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Art. -Nr.: HY-143413

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BuChE-IN-2

BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC₅₀s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu²⁺, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease.

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CAS. Nr.: 2745118-93-6
Formel: C₂₈H₂₀F₄N₆O₃
Molecular Weight:564.49

Speicherung:

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

Data Sheet (271 KB)

BuChE-IN-2 Chemical Structure

CAS. Nr.: 2745118-93-6

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 1.28 μM (BuChE), 0.67 μM (NO)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BV-2	IC₅₀	0.67 μM Compound: F9	Inhibition of NO production in LPS-induced mouse BV-2 cells pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA Inhibition of NO production in LPS-induced mouse BV-2 cells pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA	[PMID: 34752955]
BV-2	IC₅₀	1.61 μM Compound: F9	Inhibition of LPS-induced IL-1beta secretion in mouse BV-2 cells preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA Inhibition of LPS-induced IL-1beta secretion in mouse BV-2 cells preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA	[PMID: 34752955]
BV-2	IC₅₀	4.15 μM Compound: F9	Inhibition of LPS-induced TNF-alpha secretion in mouse BV-2 cells preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA Inhibition of LPS-induced TNF-alpha secretion in mouse BV-2 cells preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA	[PMID: 34752955]

In Vitro

BuChE-IN-2 (compound f9) (5-50 μM; 24 hours) shows obvious neuroprotection on H₂O₂-induced PC12 cells at 20 μM^[1].
BuChE-IN-2 (100 μM; 48 hours) can inhibit Aβ aggregation^[1].
BuChE-IN-2 (0.1-20 μM; 24 hours) has the obviously inhibitory effect on the secretion of inflammatory factors and IL-1β (IC₅₀=1.61 μM) and TNF-α (IC₅₀=4.15 μM) in BV2 cells^[1].
BuChE-IN-2 (1-10 μM; 1 hour) can significantly reduce the expression of COX-2 and iNOS in a concentration-dependent manner^[1].
BuChE-IN-2 (1-50 μM; 6 hours) has a significant inhibitory effect on ROS accumulation at 20 μM^[1].
BuChE-IN-2 (10-1000 μM; 2 hours) decreases the DPPH concentration dramatically from 86.09% to 34.62% when the concentration of BuChE-IN-2 increases from 10 μM to 1000 μM^[1].
BuChE-IN-2 (75 μM; 2 hours; MDCKII-MDR1 cells) exhibits proper blood-brain barrier permeability^[1].

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

Cell Cytotoxicity Assay

Cell Line:

PC12 cells^[1]
Concentration:

5, 20, 25, 50 μM
Incubation Time:

24 hour
Result:

Showed obvious neuroprotection on H₂O₂-induced PC12 cells at 20 μM.

Western Blot Analysis

Cell Line:

BV2 cells^[1]
Concentration:

1, 3, and 10 μM
Incubation Time:

1 hour
Result:

Significantly reduced the expression of COX-2 and iNOS in a concentration-dependent manner.

In Vivo

BuChE-IN-2 (40.96-100 mg/kg; i.g., single) shows LD₅₀ of 75.372 mg/kg in mice^[1].
BuChE-IN-2 (10 and 30 mg/kg; i.g., single) can remarkably improve the cognitive impairment in scopolamine-induced mouse models according to Morris water maze experiment^[1].

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

Animal Model:

Male C57BL mice (8-week-old, 18-23 g)^[1]
Dosage:

100, 80, 64, 51.2, 40.96 mg/kg
Administration:

i.g.; single
Result:

The median Lethal Dose (LD₅₀) of BuChE-IN-2 was 75.372 (62.383-101.673) mg/kg (95% confidence limit).

Animal Model:

Male C57BL mice (8-week-old, 18-23 g)^[1]
Dosage:

30 mg/kg, 10 mg/kg
Administration:

i.g., single
Result:

BuChE-IN-2 could remarkably improve the cognitive impairment in scopolamine-induced mouse models according to Morris water maze experiment.

Chemical Information

CAS. Nr. 2745118-93-6
Molecular Weight 564.49
Formel C₂₈H₂₀F₄N₆O₃
SMILES

O=C(NC1=CC=C(C2=NC(C3=CC(NC4=CC=C(OC(F)(F)F)C=C4)=NC=C3)=NO2)C=C1)CNC5=CC=C(F)C=C5
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

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Liu T, et al. Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. Eur J Med Chem. 2022;227:113973. [Content Brief]

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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