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DDO-7263

Catalog No. T60487 CAS 2254004-96-9

DDO-7263 is a 1,2,4-Oxadiazole derivative that upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 is a potent Nrf2 activator that activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity [1].

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DDO-7263, CAS 2254004-96-9

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Purity: 98%

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Storage & Solubility Information

Description	DDO-7263 is a 1,2,4-Oxadiazole derivative that upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 is a potent Nrf2 activator that activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity [1].
In vitro	DDO-7263 (20 μM; 2-24 h) can upregulate the protein levels of NQO1 and HO-1. DDO-7263 (2.5, 5, 10, 20, 40, 80 μM; 24 h) can upregulate the survival rate of THP-Ms and PC12 cell after treatment of 400μM H2O2 in a concentration-dependent manner. DDO-7263 has no significant decrease on cell survival rate[1].
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 T1/2 of 3.32 hours and a Cmax of 1.38 mg/mL for rats[1].

Molecular Weight	273.24
Formula	C14H9F2N3O
CAS No.	2254004-96-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 16.1 mg/mL (58.8 mM), ultrasonic and warming and heat to 60°C

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

DDO-7263 2254004-96-9 Immunology/Inflammation Nrf2 Inhibitor inhibitor inhibit

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