Nrf2 activator 19
Based on 1 Customer Validation
Nrf2 activator 19 is a BBB-penetrable NRF2/HO-1 activator. Nrf2 activator 19 exerts potent antioxidant and neuroprotective effects. Nrf2 activator 19 can also effectively reduce brain damage, reduce Reactive Oxygen Species (ROS) accumulation. Nrf2 activator 19 inhibits neuronal apoptosis. Nrf2 activator 19 promotes the recovery of neurological function and motor ability. Nrf2 activator 19 shows significant potential in ischemic stroke research.
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- Pureté : 98.10%
- Formule: C25H20O5
- Masse moléculaire:400.42
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Nrf2 activator 19 (Compound 6p) (40 μM, 24 h) shows no cytotoxicity in PC12 cells and RAW cells, the viability of PC12 cells under t-BHP injury could reach more than 90%, demonstrating a strong protective effect[1].
Nrf2 activator 19 (2.5 μM-10 μM, 24 h) can effectively reduce ROS levels in PC12 cells, and shows a decrease in malondialdehyde (MDA) levels and an increase in superoxide dismutase (SOD) activity[1].
Nrf2 activator 19 (2.5 μM-10 μM, 24 h) increases the expression of NRF2 and HO-1 proteins in a concentration-dependent manner in PC12 cells, indicating that it protects against oxidative damage by activating the NRF2 pathway
Nrf2 activator 19 (10 μM, 3 h) reduces KEAP1 expression in PC12 cells, indicating a direct interaction with KEAP1[1].
Nrf2 activator 19 (1 μM, 1 h) shows moderate metabolic stability in rat liver microsomes[1].
Nrf2 activator 19 (10 μM, 24 h) shows a permeability of 7.64% in the Transwell-based blood-brain barrier (BBB) model (bEnd.3 cells), indicating its ability to cross the BBB[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:t-BHP (200 μM) treated PC12 cells
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Concentration:2.5 μM-20 μM
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Incubation Time:24 h
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Result:Demonstrated that it plays a protective role against oxidative damage by activating the NRF2 pathway, which not only reduced the levels of MDA and ROS, but also increased the expression of SOD and the antioxidant activity is as high as 95% at a concentration of 10 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MCAO rat model[1]
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Dosage:5-20 mg/kg
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Administration:i.v. , 7 consecutive days
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Result:Reduced the infarct area of rats, indicating that it has a protective effect on the nerve damage caused by cerebral ischemia-reperfusion.
Enhanced the expression of NRF2 and HO-1 proteins in the nucleus of rat cerebral ischemia-reperfusion injury (MCAO) model in a concentration-dependent manner, and counteract ischemia-reperfusion injury by activating the NRF2 pathway.
In the Barnes maze experiment, rats were able to find the target box quickly, indicating that it can effectively restore the nerve function of rats.
Chemical Information
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Appearance Solid
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Masse moléculaire 400.42
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Formule C25H20O5
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SMILES
OC1=CC=C(C(/C=C/C2=C3C(OC(C4=CC=C(C)C=C4)=C3)=C(OC)C=C2)=O)C=C1O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (249.74 mM; Need ultrasonic; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.24 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureté et documentation
Références
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 (sealed storage, away from moisture). 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 | 2.4974 mL | 12.4869 mL | 24.9738 mL | 62.4344 mL |
| 5 mM | 0.4995 mL | 2.4974 mL | 4.9948 mL | 12.4869 mL | |
| 10 mM | 0.2497 mL | 1.2487 mL | 2.4974 mL | 6.2434 mL | |
| 15 mM | 0.1665 mL | 0.8325 mL | 1.6649 mL | 4.1623 mL | |
| 20 mM | 0.1249 mL | 0.6243 mL | 1.2487 mL | 3.1217 mL | |
| 25 mM | 0.0999 mL | 0.4995 mL | 0.9990 mL | 2.4974 mL | |
| 30 mM | 0.0832 mL | 0.4162 mL | 0.8325 mL | 2.0811 mL | |
| 40 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | 1.5609 mL | |
| 50 mM | 0.0499 mL | 0.2497 mL | 0.4995 mL | 1.2487 mL | |
| 60 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0406 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL | |
| 100 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6243 mL |
Nrf2 activator 19 Related Classifications
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