2. Neuronal Signaling NF-κB
  3. Cholinesterase (ChE) Keap1-Nrf2
  4. 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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AChE/Nrf2 modulator 1 Chemical Structure

AChE/Nrf2 modulator 1 Chemical Structure

CAS No. : 2417117-84-9

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AChE/Nrf2 modulator 1 Related Antibodies

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Description

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[1].

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.

AChE/Nrf2 modulator 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 20 μM; 5, 20 μM
Incubation Time: 5-10 h; 6 h
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.

RT-PCR[1]

Cell Line: PC12 cells
Concentration: 20 μM
Incubation Time: 0, 1, 2, 5, 10, 24 h
Result: Increased the Nrf2, HO-1, NQO1, and GCLM gene expression in dose dependent manner.

Immunofluorescence[1]

Cell Line: PC12 cells
Concentration: 5, 20 μM
Incubation Time: 12 h
Result: Induced the Nrf2 translocation into the nucleus in dose dependent manner.
In Vivo

AChE/Nrf2 modulator 1 (Compound 15a) (oral; 10 mg/kg; for 10 consecutive days) effectively shortens the latency time and escape distance to the target, increased the arrival times, and simplified the tracks in Morris water maze test induced by scopolamine and Aβ1-42[1].
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.

Animal Model: ICR mice[1]
Dosage: 10, 20 mg/kg
Administration: Intragastric administration; oral; for 10 consecutive days
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.
Molecular Weight

458.53

Formula

C27H27FN4O2
CAS No.
SMILES

CC1=CC=C(C=N1)C2=NOC(C3=CC(OCC4CCN(CC4)CC5=CC(F)=CC=C5)=CC=C3)=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AChE/Nrf2 modulator 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AChE/Nrf2 modulator 12417117-84-9Cholinesterase (ChE)Keap1-Nrf2Designing of multiple-target directed ligands (MTDLs)Alzheimer's disease (AD)acetylcholinesterase (AChE)nuclear factor erythroid 2-related factor 2 (Nrf2)eeAChEhAChEInhibitorinhibitorinhibit

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