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Digoxin ATPase inibitore

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

N. Cat.S4290

La Digoxin è un inibitore classico della Na,K-ATPase, con selettività per l'isoforma α2β3 rispetto alla comune isoforma α1β1, utilizzata nel trattamento della fibrillazione atriale e dell'insufficienza cardiaca.Questo prodotto è un prodotto chimico pericoloso (tossicità acuta/infiammabile/corrosivo per la pelle). Si prega di utilizzarlo indossando una maschera protettiva per il viso, guanti e indumenti protettivi.

Digoxin ATPase inibitore Chemical Structure

Struttura chimica

Peso molecolare: 780.94

Vai a

Controllo Qualità

Lotto: Purezza: 99.61%

99.61

Target correlati	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel GluR
Altro ATPase Inibitori	(-)-Blebbistatin Thapsigargin Brefeldin A (BFA chemical) CB-5083 Golgicide A Sodium orthovanadate Oleic Acid Bufalin Ginsenoside Rb1 CDN1163

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività	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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Informazioni chimiche, conservazione e stabilità

Peso molecolare	780.94	Formula	C₄₁H₆₄O₁₄	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	20830-75-5	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	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

Solubilità

In vitro
Lotto:

DMSO : 100 mg/mL (128.05 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

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)
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/26483500/

Applicazioni

Metodi	Biomarcatori	Immagini	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

Supporto tecnico

Istruzioni per la manipolazione

Tel: +1-832-582-8158 Ext:3

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