Digitoxin

Name: Digitoxin
Brand: MedChemExpress
SKU: HY-B1357
Rating: 5.0 (6 reviews)

Cat. No.: HY-B1357 Purity: 99.36%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .

For research use only. We do not sell to patients.

Digitoxin Chemical Structure

CAS No. : 71-63-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 42	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 42	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 25	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 33	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 74	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 101	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Digitoxin:

Gitoxin Get quote
Digitoxin-d₃ Get quote
Digitoxin (Standard) Get quote

6 Publications Citing Use of MCE Digitoxin

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Bcl-2

Caspase-9

Caspase 3

Bax

HSV-1

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.44 μM Compound: digitoxin	Cytotoxicity against human A549 cells after 72 hrs by calcein AM assay Cytotoxicity against human A549 cells after 72 hrs by calcein AM assay	[PMID: 16309329]
Cancer cell lines	IC₅₀	0.1 μM Compound: 2	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]
DU-145	IC₅₀	0.44 μM Compound: digitoxin	Cytotoxicity against human DU145 cells after 72 hrs by calcein AM assay Cytotoxicity against human DU145 cells after 72 hrs by calcein AM assay	[PMID: 16309329]
HCT-116	IC₅₀	0.44 μM Compound: digitoxin	Cytotoxicity against human HCT116 cells after 72 hrs by calcein AM assay Cytotoxicity against human HCT116 cells after 72 hrs by calcein AM assay	[PMID: 16309329]
HCT-116	IC₅₀	0.74 μM Compound: 2	Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method	[PMID: 19894733]
Hep 3B2	IC₅₀	0.44 μM Compound: digitoxin	Cytotoxicity against human Hep3B cells after 72 hrs by calcein AM assay Cytotoxicity against human Hep3B cells after 72 hrs by calcein AM assay	[PMID: 16309329]
HFF	CC₅₀	2.8 μM Compound: 1	Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by MTT assay Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by MTT assay	[PMID: 24900847]
HFF	CC₅₀	6 μM Compound: 1	Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by trypan blue exclusion assay Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by trypan blue exclusion assay	[PMID: 24900847]
HT-29	IC₅₀	0.068 μM Compound: (+)-Digitoxin	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	4.07 μM Compound: 2	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	67.6 nM Compound: Digitoxin	Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 28234008]
K562	IC₅₀	6.4 nM Compound: 1	Cytotoxicity against human K562 cells by XTT assay Cytotoxicity against human K562 cells by XTT assay	[PMID: 16309315]
KURAMOCHI	IC₅₀	5911 nM Compound: Digitoxin	Antiproliferative activity against human Kuramochi cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human Kuramochi cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 28234008]
MCF7	IC₅₀	0.02 μM Compound: 1, DT	Antiproliferative activity against human MCF7 cells assessed as cell viability treated for 48 hrs followed by compound washout measured after 72 hrs by fluorometric CellTiter-Blue reagent assay Antiproliferative activity against human MCF7 cells assessed as cell viability treated for 48 hrs followed by compound washout measured after 72 hrs by fluorometric CellTiter-Blue reagent assay	[PMID: 21421322]
MCF7	IC₅₀	0.44 μM Compound: digitoxin	Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM assay Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM assay	[PMID: 16309329]
MCF7	IC₅₀	10.2 nM Compound: 1	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 16309315]
MDA-MB-231	IC₅₀	0.48 μM Compound: (+)-Digitoxin	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	482 nM Compound: Digitoxin	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 28234008]
MDA-MB-435	IC₅₀	0.043 μM Compound: (+)-Digitoxin	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-435	IC₅₀	43.3 nM Compound: Digitoxin	Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 28234008]
NCI/ADR-RES	IC₅₀	0.44 μM Compound: digitoxin	Cytotoxicity against human NCI/ADR-RES cells after 72 hrs by calcein AM assay Cytotoxicity against human NCI/ADR-RES cells after 72 hrs by calcein AM assay	[PMID: 16309329]
NCI-H460	IC₅₀	0.44 μM Compound: digitoxin	Cytotoxicity against human NCI-H460 cells after 72 hrs by calcein AM assay Cytotoxicity against human NCI-H460 cells after 72 hrs by calcein AM assay	[PMID: 16309329]
NCI-H460	GI₅₀	10.7 nM Compound: 1	Growth inhibition of human NCI-H460 cells after 48 hrs by MTT assay Growth inhibition of human NCI-H460 cells after 48 hrs by MTT assay	[PMID: 21643465]
NCI-H460	IC₅₀	357 nM Compound: 1	Cytotoxicity against human NCI-H460 cells assessed as cell death at 50 nM after 12 hrs by Hoechst-33342 staining and propidium iodide staining Cytotoxicity against human NCI-H460 cells assessed as cell death at 50 nM after 12 hrs by Hoechst-33342 staining and propidium iodide staining	[PMID: 21643465]
OVCAR-3	IC₅₀	0.12 μM Compound: (+)-Digitoxin	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]
OVCAR-3	IC₅₀	117.1 nM Compound: Digitoxin	Antiproliferative activity against human OVCAR3 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human OVCAR3 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 28234008]
OVCAR-4	IC₅₀	425.6 nM Compound: Digitoxin	Antiproliferative activity against human OVCAR4 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human OVCAR4 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 28234008]
OVCAR-5	IC₅₀	321 nM Compound: Digitoxin	Antiproliferative activity against human OVCAR5 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human OVCAR5 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 28234008]
OVCAR-8	IC₅₀	71.5 nM Compound: Digitoxin	Antiproliferative activity against human OVCAR8 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human OVCAR8 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 28234008]
SF-268	IC₅₀	0.44 μM Compound: digitoxin	Cytotoxicity against human SF268 cells after 72 hrs by calcein AM assay Cytotoxicity against human SF268 cells after 72 hrs by calcein AM assay	[PMID: 16309329]
SK-OV-3	IC₅₀	0.44 μM Compound: digitoxin	Cytotoxicity against human SKOV3 cells after 72 hrs by calcein AM assay Cytotoxicity against human SKOV3 cells after 72 hrs by calcein AM assay	[PMID: 16309329]
TK-10	IC₅₀	3.2 nM Compound: 1	Cytotoxicity against human TK10 cells after 48 hrs by SRB assay Cytotoxicity against human TK10 cells after 48 hrs by SRB assay	[PMID: 16309315]
UACC-62	IC₅₀	33.5 nM Compound: 1	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	IC₅₀	< 0.23 μM Compound: Digitoxin	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
Vero	CC₅₀	> 50 μM Compound: Digitoxin	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

