Ouabain

別名: NSC 25485 中文名稱：烏本（箭毒）苷，G毒毛旋花苷

目錄號(hào)：S4016 Purity: 98.58%

Ouabain (NSC 25485) 是一種選擇性的Na⁺/K⁺-ATPase抑制劑，與α2 /α3亞基結(jié)合，K_i為41 nM/15 nM。此產(chǎn)品為?；罚毙远拘?易燃/皮膚腐蝕），請?jiān)诖┐鞣雷o(hù)面罩、防護(hù)手套和防護(hù)服后使用。已取得危險(xiǎn)化學(xué)品經(jīng)營許可

Ouabain Chemical Structure

CAS: 630-60-4

規(guī)格	價(jià)格	庫存
50mg	1388.39	現(xiàn)貨
1g	7944.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

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

98.58

Ouabain相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	V-ATPase F-ATPase SERCA RecA AAA ATPase family	點(diǎn)擊展開
相關(guān)產(chǎn)品	Brefeldin A (BFA) (-)-Blebbistatin CB-5083 Omecamtiv mecarbil (CK-1827452) Thapsigargin Sodium orthovanadate Golgicide A BTB06584 Ginsenoside Rb1 CDN1163 Periplocin Rhodamine 123 tetrathiomolybdate Saikosaponin D	點(diǎn)擊展開
相關(guān)化合物庫	FDA藥物庫天然產(chǎn)物庫離子通道配體庫外泌體分泌相關(guān)化合物庫鈣通道阻滯劑庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)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(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

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，K_i為41 nM/15 nM。此產(chǎn)品為?；罚毙远拘?易燃/皮膚腐蝕），請?jiān)诖┐鞣雷o(hù)面罩、防護(hù)手套和防護(hù)服后使用。

特性

阿糖苷毒結(jié)合并抑制細(xì)胞Na + / K +泵在細(xì)胞膜的作用。

靶點(diǎn)

α3 ^[1]	α2 ^[1]
15 nM(Ki)	41 nM(Ki)

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(xì)胞中，Ouabain (0.1 μM-1.0 μM)抑制Na⁺泵，并增加儲(chǔ)存的Ca²⁺。高哇巴因親和力亞型(星形膠質(zhì)細(xì)胞中α2，神經(jīng)元和肌細(xì)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(xì)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(dá)的蛋白質(zhì)。在培養(yǎng)的大鼠星形膠質(zhì)細(xì)胞中，Ouabain誘導(dǎo)的α1 mRNA增加被環(huán)己酰亞胺(10 mM)，細(xì)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(xì)胞系中誘導(dǎo)顯著的PMD(28.1% MDCK 細(xì)胞和47.9% Ma104 細(xì)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(xì)胞中更為顯著。Ouabain (10 μM)誘導(dǎo)MDCK細(xì)胞中P-Tyr持續(xù)增加，并且GSH幾乎完全恢復(fù)該作用，然而該作用在Ma104細(xì)胞中并不顯著。^[4]

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(jìn)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]
動(dòng)物實(shí)驗(yàn)	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
臨床試驗(yàn)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	--

參考文獻(xiàn)
[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. + 展開

參考文獻(xiàn)

[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.

+ 展開

化學(xué)信息&溶解度

分子量	728.77	分子式	C₂₉H₄₄O₁₂.8H₂O
CAS號(hào)	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(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (137.21 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請輸入動(dòng)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）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)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(jìn)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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C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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