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。
生物活性 | Ebselen (SPI-1005), aglutathione peroxidasemimetic, is a potentvoltage-dependentcalcium channel(VDCC)blocker[1][2]. Ebselen potently inhibitsMpro(IC50=0.67 μM) andCOVID-19virus (EC50=4.67 μM)[3].Ebselen is an inhibitor ofHIV-1capsid 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].
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. |
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体内研究 (In Vivo) | Ebselen (5, 10 mg/kg; IP) decreases 5-HT2agonist-induced head twitches in a dose-dependent manner[5].
Animal Model: | 20-25 g 10-12 week old male C57Bl6 mice[5] | Dosage: | 5, 10 mg/kg | Administration: | IP | Result: | Decreased 5-HT2agonist-induced head twitches in a dose-dependent manner. |
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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 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(182.36 mM;Need ultrasonic) 配制储备液 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 |
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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。 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本网站选购。
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