1. Neuronal Signaling Others
  2. Cholinesterase (ChE) Drug Intermediate
  3. BuChE-IN-22

BuChE-IN-22 is a pseudo-irreversible butyrylcholinesterase (BuChE) inhibitor, with IC50 values of 4 nM and 157 nM against hBuChE and hAChE, respectively. It also acts as a prodrug of 7-hydroxysertraline. BuChE-IN-22 releases 7-hydroxysertraline during BuChE inhibition. BuChE-IN-22 completely reverses Aβ25-35-induced short-term and long-term memory impairments in a mouse model of Alzheimer's disease. BuChE-IN-22 can be used in research related to Alzheimer's disease.

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

BuChE-IN-22

BuChE-IN-22 Chemical Structure

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Description

BuChE-IN-22 is a pseudo-irreversible butyrylcholinesterase (BuChE) inhibitor, with IC50 values of 4 nM and 157 nM against hBuChE and hAChE, respectively. It also acts as a prodrug of 7-hydroxysertraline. BuChE-IN-22 releases 7-hydroxysertraline during BuChE inhibition. BuChE-IN-22 completely reverses Aβ25-35-induced short-term and long-term memory impairments in a mouse model of Alzheimer's disease. BuChE-IN-22 can be used in research related to Alzheimer's disease[1].

IC50 & Target[1]

hBCHE

4 nM (IC50)

hAChE

157 nM (IC50)

In Vitro

BuChE-IN-22 (Compound 8e) (255 μM; 48 h) remains stable in the absence of hBuChE, but is completely metabolized by hBuChE within 48 h, releasing 85% of the serotonin reuptake inhibitor HO-Sert[1].

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

In Vivo

BuChE-IN-22 (Compound 8e) (0.3-3 mg/kg; i.p.; daily; 7 days) completely prevents Aβ25-35-induced spatial working memory deficits at 3 mg/kg and long-term non-spatial memory deficits at 1 mg/kg in a mouse model of Alzheimer's disease[1].

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

Animal Model: Swiss mice (male, 6 weeks old, 30-35 g, intracerebroventricular injection of 9 nmol oligomeric Aβ25-35 peptide)[1]
Dosage: 0.3 mg/kg; 1 mg/kg (long-term non-spatial memory); 3 mg/kg (spatial working memory)
Administration: i.p.; daily; 7 days (starting 20 minutes post-Aβ25-35 injection)
Result: Completely prevented Aβ25-35-induced deficits in spontaneous alternation (spatial working memory) at 3 mg/kg.
Completely prevented Aβ25-35-induced deficits in passive avoidance retention latency (long-term non-spatial memory) at 1 mg/kg.
Molecular Weight

433.37

Formula

C23H26Cl2N2O2

SMILES

CN[C@H]1CC[C@@H](C2=CC=C(Cl)C(Cl)=C2)C3=C1C=C(OC(N4CCCCC4)=O)C=C3

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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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.

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Product Name:
BuChE-IN-22
Cat. No.:
HY-181865
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