 IC50
1.08 μM
Compound: digoxin
Cytotoxicity against human SK-BR-3 cells after 72 hrs by CellTiter-Glo assay
Cytotoxicity against human SK-BR-3 cells after 72 hrs by CellTiter-Glo assay
[PMID: 22316168]
SK-MEL-28 IC50
266 nM
Compound: Digoxin
Cytotoxicity against human SK-MEL-28 cells after 3 days by MTT assay
Cytotoxicity against human SK-MEL-28 cells after 3 days by MTT assay
[PMID: 23706005]
SUM185PE IC50
0.28 μM
Compound: Digoxin
Cytotoxicity against human SUM185PE cells assessed as reduction in cell viability after 48 hrs by SRB assay
Cytotoxicity against human SUM185PE cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 32649211]
T47D IC50
0.66 μM
Compound: digoxin
Cytotoxicity against human T47D cells after 72 hrs by CellTiter-Glo assay
Cytotoxicity against human T47D cells after 72 hrs by CellTiter-Glo assay
[PMID: 22316168]
TK-10 IC50
14.6 nM
Compound: 3
Cytotoxicity against human TK10 cells after 48 hrs by SRB assay
Cytotoxicity against human TK10 cells after 48 hrs by SRB assay
[PMID: 16309315]
U-373MG ATCC IC50
146 nM
Compound: Digoxin
Cytotoxicity against human U373 cells after 3 days by MTT assay
Cytotoxicity against human U373 cells after 3 days by MTT assay
[PMID: 23706005]
UACC-62 IC50
29.5 nM
Compound: 3
Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay
Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay
[PMID: 16309315]
Vero CC50
> 50 μM
Compound: Digoxin
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
Vero IC50
0.19 μM
Compound: Digoxin
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
体外研究
(In Vitro)

Digoxin 是一种钠钾 ATP 酶抑制剂,其 Z 评分为负值-26.67,表明钠钾 ATP 酶在 CHIKV 感染中发挥作用。相对于 DMSO 处理的细胞,Digoxin 处理 U-2 OS 细胞导致 CHIKV 感染呈剂量依赖性降低,半数最大有效浓度 (EC50) 为 48.8 nM。Digoxin 处理同样降低了原代人滑膜成纤维细胞 (HSF) 和 Vero 非洲绿猴肾细胞的 CHIKV 感染,EC50 分别为 43.9 nM 和 67.3 nM。Digoxin 处理可显著减少这些细胞类型中的 CHIKV 感染,ST2 细胞中的 EC50 为 16.2 μM,C2C12 细胞中的 EC50 为 23.2 μM,分别是 EC50 的 330 和 475 倍U-2 OS 细胞中的 Digoxin。使用 1 μM Digoxin 处理 24 小时后,细胞活力仅受到轻微损害,该剂量是这些细胞中 CHIKV 抗病毒活性 Digoxin EC50 的 20 倍[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
性状

固体

颜色

White to off-white

中文名称

地高辛;异羟洋地黄毒苷

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 62.5 mg/mL (80.03 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    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); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    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。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

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

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.71%

参考文献
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

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2805 mL 6.4025 mL 12.8051 mL 32.0127 mL
5 mM 0.2561 mL 1.2805 mL 2.5610 mL 6.4025 mL
10 mM 0.1281 mL 0.6403 mL 1.2805 mL 3.2013 mL
15 mM 0.0854 mL 0.4268 mL 0.8537 mL 2.1342 mL
20 mM 0.0640 mL 0.3201 mL 0.6403 mL 1.6006 mL
25 mM 0.0512 mL 0.2561 mL 0.5122 mL 1.2805 mL
30 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0671 mL
40 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8003 mL
50 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6403 mL
60 mM 0.0213 mL 0.1067 mL 0.2134 mL 0.5335 mL
80 mM 0.0160 mL 0.0800 mL 0.1601 mL 0.4002 mL
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