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.
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- CAS No.: 2417117-84-9
- Formule: C27H27FN4O2
- Masse moléculaire:458.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
IC50: 0.07 μM (eAChE); 0.38 μM (hAChE)[1]
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.
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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.
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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Masse moléculaire 458.53
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE/Nrf2 modulator 1 Related Classifications
HY-152037 Related Classifications
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