产品
编 号：F755202
分子式：C28H20F4N6O3
分子量：564.49
分子式：C28H20F4N6O3
分子量：564.49
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CAS No: 2745118-93-6
产品详情
生物活性：
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.
体内研究：
BuChE-IN-2 (40.96-100 mg/kg; i.g., single) shows LD50 of 75.372 mg/kg in mice.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.Animal Model:Male C57BL mice (8-week-old, 18-23 g)
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)
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.
体外研究：
BuChE-IN-2 (compound f9) (5-50 μM; 24 hours) shows obvious neuroprotection on H2O2-induced PC12 cells at 20 μM.BuChE-IN-2 (100 μM; 48 hours) can inhibit Aβ aggregation.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.BuChE-IN-2 (1-10 μM; 1 hour) can significantly reduce the expression of COX-2 and iNOS in a concentration-dependent manner.BuChE-IN-2 (1-50 μM; 6 hours) has a significant inhibitory effect on ROS accumulation at 20 μM.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.BuChE-IN-2 (75 μM; 2 hours; MDCKII-MDR1 cells) exhibits proper blood-brain barrier permeability.
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.
体内研究：
BuChE-IN-2 (40.96-100 mg/kg; i.g., single) shows LD50 of 75.372 mg/kg in mice.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.Animal Model:Male C57BL mice (8-week-old, 18-23 g)
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)
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.
体外研究：
BuChE-IN-2 (compound f9) (5-50 μM; 24 hours) shows obvious neuroprotection on H2O2-induced PC12 cells at 20 μM.BuChE-IN-2 (100 μM; 48 hours) can inhibit Aβ aggregation.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.BuChE-IN-2 (1-10 μM; 1 hour) can significantly reduce the expression of COX-2 and iNOS in a concentration-dependent manner.BuChE-IN-2 (1-50 μM; 6 hours) has a significant inhibitory effect on ROS accumulation at 20 μM.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.BuChE-IN-2 (75 μM; 2 hours; MDCKII-MDR1 cells) exhibits proper blood-brain barrier permeability.
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