Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker. Ebselen potently inhibits M (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.
性状
Solid
IC50 & Target[1][2]
IC50: 0.67 μM (M)
EC50: 4.67 μM (COVID-19 virus)
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.
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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
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(In Vivo)
Ebselen (5, 10 mg/kg; IP) decreases 5-HT2 agonist-induced head twitches in a dose-dependent manner.
Medlife 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
Dosage:
5, 10 mg/kg
Administration:
IP
Result:
Decreased 5-HT2 agonist-induced head twitches in a dose-dependent manner.