1. Neuronal Signaling Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  2. Cholinesterase (ChE) Amyloid-β Interleukin Related Reactive Oxygen Species (ROS) NOD-like Receptor (NLR)
  3. BuChE-IN-20

BuChE-IN-20 is a selective butyrylcholinesterase (hBuChE) inhibitor (IC50 = 0.13 μM) with BBB permeability. BuChE-IN-20 is a L-Tryptophan derivative. BuChE-IN-20 possesses neuroprotective properties by inhibiting the production of nitric oxide (NO) and lowering the levels of ROS. BuChE-IN-20 is proficient in inhibiting the self-aggregation of amyloid-beta (Aβ) peptides. BuChE-IN-20 can be used in research for Alzheimer’s disease.

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

BuChE-IN-20 Chemical Structure

BuChE-IN-20 Chemical Structure

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Description

BuChE-IN-20 is a selective butyrylcholinesterase (hBuChE) inhibitor (IC50 = 0.13 μM) with BBB permeability. BuChE-IN-20 is a L-Tryptophan derivative. BuChE-IN-20 possesses neuroprotective properties by inhibiting the production of nitric oxide (NO) and lowering the levels of ROS. BuChE-IN-20 is proficient in inhibiting the self-aggregation of amyloid-beta (Aβ) peptides. BuChE-IN-20 can be used in research for Alzheimer’s disease[1].

IC50 & Target[1]

BChE

0.13 nM (IC50)

In Vitro

BuChE-IN-20 (Compound 4d-13) (5 μM, 10 min) shows selectivity for BuChE through enzymatic activity assays of hAChE and hBuChE[1].
BuChE-IN-20 (20 μM, 48 h) prevents the aggregation and deposition of Aβ1-42, thereby exerting neuroprotective effects by inhibiting the formation of toxic amyloid plaques, and mitigate the neurotoxicity induced by Aβ1-42 through ROS generation[1].
BuChE-IN-20 (1 mM, 30 min) exerts scavenging capacities for hydroxyl radicals 775 times that of vitamin C[1].
BuChE-IN-20 (5-10 μM, 4 h pretreatment and 8 h cotreatment with LPS) decreases intracellular reactive oxygen species (ROS) concentration-dependently in LPS (1.5 μg/mL) (HY-D1056)-induced RAW264.7 cells[1].
BuChE-IN-20 (6.25-12.5 μM, 4 h pretreatment and 24 h cotreatment with LPS) demonstrates potent inhibitory activity on LPS (2 μg/mL)-induced NO production in RAW264.7 cells[1].
BuChE-IN-20 (1-100 μM, 24 h) exerts inhibitory effects and free radical scavenging at sub-micromolar concentrations in mouse BV-2 cell line, with a safety margin of nearly 150-fold regarding cytotoxicity[1].
BuChE-IN-20 (1-10 μM, 24 h pretreatment and 24 h cotreatment with LPS) decreases IL-1β levels in LPS (100 ng/mL)-induced BV-2 cells[1].
BuChE-IN-20 (1-20 μM, 6 h pretreatment and 24 h cotreatment with NMDA/Sodium L-Glutamate) mitigates the cytotoxic effects dose-dependently in NMDA (20 mM)/Sodium L-Glutamate(Glu) (HY-N0455B)-induced SH-SY5Y cell injury model[1].

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

RT-PCR[1]

Cell Line: LPS (100 ng/mL)-induced BV-2 cells
Concentration: 1, 5, 10 μM
Incubation Time: 24 h pretreatment and 24 h cotreatment with LPS
Result: Exhibited a dose-dependent reduction in IL-1β expression, while having a lesser effect on IL-6 and TNF-α.
Inhibited the production, release, and NLRP3-mediated maturation of IL-1β directly.
Inhibited the NF-κB and MAPK signaling pathways to reduce IL-1β indirectly.
In Vivo

BuChE-IN-20 (Compound 4d-13) (10-100 mg/kg, p.o., one single dose) shows no toxic or abnormal symptoms with the maximum tolerated dose of 100 mg/kg in ICR mice model[1].
BuChE-IN-20 (10-40 mg/kg, p.o., one single dose) shows notable positive effect on improving learning and memory function in (-)-Scopolamine hydrobromide (HY-W010892) (3 mg/kg, i.p.)-induced ICR mice[1].

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

Animal Model: (-)-Scopolamine hydrobromide (HY-W010892) (3 mg/kg, i.p.)-induced ICR mice [1]
Dosage: 10-40 mg/kg
Administration: Oral gavage (p.o.)
Result: Recovered the impairment of hippocampus-dependent memory and spatial learning functions induced by (-)-Scopolamine hydrobromide.
Mitigated the cognitive impairment induced by (-)-Scopolamine hydrobromide at the dosage of 40 mg/kg via gavage, evidenced by a reduction in escape latency and a decrease in the traversed distance to the escape platform.
Molecular Weight

484.56

Formula

C29H29FN4O2

SMILES

OC1=C(F)C=C(CN[C@@H](CC2=CNC3=CC=CC=C32)C(N(C)CCC4=CNC5=C4C=CC=C5)=O)C=C1

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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    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-20
Cat. No.:
HY-172782
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