Ebselen (Synonyms: 依布硒; SPI-1005; PZ-51; CCG-39161)

目錄號: HY-13750 純度: 99.58%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計(jì)算器

Ebselen (SPI-1005) 是一種谷胱甘肽過氧化物酶模擬物，有效的電壓依賴性鈣通道 (VDCC) 阻斷劑。Ebselen 有效抑制 M^pro (IC₅₀=0.67 μM) 和 COVID-19 病毒 (EC₅₀=4.67 μM)。Ebselen 是 HIV-1 衣殼 CTD 二聚化的抑制劑。Ebselen 是一種有機(jī)硒化合物，可透過血腦屏障，具有抗炎，抗氧化和抗癌活性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Ebselen Chemical Structure

CAS No. : 60940-34-3

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規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥550	In-stock
5 mg	￥484	In-stock
10 mg	￥694	In-stock
25 mg	￥1145	In-stock
50 mg	￥1400	In-stock
100 mg	￥2400	In-stock
200 mg		詢價
500 mg		詢價

or 大包裝詢價

* Please select Quantity before adding items.

MCE 顧客使用本產(chǎn)品發(fā)表的 13 篇科研文獻(xiàn)

•Redox Biol. 2024 May 23:73:103206. [Abstract]
•Biomaterials. 24 August 2022, 121757.
•Environ Int. 2022 Jun 1;165:107327. [Abstract]
•Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
•Transplantation. 2024 May 21. [Abstract]
•Antiviral Res. 2023 Apr 17;105606. [Abstract]

•Mol Cell Biochem. 2022 Jun;477(6):1873-1885. [Abstract]
•J Enzyme Inhib Med Chem. 2020 Dec;35(1):906-912. [Abstract]
•Antiviral Res. 2019 Jun 27;169:104544. [Abstract]
•Behav Brain Res. 2023 Apr 23;114444. [Abstract]
•Biol Trace Elem Res. 2022 May 12. [Abstract]
•SLAS Discov. 2020 Sep;25(8):895-905. [Abstract]
•Exp Ther Med. 2019 Feb;17(2):1412-1419. [Abstract]

: Ebselen purchased from MCE. Usage Cited in: Exp Ther Med. 2019 Feb;17(2):1412-1419. [Abstract]; Ebselen influences the expression of apoptosis?related proteins. The effects of ebselen on C?Caspase?8, C?Caspase?3, Bax, Bcl?2 and C?PARP are analyzed by western blotting.

Ebselen 相關(guān)產(chǎn)品

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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HIV HIV-1 HIV-2

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker^[1]^[2]. Ebselen potently inhibits M^pro (IC₅₀=0.67 μM) and COVID-19 virus (EC₅₀=4.67 μM)^[3].Ebselen is an inhibitor of HIV-1 capsid CTD dimerization. Ebselen, an organoselenium compound, can permeate the blood-brain barrier and has anti-inflammatory, antioxidant and anticancer activity^[4]^[5].

IC₅₀ & Target

HIV-1

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
184B5	GI₅₀	30.1 μM Compound: EBS	Antiproliferative activity against human 184B5 cells after 72 hrs by MTT assay Antiproliferative activity against human 184B5 cells after 72 hrs by MTT assay	[PMID: 30071406]
A549	IC₅₀	> 100 μM Compound: PZ51	Antiproliferative activity against human A549 cells assessed as cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 25817772]
A549	IC₅₀	16.8 μM Compound: Ebs	Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay	[PMID: 29584939]
A549	IC₅₀	3.75 μM Compound: Ebselen	Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay	[PMID: 22483583]
BEAS-2B	GI₅₀	49.5 μM Compound: EBS	Antiproliferative activity against human BEAS2B cells after 72 hrs by MTT assay Antiproliferative activity against human BEAS2B cells after 72 hrs by MTT assay	[PMID: 30071406]
Bel-7402	IC₅₀	68.2 μM Compound: PZ51	Antiproliferative activity against human Bel7402 cells assessed as cell viability after 48 hrs by MTT assay Antiproliferative activity against human Bel7402 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 25817772]
Calu-1	GI₅₀	68.6 μM Compound: EBS	Antiproliferative activity against human HTB-54 cells after 72 hrs by MTT assay Antiproliferative activity against human HTB-54 cells after 72 hrs by MTT assay	[PMID: 30071406]
CCRF-CEM	GI₅₀	57.1 μM Compound: EBS	Antiproliferative activity against human CCRF-CEM cells after 72 hrs by MTT assay Antiproliferative activity against human CCRF-CEM cells after 72 hrs by MTT assay	[PMID: 30071406]
CHO-K1	EC₅₀	6.1 μM Compound: 7	Cytotoxicity against CHO-K1 cells by Alamar blue assay Cytotoxicity against CHO-K1 cells by Alamar blue assay	[PMID: 16962325]
HCT-116	IC₅₀	50 μM Compound: Ebs	Cytotoxicity in human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay Cytotoxicity in human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay	[PMID: 29584939]
HeLa	IC₅₀	78.5 μM Compound: PZ51	Antiproliferative activity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 25817772]
HT-29	GI₅₀	> 100 μM Compound: EBS	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 30071406]
HT-29	IC₅₀	50.4 μM Compound: Ebs	Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay	[PMID: 29584939]
MCF7	IC₅₀	> 100 μM Compound: PZ51	Antiproliferative activity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 25817772]
MCF7	IC₅₀	15.02 μM Compound: Ebselen	Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay	[PMID: 22483583]
MCF7	GI₅₀	58.8 μM Compound: EBS	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30071406]
MDA-MB-231	IC₅₀	42.3 μM Compound: 1, PZ 51, ebselen	Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay	[PMID: 22204902]
NCI-H1299	IC₅₀	27.7 μM Compound: Ebs	Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay	[PMID: 29584939]
PC-3	GI₅₀	> 100 μM Compound: EBS	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 30071406]
U-266	IC₅₀	40 μM Compound: 62	Anticancer activity against human U-266 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Anticancer activity against human U-266 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 34217061]

