| 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京