In Vitro

Digitoxin (0-80 nM, 72 h) compromised cell survival in PC12 cells^[1].
Digitoxin (4-1000 nM, 24-48 h) has an antitumor effects in MHCC97H, A549, HCT116 and HeLa cells^[3].
Digitoxin (4-100 nM, 24-48 h) disrupts the cell cycle in HeLa cells^[3].
Digitoxin (20-500 nM, 48 h) activates mitochondrial apoptosis in HeLa cells^[3].

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

Cell Viability Assay^[3]

Cell Line:	MHCC97H, A549, HCT116 and HeLa cells
Concentration:	4-1000 nM
Incubation Time:	24 h, 48 h
Result:	Dcreased the viability of these cancer cells in a dose- and time-dependent manner, with the IC₅₀ values ranging from 0.075 to 0.395 µM following digitoxin treatment for 24 h and from 0.028 to 0.077 µM following digitoxin treatment for 48 h.

Cell Cycle Analysis^[3]

Cell Line:	HeLa cells
Concentration:	4 nM, 20 nM, 100 nM
Incubation Time:	24 h, 36 h, 48 h
Result:	Increased cell population in the G2/M phase from 16.27 to 18.36, 23.46 and 31.51% at concentrations of 20 nM for12, 24 and 36 h. Increased average cell population in the G2/M phase from 16.27 to 28.07% at concentrations of 4, 20 and 100 nM for 24 h. Significantly decreased the protein expression levels of total CDK1 and phosphorylated CDK1.

Apoptosis Analysis^[3]

Cell Line:	HeLa cells
Concentration:	20 nM, 100 nM, 500 nM
Incubation Time:	48 h
Result:	Upregulated Bax expression and unaltered Bcl-2 expression. Significantly increased the expression of cytochrome c.

In Vivo

Digitoxin (1-2 mg/kg, Intraperitoneal injection, once a day for 19 days) has anticancer effects in nude mice^[3].
Digitoxin (0.3-3 μg/kg, Intraperitoneal injection, once a day for 4 days) blocks the host over-production of cytokines in the cotton rat lung^[4].

