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Digoxin ATPase 억제제

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

제품 번호S4290

Digoxin은 심방세동 및 심부전 치료에 사용되는 고전적인 Na,K-ATPase 억제제로, 일반적인 α1β1 아이소폼보다 α2β3 아이소폼에 대한 선택성을 가집니다.본 제품은 위험 화학물질(급성 독성/인화성/피부 부식성)입니다. 보호 안면 마스크, 장갑 및 의류를 착용하고 사용하십시오.

화학 구조

분자량: 780.94

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품질 관리

배치: 순도: 99.61%

99.61

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

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	780.94	화학식	C₄₁H₆₄O₁₄	보관 (수령일로부터)	3년-20°C분말
CAS 번호	20830-75-5	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	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

용해도

In vitro
배치:

DMSO : 100 mg/mL (128.05 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (128.05 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (128.05 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (128.05 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 85 mg/mL (108.84 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
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 Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	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.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

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

적용 분야

방법	바이오마커	이미지	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

기술 지원

취급 설명서

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C5=C4/X	C5:	LOG(C5):
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