DDO-7263

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD).

Western Blot AnalysisCell Line:PC12 cells Concentration:20 μM Incubation Time:2, 4, 8, 12, 24 hours Result:Upregulated the protein levels of HO-1 and NQO1 in concentration-dependent manners.

Animal Model:Male C57BL/6 mice at 10 weeks of age and body weights of 22-26 gDosage:10, 50, 100 mg/kg Administration:IP; daily for 10 days Result:Improved the reduction of vertical spontaneous activity and mitigated the loss of balance coordination caused by MPTP (20 mg/kg/day; 7 days). Protected dopaminergic neurons from MPTP. Significantly downregulated the levels of pro-inflammatory factors, including IL-1β and TNF-α, in mouse plasma.Animal Model:SD rats Dosage:7, 35, 70 mg/kg (Pharmacokinetic Analysis) Administration:IP Result:Had a T1/2 of 3.32 hours and a Cmax of 1.38 mg/mL.

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Nuclear Receptor/Transcription Factor

Keap1-Nrf2

Nrf2

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2254004-96-9

273.24

C14H9F2N3O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 17.86 mg/mL (65.36 mM; 超声助溶 (<60°C)

Cc1ccc(cn1)-c1noc(n1)-c1ccc(F)c(F)c1

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(-20℃)

With Ice Pack

≥ 2 years