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別名: NSC 25485 中文名稱:烏本(箭毒)苷,G毒毛旋花苷
Ouabain (NSC 25485) 是一種選擇性的Na+/K+-ATPase抑制劑,與α2 /α3亞基結(jié)合,Ki為41 nM/15 nM。此產(chǎn)品為危化品(急性毒性/易燃/皮膚腐蝕),請在穿戴防護面罩、防護手套和防護服后使用。 已取得危險化學品經(jīng)營許可
Ouabain Chemical Structure
CAS: 630-60-4
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
---|---|---|---|---|---|
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 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Ouabain (NSC 25485) 是一種選擇性的Na+/K+-ATPase抑制劑,與α2 /α3亞基結(jié)合,Ki為41 nM/15 nM。此產(chǎn)品為?;罚毙远拘?易燃/皮膚腐蝕),請在穿戴防護面罩、防護手套和防護服后使用。 | ||||
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特性 | 阿糖苷毒結(jié)合并抑制細胞Na + / K +泵在細胞膜的作用。 | ||||
靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Ouabain (100 nM)抑制25%的 ATPase活性。[1]在培養(yǎng)的大鼠星形膠質(zhì)細胞中,Ouabain (0.1 μM-1.0 μM)抑制Na+泵,并增加儲存的Ca2+。高哇巴因親和力亞型(星形膠質(zhì)細胞中α2,神經(jīng)元和肌細胞中α3)被限制在PM內(nèi)的網(wǎng)狀分布,平行于底層內(nèi)質(zhì)網(wǎng)或肌漿網(wǎng)。[2] 在培養(yǎng)的大鼠星形膠質(zhì)細胞中,Ouabain (0.5-1.0 mM)增加α1和β1 mRNAs的水平,而減少α2和β2 mRNAs水平。對照組和ouabain 處理的培養(yǎng)基中,Ouabain增加α1和β1,但不增加α2和β2表達的蛋白質(zhì)。在培養(yǎng)的大鼠星形膠質(zhì)細胞中,Ouabain誘導的α1 mRNA增加被環(huán)己酰亞胺(10 mM),細胞內(nèi)Ca2+螯合劑1,2-雙(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) 所阻斷。[3] Ouabain (10 μM)在兩種細胞系中誘導顯著的PMD(28.1% MDCK 細胞和47.9% Ma104 細胞被門控在M1區(qū)域,分別是對照組的11.8%和14.6%倍 ),但出乎意料的是,這種作用在Ma104細胞中更為顯著。Ouabain (10 μM)誘導MDCK細胞中P-Tyr持續(xù)增加,并且GSH幾乎完全恢復該作用,然而該作用在Ma104細胞中并不顯著。[4] |
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體內(nèi)研究(In Vivo) | ||
體內(nèi)研究活性 | Ouabain (14.4 毫克/千克.天,間歇性皮下注射)進一步增加由于心肌梗死(MI)而心臟衰竭的大鼠體內(nèi)總外周阻力(TPR),而連續(xù)的Ouabain治療使大鼠TPR正?;uabain (14.4 毫克/千克.天,連續(xù)皮下注射)顯著改善基底和最大的CO(基底:83 毫升/分鐘;最大: 134 毫升/分鐘)。 [5] |
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動物實驗 | Animal Models | 由于心肌梗死(MI)而心臟衰竭的雄性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 | -- |
分子量 | 728.77 | 分子式 | C29H44O12.8H2O |
CAS號 | 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 | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 100 mg/mL ( (137.21 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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