DDO-7263 是一种 1,2,4-Oxadiazole 衍生物，是一种有效的 Nrf2-ARE 激活剂。DDO-7263 通过与 Rpn6 结合上调 Nrf2，从而阻断 26S 蛋白酶体的组装和随后泛素化 Nrf2 的降解。DDO-7263 诱导 Nrf2 易位进入细胞核。DDO-7263 抑制 NLRP3 炎性体激活。DDO-7263 具有抗炎活性，并且有潜力用于神经退行性疾病(例如帕金森病 (PD)) 的研究。

DDO-7263 is a potent Nrf2-ARE activator. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits activation of NLRP3 inflammasome. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2.

DDO-7263 (20 μM; 2-24 h) can upregulate the protein levels of NQO1 and HO-1. DDO-7263 (2.5, 5, 10, 20, 40, 80 μM; 24 h) can upregulate the survival rate of THP-Ms and PC12 cell after treatment of 400μM H2O2 in a concentration-dependent manner. DDO-7263 has no significant decrease on cell survival rate[1].

DDO-7263 (10-100 mg/kg/day; IP; for 10 days) improves the behavioral abnormalities induced by MPTP in mice, significantly attenuates chemically induced dopaminergic neuron loss of tyrosine hydroxylase (TH) in the substantia nigra (SN) and striatum of the mouse brain and inhibits the secretion of inflammatory factors. DDO-7263 (7, 35, 70 mg/kg; IP) has a T1/2 of 3.32 hours and a Cmax of 1.38 mg/mL for rats[1].

2254004-96-9

C14H9F2N3O

273.24

DMSO:16.1 mg/mL (58.8 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years