Ouabain

别名: NSC 25485 中文名称：乌本（箭毒）苷，G毒毛旋花苷

目录号：S4016 Purity: 98.58%

Ouabain (NSC 25485) 是一种选择性的Na⁺/K⁺-ATPase抑制剂，与α2 /α3亚基结合，K_i为41 nM/15 nM。此产品为危化品（急性毒性/易燃/皮肤腐蚀），请在穿戴防护面罩、防护手套和防护服后使用。已取得危险化学品经营许可

Ouabain Chemical Structure

CAS: 630-60-4

规格	价格	库存
50mg	1388.39	现货
1g	7944.3	现货
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产品质控

批次： S401607 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false 纯度： 98.58%

98.58

Ouabain相关产品

相关靶点	V-ATPase F-ATPase SERCA RecA AAA ATPase family	点击展开
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相关化合物库	FDA药物库天然产物库离子通道配体库外泌体分泌相关化合物库钙通道阻滞剂库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
THP1	Cellular uptake in	250 mg/liter	24 hrs	Cellular uptake in methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in human mdr1 siRNAs- induced MDR1 deficient human THP1 cells assessed as increase accumulation at 250 mg/liter after 24 hrs by Western blot analysis	17548493
Hs578Bst	Cytotoxicity against human		72 hrs	Cytotoxicity against human Hs578Bst cells after 72 hrs by CellTiter-Glo assay, IC50=0.006μM	22316168
Hs578T	Cytotoxicity against human		72 hrs	Cytotoxicity against human Hs578T cells after 72 hrs by CellTiter-Glo assay, IC50=0.11μM	22316168
T47D	Cytotoxicity against human		72 hrs	Cytotoxicity against human T47D cells after 72 hrs by CellTiter-Glo assay, IC50=0.385μM	22316168
SK-BR-3	Cytotoxicity against human		72 hrs	Cytotoxicity against human SK-BR-3 cells after 72 hrs by CellTiter-Glo assay, IC50=0.403μM	22316168
MCF7	Cytotoxicity against human		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by CellTiter-Glo assay, IC50=10.6μM	22316168
A549	Cytotoxicity against human		3 days	Cytotoxicity against human A549 cells after 3 days by MTT assay, IC50=0.027μM	23706005
Hs683	Cytotoxicity against human		3 days	Cytotoxicity against human Hs683 cells after 3 days by MTT assay, IC50=0.028μM	23706005
PC3	Cytotoxicity against human		3 days	Cytotoxicity against human PC3 cells after 3 days by MTT assay, IC50=0.043μM	23706005
U373	Cytotoxicity against human		3 days	Cytotoxicity against human U373 cells after 3 days by MTT assay, IC50=0.077μM	23706005
MCF7	Cytotoxicity against human		3 days	Cytotoxicity against human MCF7 cells after 3 days by MTT assay, IC50=0.133μM	23706005
SK-MEL-28	Cytotoxicity against human		3 days	Cytotoxicity against human SK-MEL-28 cells after 3 days by MTT assay, IC50=0.211μM	23706005
MDCK	TP_TRANSPORTER: cell accumulation in			TP_TRANSPORTER: cell accumulation in OATP4C1-expressing MDCK cells, Km=0.38μM	14993604
HeLa	Cytotoxicity against human			Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis	18066055
HeLa	Inhibition of mitosis in			Inhibition of mitosis in human HeLa cells by imaging analysis	18066055
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
点击查看更多细胞系数据

生物活性

产品描述

Ouabain (NSC 25485) 是一种选择性的Na⁺/K⁺-ATPase抑制剂，与α2 /α3亚基结合，K_i为41 nM/15 nM。此产品为危化品（急性毒性/易燃/皮肤腐蚀），请在穿戴防护面罩、防护手套和防护服后使用。

特性

阿糖苷毒结合并抑制细胞Na + / K +泵在细胞膜的作用。

靶点

α3 ^[1]	α2 ^[1]
15 nM(Ki)	41 nM(Ki)

体外研究(In Vitro)
体外研究活性	Ouabain (100 nM)抑制25%的 ATPase活性。^[1]在培养的大鼠星形胶质细胞中，Ouabain (0.1 μM-1.0 μM)抑制Na⁺泵，并增加储存的Ca²⁺。高哇巴因亲和力亚型(星形胶质细胞中α2，神经元和肌细胞中α3)被限制在PM内的网状分布，平行于底层内质网或肌浆网。^[2] 在培养的大鼠星形胶质细胞中，Ouabain (0.5-1.0 mM)增加α1和β1 mRNAs的水平，而减少α2和β2 mRNAs水平。对照组和ouabain 处理的培养基中，Ouabain增加α1和β1，但不增加α2和β2表达的蛋白质。在培养的大鼠星形胶质细胞中，Ouabain诱导的α1 mRNA增加被环己酰亚胺(10 mM)，细胞内Ca²⁺螯合剂1,2-双(2-氨基苯氧基)乙烷-N,N,N',N'-四乙酸四乙酰氧甲酯(30 mM)，和FK506 (1 nM) 所阻断。^[3] Ouabain (10 μM)在两种细胞系中诱导显著的PMD(28.1% MDCK 细胞和47.9% Ma104 细胞被门控在M1区域，分别是对照组的11.8%和14.6%倍 )，但出乎意料的是，这种作用在Ma104细胞中更为显著。Ouabain (10 μM)诱导MDCK细胞中P-Tyr持续增加，并且GSH几乎完全恢复该作用，然而该作用在Ma104细胞中并不显著。^[4]

体内研究(In Vivo)
体内研究活性	Ouabain (14.4 毫克/千克.天，间歇性皮下注射)进一步增加由于心肌梗死(MI)而心脏衰竭的大鼠体内总外周阻力(TPR)，而连续的Ouabain治疗使大鼠TPR正常化。Ouabain (14.4 毫克/千克.天，连续皮下注射)显著改善基底和最大的CO(基底:83 毫升/分钟；最大: 134 毫升/分钟)。 ^[5]
动物实验	Animal Models	由于心肌梗死(MI)而心脏衰竭的雄性Wistar大鼠。
	Dosages	14.4毫克/千克
	Administration	皮下注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT03034005	Completed	Asthma	Bispebjerg Hospital	March 27 2017	Phase 4
NCT04630132	Unknown status	Aging\|Frailty\|Hypertension\|CKD	IRCCS San Raffaele\|Cariplo Foundation	March 25 2017	--

参考文献
[1] Lucchesi PA, et al. J Biol Chem, 1991, 266(14), 9327-9331. [2] Juhaszova M, et al. Proc Natl Acad Sci U S A, 1997, 94(5), 1800-1805. [3] Hosoi R, et al. J Neurochem, 1997, 69(5), 2189-2196. [4] Valente RC, et al. FASEB J, 2003, 17(12), 1700-1702. [5] Nelissen-Vrancken HJ, et al. Naunyn Schmiedebergs Arch Pharmacol, 1997, 356(2), 203-209. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	728.77	分子式	C₂₉H₄₄O₁₂.8H₂O
CAS号	630-60-4	SDF	Download Ouabain SDF
Smiles	CC1C(C(C(C(O1)OC2CC(C3(C4C(CCC3(C2)O)C5(CCC(C5(CC4O)C)C6=CC(=O)OC6)O)CO)O)O)O)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (137.21 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

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* 必填项

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