1. Neuronal Signaling
  2. AChE
  3. AChE/BChE-IN-1

AChE/BChE-IN-1 

Cat. No.: HY-131971
Handling Instructions

AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease.

For research use only. We do not sell to patients.

AChE/BChE-IN-1 Chemical Structure

AChE/BChE-IN-1 Chemical Structure

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Description

AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease[1].

IC50 & Target

IC50: 1.06 nM (hAChE); 7.3 nM (hBChE)[1]

In Vitro

AChE/BChE-IN-1 (compound 5i) is notactive against hBACE-1 at the tested concentration (1 μM)[1].
AChE/BChE-IN-1 scavenges the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical, with an IC50 of 92.0 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AChE/BChE-IN-1 (2 mg/kg; i.p. 3 times per week for 4 weeks) rescues learning and memory impairments, delays the Alzheimer-like pathology progression, improves basal synaptic efficacy, and significantly reduces hippocampal oxidative stress and neuroinflammation in 10 month-old APP/PS1 mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: AβPPswe/PS-1 double transgenic male mice (10 months)[1]
Dosage: 2 mg/kg
Administration: I.p. 3 times per week for 4 weeks
Result: Significantly enhanced learning and memory.
Reduced Aβ42/Aβ40 ratio in the hippocampus.
Increased the strength of synaptic transmission, without affecting long-term potentiation (LTP).
Decreased the levels of oxidative stress and neuroinflammation markers in the hippocampus.
Molecular Weight

587.11

Formula

C₃₂H₃₅ClN₆O₃

SMILES

OC1=C(C=C(C=C1)CNC(CC2=CN(N=N2)CCCCC3=C[[email protected]@H](C[[email protected]]4C3)CC5=C4C(N)=C6C(C=C(C=C6)Cl)=N5)=O)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

AChE/BChE-IN-1AChEAcetylcholinesterasedualButyrylcholinesterasehAChEhBChEantioxidantAlzheimerInhibitorinhibitorinhibit

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Product Name:
AChE/BChE-IN-1
Cat. No.:
HY-131971
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