2. Neuronal Signaling Immunology/Inflammation
  3. Cholinesterase (ChE) COX
  4. BChE-IN-46

BChE-IN-46 is a selective and brain-penetrant BChE inhibitor (eqBChE IC50 = 7.44 × 10−5 μM, SI > 270,000; hBChE, IC50 = 1.48 × 10−3 μM). BChE-IN-46 has COX-2 inhibitory activity (IC50 = 0.11 μM). BChE-IN-46 exhibits neuroprotective effects, enhances acetylcholine levels, and alleviates cognitive deficits, anxiety, and learning/memory impairments. BChE-IN-46 can be used for the development of anti-Alzheimer's disease drugs.

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

BChE-IN-46

BChE-IN-46 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

BChE-IN-46 Related Antibodies

Top Publications Citing Use of Products

View All Cholinesterase (ChE) Isoform Specific Products:

View All Isoforms
AChE BChE

View All COX Isoform Specific Products:

View All Isoforms
COX COX-1 COX-2 COX-3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BChE-IN-46 is a selective and brain-penetrant BChE inhibitor (eqBChE IC50 = 7.44 × 10−5 μM, SI > 270,000; hBChE, IC50 = 1.48 × 10−3 μM). BChE-IN-46 has COX-2 inhibitory activity (IC50 = 0.11 μM). BChE-IN-46 exhibits neuroprotective effects, enhances acetylcholine levels, and alleviates cognitive deficits, anxiety, and learning/memory impairments. BChE-IN-46 can be used for the development of anti-Alzheimer's disease drugs[1].

IC50 & Target[1]

COX-2

0.11 μM (IC50)

hBCHE

1.48 nM (IC50)

eqBCHE

74.4 pM (IC50)

In Vitro

BChE-IN-46 (Compound 17) (100 μM, 24 h) possesses the promising in vitro cell safety in BV2, PC12 and HT22 cell[1].
BChE-IN-46 (5-20 μM, 24 h) has anti-inflammatory activity in Lipopolysaccharides (LPS) (HY-D1056)-induced BV2 cells[1].
BChE-IN-46 (10-40 μM, 24 h) has neuroprotective effects against Aβ in β-Amyloid (1-42) (Aβ1-42) (HY-P1363)-induced injury in PC12 cells[1].

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

BChE-IN-46 Related Antibodies

Cell Viability Assay[1]

Cell Line: BV2, PC12 and HT22 cell
Concentration: 100 μM
Incubation Time: 24 h
Result: Exhibited weak or no toxicity on BV2, PC12 and HT22 cell.

ELISA Assay[1]

Cell Line: LPS (1 μg/mL)-induced BV2 cells
Concentration: 5, 10, and 20 μM
Incubation Time: 24 h
Result: Reduced LPS-induced NO, IL-6, and TNF-α production in a concentration-dependent manner.

Cell Viability Assay[1]

Cell Line: Aβ1-42-induced PC12 cell
Concentration: 10, 20, and 40 μM
Incubation Time: 24 h
Result: Exhibited a dose-dependent protection against Aβ1-42-induced toxicity in PC12 cells and the protective efficacy.
In Vivo

BChE-IN-46 (compound 17) (3-25 mg/kg, i.p., once daily, 16 days) improves Scopolamine (HY-N0296)-induced cognitive deficits, anxiety, and learning/memory impairments in male Kunming mice[1].
BChE-IN-46 (250 mg/kg, i.p., once) inherits favorable in vivo safety in Kunming mice[1].
BChE-IN-46 (100 mg/kg, i.p., once) has effective BBB penetration and CSF retention in male SD rats[1].

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

Animal Model: Scopolamine (3 mg/kg, i.p.) -induced male Kunming mice (25 g-30 g, 6 weeks)[1].
Dosage: 3, 12.5, 25 mg/kg
Administration: i.p., once daily, 16 days
Result: Increased both movement distance and residence time in the central region.
Produces no cholinergic adverse effects or motor deficits in mice.
Reduced path length.
Ameliorated scopolamine-induced cholinergic dysfunction primarily through BChE inhibition-mediated ACh restoration.
Attenuated increases in hippocampal TNF-α and IL-6.
Reversed the scopolamine-induced reduction in Nissl positive neurons and ameliorated neuronal damage.
Animal Model: Kunming mice (30 g-35 g, 6 weeks)[1].
Dosage: 250 mg/kg
Administration: i.p., once, dissolved in a mixed solvent composed of DMSO (HY-Y0320C), HS-15 (HY-Y1893), castor oil (HY-107799) and normal saline (HY-W460471) (8/5/5/82, V/V/V/V).
Result: Had no mortality or treatment-related abnormalities.
Did not significantly alter the mean body weight.
Resulted in normal tissue architecture in major organs, with no treatment-related lesions observed.
Animal Model: male SD rats (220 g-250 g, 8 weeks)[1].
Dosage: 100 mg/kg
Administration: i.p., once
Result: Maintained sustained concentrations in cerebrospinal fluid (CSF) between 20 min and 2 h.
Molecular Weight

420.50

Formula

C24H28N4O3
SMILES

CC(C=C1)=CC(OC(N2CCC2)=O)=C1C(NCCC3=CNC4=CC(N(C)C)=CC=C43)=O
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

BChE-IN-46 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

BChE-IN-46Cholinesterase (ChE)COXCyclooxygenaseAlzheimer's diseaseBChEblood-brain barrierCOX-2Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
BChE-IN-46
Cat. No.:
HY-179363
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.