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Digoxin ATPase remmer

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

Cat.nr.S4290

Digoxin is een klassieke Na,K-ATPase-remmer, met selectiviteit voor de α2β3-isoform boven de gangbare α1β1-isoform, gebruikt bij de behandeling van atriumfibrillatie en hartfalen.Dit product is een gevaarlijke chemische stof (acute toxiciteit/ontvlambaar/huidcorrosief). Gelieve het te gebruiken met een beschermend gezichtsmasker, handschoenen en kleding.

Digoxin ATPase remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 780.94

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Kwaliteitscontrole

Batch: Zuiverheid: 99.61%

99.61

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

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	780.94	Formule	C₄₁H₆₄O₁₄	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	20830-75-5	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid

In vitro
Batch:

DMSO : 100 mg/mL (128.05 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

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

Toepassingen

Methoden	Biomarkers	Afbeeldingen	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

Technische ondersteuning

Gebruiksaanwijzing

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

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