DDO-7263

CAS号

2254004-96-9

分子式

C14H9F2N3O

主要靶点

Nrf2

仅限科研使用

Cat No : CM10550

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Synonyms

Nrf2



产品信息

CAS号 2254004-96-9
分子式 C14H9F2N3O
主要靶点 Nrf2
主要通路 免疫与炎症
分子量 273.24
纯度 99.75%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Shipping with blue ice.
别名 Nrf2

体内活性

DDO-7263(10-100 mg/kg/天;IP方式;持续10天)能显著改善MPTP在小鼠中引起的行为异常,显著减少化学诱导的小鼠脑黑质(SN)和纹状体中多巴胺神经元失去酪氨酸羟化酶(TH)的现象,并抑制炎症因子的分泌。DDO-7263(7, 35, 70 mg/kg;IP)在大鼠体内的半衰期为3.32小时,最大血药浓度(Cmax)为1.38 mg/mL[1]。

体外活性

DDO-7263(20 μM; 2-24小时)能够上调NQO1与HO-1的蛋白水平。DDO-7263(2.5、5、10、20、40、80 μM; 24小时)在处理400μM H2O2后,能够以浓度依赖的方式上调THP-Ms及PC12细胞的存活率。DDO-7263对细胞存活率没有显著降低[1]。

溶解度

DMSO:16.1 mg/mL (58.8 mM)

参考文献

1.Xu LL, 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.Dai Z, 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.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2