| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
DDO-7263 targets Nrf2 (nuclear factor erythroid 2-related factor 2), a master regulator of the antioxidant response, and the 26S proteasome. By binding to Rpn6, a subunit of the 26S proteasome, DDO-7263 blocks the assembly of the proteasome and prevents the degradation of ubiquitinated Nrf2. This leads to Nrf2 accumulation and activation of the Nrf2-ARE signaling pathway, which upregulates antioxidant and cytoprotective genes.
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| ln Vitro |
In a concentration-dependent manner, DDO-7263 (20 μM; 2-24 h) can increase the levels of HO-1 and NQO1 proteins [1]. At 400 μM H2O2, PC12 and THP-Ms cells can be upregulated by DDO-7263 (2.5, 5, 10, 20, 40, 80 μM; 24 h) in a concentration-dependent way. Cell viability is not substantially decreased by DDO-7263 alone [1].
DDO-7263 is a potent Nrf2-ARE activator that upregulates Nrf2 through binding to Rpn6 to block the assembly of the 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. It activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity. The compound inhibits NLRP3 inflammasome activation and shows neuroprotective effects. DDO-7263 has potential for neurodegenerative disease research, such as Parkinson's disease. |
| ln Vivo |
DDO-7263 (10-100 mg/kg/day; i.p.; for 10 days) dramatically reduces chemically induced dopaminergic neuron tyrosine hydroxylase in the substantia nigra (SN) (TH) loss and mouse brain striatum, as well as inhibits the secretion of inflammatory factors. It also improves MPTP-induced behavioral abnormalities in mice [1]. In rats, DDO-7263 (7, 35, 70 mg/kg; IP) had a Cmax of 1.38 mg/mL and a T1/2 of 3.32 hours [1].
In vivo, DDO-7263 exerts anti-inflammatory activity and has potential for neurodegenerative disease research, such as Parkinson's disease. As a potent Nrf2 activator, it is expected to provide neuroprotection by upregulating antioxidant defenses and reducing inflammation in vivo. Specific in vivo efficacy studies and animal model data are not extensively detailed in the public domain. The compound is intended for research use only. |
| Enzyme Assay |
The in vitro enzyme/receptor binding assay for DDO-7263 typically involves measuring its binding to Rpn6 or its effects on Nrf2-ARE activation. For Nrf2-ARE activation, cells are treated with varying concentrations of DDO-7263 (typically 0.001-100 µM) and ARE-driven luciferase reporter activity is measured. For Rpn6 binding, surface plasmon resonance (SPR) or pull-down assays can be performed. The compound is dissolved in DMSO and diluted in assay buffer.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: PC12 cells Tested Concentrations: 20 μM Incubation Duration: 2, 4, 8, 12, 24 hrs (hours) Experimental Results: Upregulated the protein levels of HO-1 and NQO1 in concentration-dependent manners. In vitro cellular assays for DDO-7263 typically involve treating cells with the compound at concentrations ranging from 0.001 to 10 µM for various time periods. Nrf2 protein levels are assessed by Western blot. Nrf2-ARE target gene expression (such as HO-1, NQO1) is measured by qPCR. NLRP3 inflammasome activation is assessed by measuring IL-1β and IL-18 production by ELISA. Cell viability is assessed using MTT or other standard assays. The compound is dissolved in DMSO and diluted in cell culture medium. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice at 10 weeks of age and body weights of 22-26 g[1]
Doses: 10, 50, 100 mg/kg Route of Administration: IP; daily for 10 days Experimental Results: 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. Dramatically downregulated the levels of pro-inflammatory factors, including IL-1β and TNF-α, in mouse plasma. Animal/Disease Models: SD rats[1] Doses: 7, 35, 70 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: IP Experimental Results: Had a T1/2 of 3.32 hrs (hours) and a Cmax of 1.38 mg/mL. In vivo animal studies for DDO-7263 are not extensively documented. For potential in vivo applications, the compound could be administered to mice via oral gavage or intraperitoneal injection at doses determined from preliminary studies. Parkinson's disease models or other neurodegenerative disease models could be used to evaluate neuroprotective efficacy. Brain tissue is collected for histological and biochemical analysis. Nrf2 target gene expression and inflammatory markers are assessed. |
| ADME/Pharmacokinetics |
DDO-7263 has a molecular weight of 273.24 g/mol and formula C14H9F2N3O. The compound is a 1,2,4-oxadiazole derivative. It is soluble in DMSO and other organic solvents. Recommended storage is typically -20°C for powder and -80°C for solvent. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination.
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| Toxicity/Toxicokinetics |
DDO-7263 is intended for research use only and is not approved for human therapeutic applications. As an Nrf2 activator that modulates the proteasome, the compound may affect normal cellular processes, which could contribute to potential toxicity. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. Appropriate safety precautions should be taken when handling.
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| References |
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| Additional Infomation |
DDO-7263 (CAS 2254004-96-9) is a potent small molecule Nrf2-ARE activator with a molecular weight of 273.24 g/mol and formula C14H9F2N3O. It upregulates Nrf2 through binding to Rpn6 to block 26S proteasome assembly. DDO-7263 activates the Nrf2-ARE signaling pathway, exerts anti-inflammatory activity, inhibits NLRP3 inflammasome activation, and shows neuroprotective effects. It has potential for neurodegenerative disease research, such as Parkinson's disease.
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| Molecular Formula |
C14H9F2N3O
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| Molecular Weight |
273.24
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| Exact Mass |
273.07
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| Elemental Analysis |
C, 61.54; H, 3.32; F, 13.91; N, 15.38; O, 5.86
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| CAS # |
2254004-96-9
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| PubChem CID |
145989809
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| Appearance |
White to off-white solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
334
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=NC=C(C=C1)C2=NOC(=N2)C3=CC(=C(C=C3)F)F
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| InChi Key |
HITVBBDLWZDVIV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H9F2N3O/c1-8-2-3-10(7-17-8)13-18-14(20-19-13)9-4-5-11(15)12(16)6-9/h2-7H,1H3
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| Chemical Name |
5-(3,4-difluorophenyl)-3-(6-methylpyridin-3-yl)-1,2,4-oxadiazole
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| Synonyms |
DDO-7263; DDO7263; DDO 7263;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~17.86 mg/mL (~65.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.79 mg/mL (6.55 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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