| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Nrf2 activator 19 (compound 6p) (40 μM, 24 h) showed no cytotoxicity to PC12 cells and RAW cells. Under tert-butyl hydroperoxide (t-BHP) damage, the survival rate of PC12 cells could reach more than 90%, showing a strong protective effect [1]. Nrf2 activator 19 (2.5 μM-10 μM, 24 h) could effectively reduce the level of reactive oxygen species (ROS) in PC12 cells, reduce the level of malondialdehyde (MDA), and increase the activity of superoxide dismutase (SOD) [1]. Nrf2 activator 19 (2.5 μM-10 μM, 24 h) increased the expression of NRF2 and HO-1 proteins in PC12 cells in a concentration-dependent manner, indicating that it resists oxidative damage by activating the NRF2 pathway. Nrf2 activator 19 (10 μM, 3 h) could reduce the expression of KEAP1 in PC12 cells, indicating that it has a direct interaction with KEAP1 [1]. Nrf2 activator 19 (1 μM, 1 h) exhibited moderate metabolic stability in rat liver microsomes[1]. Nrf2 activator 19 (10 μM, 24 h) showed 7.64% permeability in a Transwell-based blood-brain barrier (BBB) model (bEnd.3 cells), indicating that it could cross the BBB[1].
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|---|---|
| ln Vivo |
Nrf2 activator 19 (5-20 mg/kg, intravenous injection, for 7 consecutive days) can improve the recovery of neurological function in a rat model of cerebral ischemia-reperfusion injury (MCAO) and prevent ischemia-reperfusion injury by activating the NRF2 pathway [1].
|
| Cell Assay |
Western Blot analysis [1]
Cell Types: PC12 cells treated with t-BHP (200 μM) Tested Concentrations: 2.5 μM-20 μM Incubation Duration: 24 hours Experimental Results: It was shown that it exerts a protective effect against oxidative damage by activating the NRF2 pathway, not only reducing the levels of MDA and ROS, but also increasing the expression of SOD. The antioxidant activity was as high as 95% at a concentration of 10 μM. |
| Animal Protocol |
Animal/Disease Models:MCAO rat model [1]
Doses: 5-20 mg/kg Route of Administration: Intravenous injection for 7 consecutive days Experimental Results: Reduced infarct area in rats, indicating a protective effect against cerebral ischemia-reperfusion injury. Enhanced the expression of NRF2 and HO-1 proteins in the nucleus of rats in a concentration-dependent manner, and counteracted ischemia-reperfusion injury by activating the NRF2 pathway. In the Barnes maze experiment, rats were able to quickly find the target box, indicating that it can effectively restore the nerve function of rats. |
| References |
| Molecular Formula |
C25H20O5
|
|---|---|
| Molecular Weight |
400.42
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
OC1=CC=C(C(/C=C/C2=C3C(OC(C4=CC=C(C)C=C4)=C3)=C(OC)C=C2)=O)C=C1O
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4974 mL | 12.4869 mL | 24.9738 mL | |
| 5 mM | 0.4995 mL | 2.4974 mL | 4.9948 mL | |
| 10 mM | 0.2497 mL | 1.2487 mL | 2.4974 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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