1. Neuronal Signaling
  2. Cholinesterase (ChE) Amyloid-β Tau Protein
  3. BChE-IN-41

BChE-IN-41 is a highly selective Butyrylcholinesterase (BChE) inhibitor (IC50 =12 nM, Ki = 6.6 nM). BChE-IN-41 has high brain penetration with a brain-to-plasma ratio of 9.0. BChE-IN-41 has pro-cognitive effects on mice with AD-like symptoms induced by Scopolamine (HY-N0296) and Aβ1-42.

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BChE-IN-41 Chemical Structure

BChE-IN-41 Chemical Structure

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Description

BChE-IN-41 is a highly selective Butyrylcholinesterase (BChE) inhibitor (IC50 =12 nM, Ki = 6.6 nM). BChE-IN-41 has high brain penetration with a brain-to-plasma ratio of 9.0. BChE-IN-41 has pro-cognitive effects on mice with AD-like symptoms induced by Scopolamine (HY-N0296) and Aβ1-42[1].

IC50 & Target

hAChE

22110 nM (IC50)

In Vitro

BChE-IN-41 (Compound (R)-(−)-3) (5 μM, 48 h) exhibits neuroprotective activity by diminishing Aβ1−42-induce SH-SY5Y cells death[1].

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

Cell Viability Assay[1]

Cell Line: HepG2 cells, SH-SY5Y cells
Concentration: 1 μM, 5 μM, 10 μM, 20 μM, 50 μM, 100 μM
Incubation Time: 48 h
Result: Had comparable cytotoxicity profiles in both HepG2 cells and SH-SY5Y cells.

Cell Cytotoxicity Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 2.5 μM, 5 μM
Incubation Time: 48 h
Result: Reversed Aβ toxicity and reduced cell death at 5 μM; its effect was not significant at 2.5 μM.
In Vivo

BChE-IN-41 (Compound (R)-(−)-3) (10-100 mg/kg, i.g, sing dose) is highly potent and has high brain penetration and low toxicity in wild-type Balb/c mice, with no histopathological changes in mice[1].
BChE-IN-41 (1-10 mg/kg, i.p, sing dose) improves contextual memory deficits and recognition memory deficits in adult male CD-1 mice induced by scopolamine[1].
BChE-IN-41 (10 mg/kg, i.p, at the corresponding doses for 14 days) improves learning ability and cognitive function in ICR male mice induced by Aβ1-42 oligomers[1].

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

Animal Model: Female and male wild-type Balb/c mice (3 months)[1]
Dosage: 10 mg/kg, 100 mg/kg
Administration: Oral gavage (i.g.), sing dose
Result: Exhibited high brain penetration with a brain-to-plasma ratio of 9.0.
Caused no mortality or tissue lesions in mice, and no abnormalities were found in histological examination.
Caused steady weight gain with no signs of acute toxicity.
Animal Model: Scopolamine (HY-N0296) (1 mg/kg, s.c) induced AD model in adult male CD-1 mice (18-22 g)[1]
Dosage: 1 mg/kg, 10 mg/kg
Administration: Intraperitoneal injection (i.p.), sing dose
Result: Prolonged the latency to enter the dark chamber and improved the contextual memory deficit.
Demonstrated prolonged step-through latency compared to mice treated with scopolamine only.
Enhanced preference for novel objects and increased the discrimination index (DI) and reversed the recognition memory deficit.
Animal Model: Aβ1-42 oligomers (10 µg per mouse, i.c.v) induced AD-like cognitive deficits model in ICR male mice (8-10 weeks, 18−20 g)[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), at the corresponding doses for 14 days.
Result: Caused no motor impairment in the rotarod test (6/18/24 rpm).
Resulted in shorter escape latency and shorter distance to reach the target area, and improved Aβ1-42-induced cognitive deficits.
Molecular Weight

394.53

Formula

C23H26N2O2S

SMILES

CN(S(=O)(C1=CC=C(C=CC=C2)C2=C1)=O)C[C@@H](C3)CCN3CC4=CC=CC=C4

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:
BChE-IN-41
Cat. No.:
HY-174381
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