In the acute toxicity study, Nrf2 activator-3 (compound 24) shows toxicity to the experimental mice at 1000 mg/kg, the LD50 of intraperitoneal injection is 789 mg/kg, and the 95% confidence interval was 550-1000 mg/kg in balb/c mice[1].In in vivo pharmacokinetic properties study, Nrf2 activator-3 (5 mg/kg; Intraperitoneal injection) shows that plasma reached a maximum (323.06 ng/mL) at 2 h. The Tmax, Cmax, AUC0-inf, F% and T1/2 values are 2 hour, 323.06 ng/mL, 2929.88 ng/mL*h, 28%, 12.75 hours respctively[1].Nrf2 activator-3 (5 mg/kg; .i.v.) shows Tmax, Cmax, AUC0-inf, and T1/2 values are 0.08 hours, 6911.14 ng/mL, 10182.73 ng/mL*h, and 8.26 hours respctively[1].Nrf2 activator-3 (3 mg/kg; 10 mg/kg;30 mg/kg) reduces the cerebral infarction volume and leads to decreased neurological deficits in MCAO rats[1].
| Animal Model: | MCAO rats |
| Dosage: | 3 mg/kg; 10 mg/kg; 30 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Attenuated cerebral ischemic injury.(low dose: 16.37 ± 6.51%, medium dose: 14.49 ± 5.62%, high dose: 12.23 ± 8.50%), which was similar to the effect of Edaravone (12.77 ± 5.82%). |
| Animal Model: | MCAO rats |
| Dosage: | 3 mg/kg; 10 mg/kg; 30 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Attenuated cerebral ischemic injury.(low dose: 16.37 ± 6.51%, medium dose: 14.49 ± 5.62%, high dose: 12.23 ± 8.50%), which was similar to the effect of Edaravone (12.77 ± 5.82%). |
