• 产品描述： Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker. Ebselen potently inhibits Mpro (IC50=0.67 μM) and COVID-19 virus (EC50=4.67 μM).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

• 靶点： IC50: 0.67 μM (Mpro) EC50: 4.67 μM (COVID-19 virus);Phosphatase;VirusProtease;CalciumChannel;COX;HIVProtease

• 体外研究：
  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. Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming capsid uncoating process. Ebselen permeates the blood-brain barrier and inhibits endogenous inositol monophosphatase in mouse brain. Ebselen inhibits inositol monophosphatase (IMPase). Ebselen inhibits QSOX1 enzymatic activity and suppresses invasion of pancreatic, renal cancer cell lines. RT-PCR 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：
  Ebselen (5, 10 mg/kg; IP) decreases 5-HT2 agonist-induced head twitches in a dose-dependent manner. Animal Model: 20-25 g 10-12 week old male C57Bl6 mice Dosage: 5, 10 mg/kg Administration: IP Result: Decreased 5-HT2 agonist-induced head twitches in a dose-dependent manner.

• 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. Free Radic Biol Med. 1993 Mar;14(3):313-23. 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.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.647 ml	18.236 ml	36.472 ml
  5 mM	0.729 ml	3.647 ml	7.294 ml
  10 mM	0.365 ml	1.824 ml	3.647 ml
  50 mM	0.073 ml	0.365 ml	0.729 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *