Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 0.07 μM (eAChE); 0.38 μM (hAChE)[1]
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ln Vitro |
With IC50 values of 0.07 μM and 0.38 μM, respectively, AChE/Nrf2 modulator 1 (Compound 15a) exhibits strong Nrf2 induction and outstanding AChE inhibitory action on eeAChE and hAChE [1]. In addition to upregulating Nrf2's transcription and protein levels, as well as those of its downstream proteins HO1, NQO1, and GCLM, AChE/Nrf2 modulator 1 (5, 20 μM; 5–12 h) facilitates Nrf2's movement from the cytoplasm to the nucleus [1]. Significant neuroprotective actions of AChE/Nrf2 modulator 1 (1, 2.5, 5, 10, 20, 40 μM) include shielding cells from oxidative stress and Aβ1-42 aggregation-induced cell damage, promoting antioxidant stress and anti-inflammatory properties, and lowering ROS and pro-inflammatory cytokine production [1].
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ln Vivo |
For Morris water induction by scopolamine and Aβ1-42 Trajectories, AChE/Nrf2 modulator 1 (Compound 15a) (oral; 10 mg/kg; 10 consecutive days) efficiently reduces the latency and escape distance to the target, lengthens arrival time, and streamlines the process[1]. Pro-inflammatory factor levels in mouse model brains can be markedly decreased by AChE/Nrf2 modulator 1[1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: PC12 cells Tested Concentrations: 20 μM; 5, 20 μM Incubation Duration: 5-10 h; 6 h Experimental Results: Dramatically activated the expression of Nrf2 downstream proteins. Increase the level of Nrf2 and its downstream protein HO-1, NQO1, and GCLM in a dose-dependent manner at 6 h. Increased the translocation of Nrf2 into the nucleus. RT-PCR[1] Cell Types: PC12 cells Tested Concentrations: 20 μM Incubation Duration: 0, 1, 2 , 5, 10, 24 h Experimental Results: Increased the Nrf2, HO-1, NQO1, and GCLM gene expression in dose dependent manner. Immunofluorescence[1] Cell Types: PC12 cells Tested Concentrations: 5, 20 μM Incubation Duration: 12 h Experimental Results: Induced the Nrf2 translocation into the nucleus in dose dependent manner. |
Animal Protocol |
Animal/Disease Models: ICR mice[1]
Doses: 10, 20 mg/kg Route of Administration: intragastric (po) administration; oral; for 10 days Experimental Results: Dramatically decreased the latency time to target and simplified the traveled distance and demonstrated a good effect on ameliorating ethological changes and memory spatial impairment by rescuing cholinergic function. demonstrated an obvious reduction of pro-inflammation factors level and Dramatically increased the content of TGF-β1. |
References |
[1]. Yuanyuan Wang, et al. Design, synthesis and evaluation of fused hybrids with acetylcholinesterase inhibiting and Nrf2 activating functions for Alzheimer's disease. Eur J Med Chem. 2022 Dec 15;244:114806.
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Molecular Formula |
C27H27FN4O2
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Molecular Weight |
458.53
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CAS # |
2417117-84-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
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 | 2.1809 mL | 10.9044 mL | 21.8088 mL | |
5 mM | 0.4362 mL | 2.1809 mL | 4.3618 mL | |
10 mM | 0.2181 mL | 1.0904 mL | 2.1809 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.