Home Transmembrane Transporters ATPase inhibitor Digoxin For research use only.

Digoxin

Synonyms: NSC 95100, 12β-Hydroxydigitoxin

Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.

Digoxin Chemical Structure

Digoxin Chemical Structure

CAS No. 20830-75-5

Purity & Quality Control

Digoxin Related Products

Signaling Pathway

ATPase Signaling Pathways

ATPase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
rat hepatocytes Function assay Drug uptake in rat hepatocytes, Km=0.18 μM 20926619
human hepatocytes Function assay 0.05 to 10 uM Drug uptake in sandwich-cultured human hepatocytes at 0.05 to 10 uM at 37 degC by Michaelis-Menten kinetics/scintillation spectroscopy, Km=2.39 μM 20926619
LLC-PK1 Function assay TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp2-expressing LLC-PK1 cells, Ki=0.037μM 11408557
High Five (BTI-TN5B1-4) Function assay TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells, Km=25.9μM 11785684
LLC-PK1 Function assay TP_TRANSPORTER: inhibition of Taurocholate uptake in Oatp2-expressing LLC-PK1 cells, Ki=0.58μM 11792694
LLC-PK1 Function assay TP_TRANSPORTER: uptake in Oatp2-expressing LLC-PK1 cells, Km=1.07μM 11792694
LLC-PK1 Function assay TP_TRANSPORTER: uptake in Oatp2-expressing LLC-PK1 cells, Km=0.279μM 11883641
MDCK Function assay TP_TRANSPORTER: cell accumulation in OATP4C1-expressing MDCK cells, Km=7.8μM 14993604
MDCK Function assay TP_TRANSPORTER: cell accumulation in OATP4C1-expressing MDCK cells, Km=8μM 14993604
TK10 Cytotoxicity assay 48 hrs Cytotoxicity against human TK10 cells after 48 hrs by SRB assay, IC50=0.0146μM 16309315
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, IC50=0.0241μM 16309315
K562 Cytotoxicity assay Cytotoxicity against human K562 cells by XTT assay, IC50=0.0282μM 16309315
UACC62 Cytotoxicity assay 48 hrs Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay, IC50=0.0295μM 16309315
HeLa Cytotoxicity assay Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis 18066055
HeLa Function assay Inhibition of mitosis in human HeLa cells by imaging analysis 18066055
colon cancer Cytotoxicity assay 72 hrs Cytotoxicity against human colon cancer cells after 72 hrs by FMCA method, IC50=0.1μM 19894733
CC20 Cytotoxicity assay 72 hrs Cytotoxicity against human CC20 cells after 72 hrs by FMCA method, IC50=0.24μM 19894733
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method, IC50=0.27μM 19894733
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method, IC50=1.4μM 19894733
Hs578Bst Cytotoxicity assay 72 hrs Cytotoxicity against human Hs578Bst cells after 72 hrs by CellTiter-Glo assay, IC50=0.04μM 22316168
Hs578T Cytotoxicity assay 72 hrs Cytotoxicity against human Hs578T cells after 72 hrs by CellTiter-Glo assay, IC50=0.251μM 22316168
T47D Cytotoxicity assay 72 hrs Cytotoxicity against human T47D cells after 72 hrs by CellTiter-Glo assay, IC50=0.66μM 22316168
SK-BR-3 Cytotoxicity assay 72 hrs Cytotoxicity against human SK-BR-3 cells after 72 hrs by CellTiter-Glo assay, IC50=1.08μM 22316168
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by CellTiter-Glo assay, IC50=4.7μM 22316168
Hs578Bst Cytotoxicity assay 40 uM 72 hrs Cytotoxicity against human Hs578Bst cells at 40 uM after 72 hrs by CellTiter-Glo assay relative to untreated control, IC50=47.7μM 22316168
CHO Function assay pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, IC50=3.23594μM 23571415
CHO Function assay pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, IC50=13.1826μM 23571415
Hs683 Cytotoxicity assay 3 days Cytotoxicity against human Hs683 cells after 3 days by MTT assay, IC50=0.04μM 23706005
A549 Cytotoxicity assay 3 days Cytotoxicity against human A549 cells after 3 days by MTT assay, IC50=0.05μM 23706005
PC3 Cytotoxicity assay 3 days Cytotoxicity against human PC3 cells after 3 days by MTT assay, IC50=0.075μM 23706005
