产品
编 号：F754953
分子式：C32H35ClN6O3
分子量：587.11
分子式：C32H35ClN6O3
分子量：587.11
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CAS No: 2720624-42-8
产品详情
生物活性：
AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease.
体内研究：
AChE/BChE-IN-1 (2 mg/kg; i.p. 3 times per week for 4 weeks) rescues learning and memory impairments, delays the Alzheimer-like pathology progression, improves basal synaptic efficacy, and significantly reduces hippocampal oxidative stress and neuroinflammation in 10 month-old APP/PS1 mice.Animal Model:AβPPswe/PS-1 double transgenic male mice (10 months)
Dosage:2 mg/kg
Administration:I.p. 3 times per week for 4 weeks
Result:Signi?cantly enhanced learning and memory.Reduced Aβ42/Aβ40 ratio in the hippocampus.Increased the strength of synaptic transmission, without a?ecting long-term potentiation (LTP).Decreased the levels of oxidative stress and neuroin?ammation markers in the hippocampus.
体外研究：
AChE/BChE-IN-1 (compound 5i) is notactive against hBACE-1 at the tested concentration (1 μM).AChE/BChE-IN-1 scavenges the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical, with an IC50 of 92.0 μM.
AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease.
体内研究：
AChE/BChE-IN-1 (2 mg/kg; i.p. 3 times per week for 4 weeks) rescues learning and memory impairments, delays the Alzheimer-like pathology progression, improves basal synaptic efficacy, and significantly reduces hippocampal oxidative stress and neuroinflammation in 10 month-old APP/PS1 mice.Animal Model:AβPPswe/PS-1 double transgenic male mice (10 months)
Dosage:2 mg/kg
Administration:I.p. 3 times per week for 4 weeks
Result:Signi?cantly enhanced learning and memory.Reduced Aβ42/Aβ40 ratio in the hippocampus.Increased the strength of synaptic transmission, without a?ecting long-term potentiation (LTP).Decreased the levels of oxidative stress and neuroin?ammation markers in the hippocampus.
体外研究：
AChE/BChE-IN-1 (compound 5i) is notactive against hBACE-1 at the tested concentration (1 μM).AChE/BChE-IN-1 scavenges the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical, with an IC50 of 92.0 μM.
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