Ouabain

别名: NSC 25485 中文名称:乌本(箭毒)苷,G毒毛旋花苷

Ouabain (NSC 25485) 是一种选择性的Na+/K+-ATPase抑制剂,与α2 /α3亚基结合,Ki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

Ouabain Chemical Structure

CAS: 630-60-4

规格 价格 库存 购买数量
50mg RMB 1388.39 现货
1g RMB 7944.3 现货
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客户使用Selleck的Ouabain发表文献8

客户使用该产品的1个实验数据

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

相关信号通路图

ATPase抑制剂选择性比较

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,Ki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
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 --

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)

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

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)

mg/kg g μL

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,: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: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: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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