| Chemical Properties | Back Directory | [Boiling point ]
607.831±65.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.348±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
7.118±0.40(predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
Nrf2 activator-3 is a potent Nrf2 activator. Nrf2 activator-3 is used for cerebral ischemic injury research[1]. | [in vivo]
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%). |
| [References]
[1] Yaoqiang Lao, et al. Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury. Eur J Med Chem. 2022 Jun 5;236:114315. DOI:10.1016/j.ejmech.2022.114315 |
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