U373 Cytotoxicity assay 3 days Cytotoxicity against human U373 cells after 3 days by MTT assay, IC50=0.146μM 23706005
SK-MEL-28 Cytotoxicity assay 3 days Cytotoxicity against human SK-MEL-28 cells after 3 days by MTT assay, IC50=0.266μM 23706005
MCF7 Cytotoxicity assay 3 days Cytotoxicity against human MCF7 cells after 3 days by MTT assay, IC50=0.426μM 23706005
Drosophila Schneider cells Function assay Antagonist activity at transactivation domain of RORgammat (unknown origin) expressed in Drosophila Schneider cells co-expressing Gal4-DNA binding domain, IC50=2μM 24040486
Drosophila Schneider cells Function assay Antagonist activity at transactivation domain of RORgammat (unknown origin) expressed in Drosophila Schneider cells co-expressing Gal4-DNA binding domain, IC50=2μM 24040486
RKO-AS45-1 Cytotoxicity assay 48 hrs Cytotoxicity against human RKO-AS45-1 cells after 48 hrs by MTT assay, IC50=0.42μM 26122772
HeLa Cytotoxicity assay 48 hrs Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50=2.2μM 26122772
HeLa Function assay 150 nM 24 hrs Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting 26122772
HeLa Function assay 150 nM 24 hrs Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting 26122772
HeLa Function assay 150 nM 24 hrs Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting 26122772
HeLa Function assay 150 nM 24 hrs Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting 26122772
HeLa Function assay 150 nM 24 hrs Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting 26122772
HeLa Function assay 150 nM 24 hrs Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting 26122772
HeLa Function assay 150 nM 24 hrs Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting 26122772
HeLa Function assay 150 nM 24 hrs Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting 26122772
Kasumi-1 Cytotoxicity assay 48 hrs Cytotoxicity against human Kasumi-1 cells incubated for 48 hrs by MTS assay, IC50=0.093μM 27983842
MV4-11 Cytotoxicity assay 48 hrs Cytotoxicity against human MV4-11 cells incubated for 48 hrs by MTS assay, IC50=0.111μM 27983842
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells incubated for 72 hrs by SRB assay, IC50=0.38μM 27983842
H1299 Cytotoxicity assay 24 hrs Cytotoxicity against human H1299 cells incubated for 24 hrs by MTT assay, IC50=0.46μM 27983842
CCD-112CoN Cytotoxicity assay 72 hrs Cytotoxicity against human CCD-112CoN cells incubated for 72 hrs, IC50=2.4μM 27983842
DU145 Function assay 50 uM 5 hrs Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay 31120251
DU145 Function assay 50 uM 5 hrs Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay 31120251
DU145 Function assay 50 uM 5 hrs Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay 31120251
DU145 Function assay 50 uM 5 hrs Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay 31120251
DU145 Function assay 50 uM 5 hrs Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay 31120251
DU145 Function assay 50 uM 5 hrs Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay 31120251
DU145 Function assay 50 uM 5 hrs Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay 31120251
DU145 Function assay 50 uM 5 hrs Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay 31120251
Click to View More Cell Line Experimental Data

Biological Activity

Description Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
Targets
Na,K-ATPase α2β3 [1] Na,K-ATPase α2β1 [1] Na,K-ATPase α1β1 [1]
42.8 nM(Ki) 58.7 nM(Ki) 268 nM(Ki)

Chemical Information & Solubility

Molecular Weight 780.94 Formula

C41H64O14
CAS No. 20830-75-5 SDF Download Digoxin SDF
Smiles CC1C(C(CC(O1)OC2C(OC(CC2O)OC3C(OC(CC3O)OC4CCC5(C(C4)CCC6C5CC(C7(C6(CCC7C8=CC(=O)OC8)O)C)O)C)C)C)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (128.05 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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