PeptideDB

BuChE-IN-2

CAS: 2745118-93-6 F: C28H20F4N6O3 W: 564.49

BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC50s of 1.28 μM and 0.67 μM for BuChE and NO). Bu
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This product is for research use only, not for human use. We do not sell to patients.

Bioactivity 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[1].
Target IC50: 1.28 μM (BuChE), 0.67 μM (NO)
Invitro 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]. Cell Cytotoxicity Assay Cell Line:
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]. Animal Model:
Name BuChE-IN-2
CAS 2745118-93-6
Formula C28H20F4N6O3
Molar Mass 564.49
Transport Room temperature in continental US; may vary elsewhere.
Storage

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

Reference [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.