DDO-7263

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DDO-7263

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2254004-96-9

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价
50mg	询价

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。

Cas No.	2254004-96-9
分子式	C14H9F2N3O
分子量	273.24
溶解度	DMSO : 17.86 mg/mL (65.36 mM; ultrasonic and warming and heat to 60°C)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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)[1][2]. DDO-7263 (20 μM; 2-24 h) can upregulate the protein levels of HO-1 and NQO1 in concentration-dependent manners[1]. DDO-7263 (2.5, 5, 10, 20, 40, 80 μM; 24 h) can upregulate the survival rate of PC12 and THP-Ms cell after 400 μM H2O2 in a concentration-dependent manner. DDO-7263 alone 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[1]. 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]. [1]. Li-Li Xu, et al. 5-(3,4-Difluorophenyl)-3-(6-methylpyridin-3-yl)-1,2,4-oxadiazole (DDO-7263), a novel Nrf2 activator targeting brain tissue, protects against MPTP-induced subacute Parkinson's disease in mice by inhibiting the NLRP3 inflammasome and protects PC12 cells against oxidative stress. Free Radic Biol Med. 2019 Apr;134:288-303. [2]. Zhen Dai, et al. Target Fishing Reveals a Novel Mechanism of 1,2,4-Oxadiazole Derivatives Targeting Rpn6, a Subunit of 26S Proteasome. J Med Chem. 2022 Mar 24;65(6):5029-5043.