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Art. -Nr.: HY-190812

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BChE-IN-57

BChE-IN-57 is a mixed-type, selective BChE inhibitor with IC₅₀ values of 0.20 and 0.35 μM for eqBChE and hBChE, respectively. BChE-IN-57 reduces hydrogen peroxide-induced intracellular ROS accumulation and mitochondrial membrane potential loss through antioxidant protection. BChE-IN-57 inhibits the production of NO and pro-inflammatory cytokines and downregulates inflammatory enzyme markers. BChE-IN-57 chelates metal ions, including copper. BChE-IN-57 can be used for research on Alzheimer's disease.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₅H₂₃FN₄O
Molecular Weight:414.47

Speicherung:

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

BChE-IN-57 Chemical Structure

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

eqBCHE

0.20 μM (IC₅₀)

hBCHE

0.35 μM (IC₅₀)

eel AChE

>50 μM (IC₅₀)

Alle Cholinesterase (ChE) Isoform-spezifische Produkte anzeigen :

AChE
BChE

Alle NO Synthase Isoform-spezifische Produkte anzeigen :

In Vitro

Innate ImmunityCytokines and ChemokinesOxidative StressMitochondrial FunctionOthers

Innate Immunity

BChE-IN-57 (5-20 µM; 4 h) downregulates LPS-induced iNOS and COX-2 expression in BV2 cells^[1].

Innate Immunity

Cytokines and Chemokines

BChE-IN-57 (2.5-20 µM) dose-dependently inhibits LPS-induced production of NO, TNF-α, and IL-1β in BV2 cells^[1].

Oxidative Stress

BChE-IN-57 (1.25-10 μM; 4 h) protects HT22 cells against H₂O₂-induced loss of cell viability^[1].
BChE-IN-57 (5-10 µM; 4 h) inhibits H₂O₂-induced intracellular ROS accumulation in HT22 cells^[1].

Oxidative Stress

Mitochondrial Function

BChE-IN-57 (5-10 µM; 4 h) attenuates H₂O₂-induced mitochondrial membrane potential dissipation in HT22 cells^[1].

Others

BChE-IN-57 (Compound 6j) (10-20 min) potently inhibits eqBChE (IC₅₀ 0.20 µM) and hBChE (0.35 µM), with over 250-fold selectivity over eeAChE^[1].
BChE-IN-57 (100-400 nM; 20 min) inhibits eqBChE in a mixed-type manner with a K_i of 0.112 µM^[1].
BChE-IN-57 (6.25-100 µM) exhibits a favorable safety profile in HT22, BV2, and L02 cells, showing certain toxicity only at 50 and 100 µM^[1].

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

Cell Viability Assay^[1]

Cell Line:

HT22 cells
Concentration:

non-toxic concentrations (1.25-10 μM)
Incubation Time:

4 h (pre-incubation); 12 h (H2O2 exposure)
Result:

Improved the viability of H₂O₂-exposed cells to varying degrees.

Western Blot Analysis^[1]

Cell Line:

BV2 microglial cells
Concentration:

5, 10, 20 µM
Incubation Time:

4 h (pre-incubation)
Result:

LPS challenge significantly upregulated iNOS and COX-2.
At 20 µM, significantly downregulated both iNOS and COX-2 expression compared with the LPS-challenged group.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	MRT_0-t
Mice^[1]	40 mg/kg	p.o.	4.09 h	1.33 h	215.01 ng/mL	958.38 ng·h/mL	4.18 h

In Vivo

BChE-IN-57 (1000 mg/kg; oral; single dose) is well tolerated in mice^[1].

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

Animal Model:

Healthy C57BL mice^[1]
Dosage:

1000 mg/kg
Administration:

p.o.
Result:

Showed that the physiological state of the mice is normal, as evidenced by stable food and water intake and continuous body weight gain.
No obvious abnormal behaviors or other clinical signs were observed.

Related Protocols :

Chemical Information

Molecular Weight 414.47
Formel C₂₅H₂₃FN₄O
SMILES

O=C(C1=CC(C2=NC=CC=C2)=NC3=CC=CC=C13)NCCN(CC4=CC=C(F)C=C4)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Gao H, et al. Virtual screening, structural optimization, computational studies, and biological evaluation of quinoline derivatives as selective butyrylcholinesterase inhibitors. Bioorganic chemistry. 2026 Oct 05;183:110617.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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BChE-IN-57

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