DDO-7263
Based on 1 publication(s) in Google Scholar
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).
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- Purity : 99.83%
- CAS No.: 2254004-96-9
- 화학식: C14H9F2N3O
- 분자량:273.24
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DDO-7263
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Biological Activity
제품 설명
In Vitro
DDO-7263 (20 μM; 2-24 h) can upregulate the protein levels of HO-1 and NQO1 in concentration-dependent manners[1].
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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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC12 cells
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Concentration:20 μM
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Incubation Time:2, 4, 8, 12, 24 hours
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Result:Upregulated the protein levels of HO-1 and NQO1 in concentration-dependent manners.
In Vivo
? 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice at 10 weeks of age and body weights of 22-26 g[1]
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Dosage:10, 50, 100 mg/kg
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Administration:IP; daily for 10 days
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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.
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Animal Model:SD rats[1]
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Dosage:7, 35, 70 mg/kg (Pharmacokinetic Analysis)
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Administration:IP
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Result:Had a T1/2 of 3.32 hours and a Cmax of 1.38 mg/mL.
Chemical Information
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CAS No. 2254004-96-9
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Appearance Solid
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분자량 273.24
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화학식 C14H9F2N3O
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Color White to off-white
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SMILES
CC1=NC=C(C2=NOC(C3=CC(F)=C(C=C3)F)=N2)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
In Vitro:
DMSO : 17.86 mg/mL (65.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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 protec [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6598 mL | 18.2989 mL | 36.5979 mL | 91.4947 mL |
| 5 mM | 0.7320 mL | 3.6598 mL | 7.3196 mL | 18.2989 mL | |
| 10 mM | 0.3660 mL | 1.8299 mL | 3.6598 mL | 9.1495 mL | |
| 15 mM | 0.2440 mL | 1.2199 mL | 2.4399 mL | 6.0996 mL | |
| 20 mM | 0.1830 mL | 0.9149 mL | 1.8299 mL | 4.5747 mL | |
| 25 mM | 0.1464 mL | 0.7320 mL | 1.4639 mL | 3.6598 mL | |
| 30 mM | 0.1220 mL | 0.6100 mL | 1.2199 mL | 3.0498 mL | |
| 40 mM | 0.0915 mL | 0.4575 mL | 0.9149 mL | 2.2874 mL | |
| 50 mM | 0.0732 mL | 0.3660 mL | 0.7320 mL | 1.8299 mL | |
| 60 mM | 0.0610 mL | 0.3050 mL | 0.6100 mL | 1.5249 mL |
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