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Digoxin ATPase inhibitor

Name: Digoxin
Brand: Selleck Chemicals
SKU: S4290
Rating: 5 (19 reviews)

Cat. No.: S4290

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 ATPase inhibitor Chemical Structure

Estructura química

Peso molecular: 780.94

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Control de calidad (Quality Control)

Lote: Pureza: 99.61%

99.61

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Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	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
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	780.94	Fórmula	C₄₁H₆₄O₁₄	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	20830-75-5	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	NSC 95100, 12β-Hydroxydigitoxin			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

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 100 mg/mL (128.05 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	2.000mg/ml (2.56mM)	Taking the 1 mL working solution as an example, add 20 μL of 100 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC₅₀/Ki	Na,K-ATPase α2β3 42.8 nM(Ki) Na,K-ATPase α2β1 58.7 nM(Ki) Na,K-ATPase α1β1 268 nM(Ki)
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/26483500/

Aplicaciones (Applications)

Métodos	Biomarcadores	Imágenes	PMID
Western blot	p-Src / Src / p-EGFR / EGFR / p-STAT3 / STAT3 p-PI3K / PI3K / p-AKT / AKT / p-MEK / MEK / p-ERK / ERK / p-FAK / FAK / p-SAPK/JNK / p-Paxillin / Paxillin / p-p130Cas / p130Cas Nrf2		25955608
Growth inhibition assay	Cell viability		25955608

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):