DDO-7263|cas:2254004-96-9|西域试剂

DDO-7263,99.63%

产品编号：Bellancom-144634| CAS NO：2254004-96-9| 分子式：C₁₄H₉F₂N₃O| 分子量：273.24

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货号	价格	库存与货期
Bellancom-144634	￥2500.00	杭州北京（现货）
Bellancom-144634	￥4200.00	杭州北京（现货）
Bellancom-144634	￥9200.00	杭州北京（现货）
Bellancom-144634	￥15000.00	杭州北京（现货）

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DDO-7263

产品介绍

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。

生物活性

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).

体外研究

DDO-7263 (20 μM; 2-24 h) can upregulate the protein levels of HO-1 and NQO1 in concentration-dependent manners.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell 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.

体内研究
(In Vivo)

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 T_1/2 of 3.32 hours and a C_max of 1.38 mg/mL for rats.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6 mice at 10 weeks of age and body weights of 22-26 g
Dosage:	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 T_1/2 of 3.32 hours and a C_max of 1.38 mg/mL.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6 mice at 10 weeks of age and body weights of 22-26 g
Dosage:	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 T_1/2 of 3.32 hours and a C_max of 1.38 mg/mL.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6 mice at 10 weeks of age and body weights of 22-26 g
Dosage:	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 T_1/2 of 3.32 hours and a C_max of 1.38 mg/mL.

性状

Solid

溶解性数据

In Vitro:

DMSO : 17.86 mg/mL (65.36 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6598 mL	18.2989 mL	36.5979 mL
5 mM	0.7320 mL	3.6598 mL	7.3196 mL
10 mM	0.3660 mL	1.8299 mL	3.6598 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: 1.79 mg/mL (6.55 mM); Clear solution; Need ultrasonic

此方案可获得 1.79 mg/mL (6.55 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 17.9 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。