AChE/Nrf2 modulator 1
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 2417117-84-9
- Formula: C27H27FN4O2
- Molecular Weight:458.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
IC50: 0.07 μM (eAChE); 0.38 μM (hAChE)[1]
In Vitro
AChE/Nrf2 modulator 1 (Compound 15a) has significant Nrf2 inductivity and excellent AChE inhibitory for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively[1].
AChE/Nrf2 modulator 1 (5, 20 μM; 5-12 h) upregulates the protein and transcription level of Nrf2 and the downstream proteins HO1, NQO1, and GCLM and promotes Nrf2 translocation from cytoplasm into nuclei[1].
AChE/Nrf2 modulator 1 (1, 2.5, 5, 10, 20, 40 μM) exhibits important neuroprotective function in protecting the cells from being damaged by H202 and Aβ1-42 aggregation and exertes antioxidant stress and anti-inflammatory activities in reducing the production of ROS and pro-inflammatory cytokines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:PC12 cells
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Concentration:20 μM; 5, 20 μM
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Incubation Time:5-10 h; 6 h
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Result:Significantly 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.
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Cell Line:PC12 cells
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Concentration:20 μM
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Incubation Time:0, 1, 2, 5, 10, 24 h
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Result:Increased the Nrf2, HO-1, NQO1, and GCLM gene expression in dose dependent manner.
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Cell Line:PC12 cells
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Concentration:5, 20 μM
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Incubation Time:12 h
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Result:Induced the Nrf2 translocation into the nucleus in dose dependent manner.
In Vivo
AChE/Nrf2 modulator 1 (10, 20 mg/kg; intragastric administration) significantly reduces the levels of proinflammatory factors in the mice model brains[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice[1]
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Dosage:10, 20 mg/kg
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Administration:Intragastric administration; oral; for 10 consecutive days
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Result:Significantly reduced the latency time to target and simplified the traveled distance and exhibited a good effect on ameliorating ethological changes and spatial memory impairment by rescuing cholinergic function
. Showed an obvious reduction of pro-inflammation factors level and significantly increased the content of TGF-β1.
Chemical Information
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CAS No. 2417117-84-9
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Molecular Weight 458.53
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Formula C27H27FN4O2
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SMILES
CC1=CC=C(C=N1)C2=NOC(C3=CC(OCC4CCN(CC4)CC5=CC(F)=CC=C5)=CC=C3)=N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE/Nrf2 modulator 1 Related Classifications
HY-152037 Related Classifications
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