體外研究
(In Vitro)

Ebselen (SPI-1005；0.4-100 μM；20-24 小時) 在 10 μM 濃度下對 COVID-19 病毒感染的 Vero 細(xì)胞表現(xiàn)出強(qiáng)大的抗病毒作用。Ebsele 與 COVID-19 病毒 Mpro 中催化二元體的 C145 共價結(jié)合^[3]。
Ebselen 通過削弱進(jìn)入的衣殼脫殼過程來抑制 HIV-1 生命周期的早期病毒進(jìn)入后事件^[4]。
Ebselen 可滲透血腦屏障并抑制小鼠腦中的內(nèi)源性肌醇單磷酸酶。Ebselen 抑制肌醇單磷酸酶 (IMPase)^[5]。
Ebselen 可抑制 QSOX1 酶活性并抑制胰腺癌細(xì)胞系和腎癌細(xì)胞系的侵襲^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR^[3]

Cell Line:	COVID-19 virus infected Vero cells
Concentration:	0.4, 1.2, 3.7, 11.1, 33.3, 100 μM
Incubation Time:	20-24 hours
Result:	Showed strong antiviral effects at a concentration of 10 μM treatment.

體內(nèi)研究
(In Vivo)

Ebselen（5、10 mg/kg；IP）以劑量依賴性方式減少 5-HT₂ 激動劑引起的頭部抽搐^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	20-25 g 10-12 week old male C57Bl6 mice^[5]
Dosage:	5, 10 mg/kg
Administration:	IP
Result:	Decreased 5-HT₂ agonist-induced head twitches in a dose-dependent manner.

Clinical Trial

分子量

274.18

Formula

C₁₃H₉NOSe

CAS 號

60940-34-3

性狀

固體

顏色

Light yellow to green yellow

中文名稱

依布硒；依布硒林

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 50 mg/mL (182.36 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	3.6472 mL	18.2361 mL	36.4723 mL
5 mM	0.7294 mL	3.6472 mL	7.2945 mL
10 mM	0.3647 mL	1.8236 mL	3.6472 mL

查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?個月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實(shí)驗(yàn)：

請根據(jù)您的實(shí)驗(yàn)動物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.12 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.12 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個月以上的動物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計(jì)算器

請輸入動物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量

請輸入您的動物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購。，Tween 80，均可在 MCE 網(wǎng)站選購。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。

動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.58%

選擇批次：

Data Sheet (648 KB) SDS (788 KB)

COA (288 KB) HNMR (274 KB) LCMS (122 KB) 元素分析報(bào)告 (213 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Liang Q, et al. Electrical Stimulation Degenerated Cochlear Synapses Through Oxidative Stress in NeonatalCochlear Explants. Front Neurosci. 2019 Oct 14;13:1073. [Content Brief]

[2]. H Sies, et al. Ebselen, a Selenoorganic Compound as Glutathione Peroxidase Mimic [Content Brief]

[3]. Jin Z, et al. Structure of M^pro from COVID-19 virus and discovery of its inhibitors. Nature. 2020 Apr 9. [Content Brief]

[4]. Thenin-Houssier S, et al. Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication. Antimicrob Agents Chemother. 2016 Mar 25;60(4):2195-208. [Content Brief]

[5]. Singh N, et al. A safe lithium mimetic for bipolar disorder. Nat Commun. 2013;4:1332. doi: 10.1038/ncomms2320. [Content Brief]

[6]. Hanavan PD, et al. Ebselen inhibits QSOX1 enzymatic activity and suppresses invasion of pancreatic and renal cancer cell lines. Oncotarget. 2015 Jul 30;6(21):18418-28. [Content Brief]

Ebselen 相關(guān)分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.6472 mL	18.2361 mL	36.4723 mL	91.1806 mL
	5 mM	0.7294 mL	3.6472 mL	7.2945 mL	18.2361 mL
	10 mM	0.3647 mL	1.8236 mL	3.6472 mL	9.1181 mL
	15 mM	0.2431 mL	1.2157 mL	2.4315 mL	6.0787 mL
	20 mM	0.1824 mL	0.9118 mL	1.8236 mL	4.5590 mL
	25 mM	0.1459 mL	0.7294 mL	1.4589 mL	3.6472 mL
	30 mM	0.1216 mL	0.6079 mL	1.2157 mL	3.0394 mL
	40 mM	0.0912 mL	0.4559 mL	0.9118 mL	2.2795 mL
	50 mM	0.0729 mL	0.3647 mL	0.7294 mL	1.8236 mL
	60 mM	0.0608 mL	0.3039 mL	0.6079 mL	1.5197 mL
	80 mM	0.0456 mL	0.2280 mL	0.4559 mL	1.1398 mL
	100 mM	0.0365 mL	0.1824 mL	0.3647 mL	0.9118 mL

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ebselen (Synonyms: 依布硒; SPI-1005; PZ-51; CCG-39161)

MCE 顧客使用本產(chǎn)品發(fā)表的 13 篇科研文獻(xiàn)