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

Animal Model:	nude mice harboring HeLa tumor xenografts^[3]
Dosage:	1 mg/kg, 2 mg/kg
Administration:	Intraperitoneal injection (i.p.)
Result:	Decreased the tumor volume from 330.71±45.61 to 214.56.93±73.25 mm. Strongly increased the protein levels of cleaved caspase-3. Reduced the number of Ki-67-positive cells.

Animal Model:	cotton rats^[4]
Dosage:	0.3 μg/kg, 1 μg/kg, 3 μg/kg
Administration:	Intraperitoneal injection (i.p.)
Result:	Blocked cytokine storm. Differentially affected cytokine expression. Left immune cell density intact in virus-infected lung.

Clinical Trial

Molecular Weight

764.94

Formula

C₄₁H₆₄O₁₃

CAS No.

71-63-6

Appearance

Solid

Color

White to off-white

SMILES

C[C@H]1O[C@](O[C@@H]2[C@@H](C)O[C@](O[C@H]3[C@@H](O)C[C@@](O[C@@H]4C[C@](CC[C@]5([H])[C@]6([H])CC[C@@]7(C)[C@]5(O)CC[C@@H]7C(CO8)=CC8=O)([H])[C@]6(C)CC4)([H])O[C@@H]3C)([H])C[C@@H]2O)([H])C[C@H](O)[C@@H]1O

Structure Classification

Steroids

Initial Source

Microorganisms

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (130.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3073 mL	6.5365 mL	13.0729 mL
5 mM	0.2615 mL	1.3073 mL	2.6146 mL
10 mM	0.1307 mL	0.6536 mL	1.3073 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.36%

Select Batch:

Data Sheet (281 KB) SDS (644 KB)

COA (250 KB) HNMR (329 KB) LCMS (253 KB)

Handling Instructions (2659 KB)

References

[1]. Arispe N, et al. Heart failure drug digitoxin induces calcium uptake into cells by forming transmembrane calcium channels [J]. Proceedings of the National Academy of Sciences, 2008, 105(7): 2610-2615. [Content Brief]

[2]. Su C T, Hsu J T A, Hsieh H P, et al. Anti-HSV activity of digitoxin and its possible mechanisms [J]. Antiviral research, 2008, 79(1): 62-70.

[3]. Gan H, Qi M, Chan C, et al. Digitoxin inhibits HeLa cell growth through the induction of G2/M cell cycle arrest and apoptosis in vitro and in vivo [J]. International Journal of Oncology, 2020, 57(2): 562-573.

[4]. Pollard B S, Blanco J C, Pollard J R. Classical drug digitoxin inhibits influenza cytokine storm, with implications for COVID-19 therapy [J]. in vivo, 2020, 34(6): 3723-3730.

[5]. Haux J. Digitoxin is a potential anticancer agent for several types of cancer [J]. Medical hypotheses, 1999, 53(6): 543-548.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.3073 mL	6.5365 mL	13.0729 mL	32.6823 mL
	5 mM	0.2615 mL	1.3073 mL	2.6146 mL	6.5365 mL
	10 mM	0.1307 mL	0.6536 mL	1.3073 mL	3.2682 mL
	15 mM	0.0872 mL	0.4358 mL	0.8715 mL	2.1788 mL
	20 mM	0.0654 mL	0.3268 mL	0.6536 mL	1.6341 mL
	25 mM	0.0523 mL	0.2615 mL	0.5229 mL	1.3073 mL
	30 mM	0.0436 mL	0.2179 mL	0.4358 mL	1.0894 mL
	40 mM	0.0327 mL	0.1634 mL	0.3268 mL	0.8171 mL
	50 mM	0.0261 mL	0.1307 mL	0.2615 mL	0.6536 mL
	60 mM	0.0218 mL	0.1089 mL	0.2179 mL	0.5447 mL
	80 mM	0.0163 mL	0.0817 mL	0.1634 mL	0.4085 mL
	100 mM	0.0131 mL	0.0654 mL	0.1307 mL	0.3268 mL

Digitoxin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Digitoxin

Customer Review

Other Forms of Digitoxin:

6 Publications Citing Use of MCE Digitoxin

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Digitoxin

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Digitoxin Related Antibodies

6 Publications Citing Use of MCE Digitoxin

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View All Bcl-2 Family Isoform Specific Products:

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View All HSV Isoform Specific Products:

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Biological Activity

Purity & Documentation

References

Customer Review

Digitoxin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Digitoxin Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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