Nrf2 activator-3

• CAT Number: I041195
• CAS Number: 2766570-23-2
• Molecular Formula: C23H18F3N3O2
• Molecular Weight: 425.40
• Purity: ≥95%
• Synonyms: 2-[1-(3,5-dimethylphenyl)-5-(2-hydroxyphenyl)-1,2,4-triazol-3-yl]-5-(trifluoromethyl)phenol
• InChI: InChI=1S/C23H18F3N3O2/c1-13-9-14(2)11-16(10-13)29-22(18-5-3-4-6-19(18)30)27-21(28-29)17-8-7-15(12-20(17)31)23(24,25)26/h3-12,30-31H,1-2H3
• InChIKey: INMUTDNBXNPVRS-UHFFFAOYSA-N
• SMILES: CC1=CC(=CC(=C1)N2C(=NC(=N2)C3=C(C=C(C=C3)C(F)(F)F)O)C4=CC=CC=C4O)C

Nrf2 activator-3 is a potent Nrf2 activator. Nrf2 activator-3 is used for cerebral ischemic injury research[1].
Nrf2 activator-3 (compound 24) (1 μM, 5 μM, and 10 μM) is against SNP (400 μM)-induced cell death with IC50 values of 76.86±3.54 μM, 101.59±3.34 μM, and 105.1±1.84 μM at 1 μM, 5 μM, and 10 μM, respectively in PC12 cells[1]。
Nrf2 activator-3 (1-200 μM) is against PC12 and hacat cell with IC50 values of 262.70±1.98 μM and 126.70±10.39 μM, respctively[1]。
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].

Reference

[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.
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