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

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Ebselen (Synonyms: 依布硒; SPI-1005; PZ-51; CCG-39161) 纯度: 99.58%

Ebselen (SPI-1005) 是一种谷胱甘肽过氧化物酶模拟物，有效的电压依赖性钙通道 (VDCC) 阻断剂。Ebselen 有效抑制 Mpro (IC50=0.67 μM) 和 COVID-19 病毒 (EC50=4.67 μM)。Ebselen 是 HIV-1 衣壳 CTD 二聚化的抑制剂。Ebselen 是一种有机硒化合物，可透过血脑屏障，具有抗炎，抗氧化和抗癌活性。

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

Ebselen Chemical Structure

CAS No. : 60940-34-3

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10 mg ￥700 In-stock
50 mg ￥1400 In-stock
100 mg ￥2400 In-stock
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Ebselen 相关产品

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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 Mpro (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

IC50: 0.67 μM (Mpro)[3]
EC50: 4.67 μM (COVID-19 virus)[3]
体外研究
(In Vitro)

Ebselen (SPI-1005; 0.4-100 μM; 20-24 hours) shows strong antiviral effects at a concentration of 10 μM treatment in COVID-19 virus infected Vero cells. Ebsele covalently binds to C145 of the catalytic dyad in COVID-19 virus Mpro[3].
Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming capsid uncoating process[4].
Ebselen permeates the blood-brain barrier and inhibits endogenous inositol monophosphatase in mouse brain. Ebselen inhibits inositol monophosphatase (IMPase)[5].
Ebselen inhibits QSOX1 enzymatic activity and suppresses invasion of pancreatic, renal cancer cell lines[6].

上海金畔生物科技有限公司 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.

体内研究
(In Vivo)

Ebselen (5, 10 mg/kg; IP) decreases 5-HT2 agonist-induced head twitches in a dose-dependent manner[5].

上海金畔生物科技有限公司 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 号

60940-34-3
中文名称

依布硒；依布硒林
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (182.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6472 mL 18.2362 mL 36.4724 mL
5 mM 0.7294 mL 3.6472 mL 7.2945 mL
10 mM 0.3647 mL 1.8236 mL 3.6472 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.12 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

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

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

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

    [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.

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

    [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.

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