产品
编 号：F762943
分子式：C22H30N2O4S2
分子量：450.61
分子式：C22H30N2O4S2
分子量：450.61
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CAS No: 3033542-32-1
产品详情
生物活性：
AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD).
体内研究：
AChE-IN-24 (compound 4c2) (oral; 0, 625, 1250, and 2500 mg/kg) is well tolerated and no toxicity in KM mice.AChE-IN-24 (7.5 mg/kg, 15 mg/kg and 30mg/kg; once) ameliorates cognitive deficit induced by Scopolamine, suggesting a practicable therapeutic effect on AD.Animal Model:KM mice
Dosage:0, 625, 1250, and 2500 mg/kg
Administration:oral; 0, 625, 1250, and 2500 mg/kg
Result:Not discovered abnormal behavior and acute toxicity were monitored for the first 4 hafter administration, no acute neurological toxicities inclusive of tremor, convulsion,and death and no obvious signs of poisoning in the heart, liver, lungs, kidneys,and brain.
Animal Model:The cognitive deficit mice model
Dosage:7.5 mg/kg, 15 mg/kg and 30mg/kg
Administration:7.5 mg/kg, 15 mg/kg and 30mg/kg; once
Result:Reversed the step-down latency and number of errors in a concentration-dependent manner.
体外研究：
AChE-IN-24 (compound 4c2) has good hAChE inhibitory activity with IC50values of 0.053 μM but owns little inhibition to hBuChE.AChE-IN-2 has inhibitory activity for electric eel acetylcholinesterase (eeAChE) and equine serum butyrylcholinesterase (eqBuChE) with IC50values of 0.088 μM and 7.5μM, respectively.AChE-IN-24 (0-0.2 μM) can cross the BBB comfortably by means of passive diffusion.AChE-IN-2 (0-40 μM) triggers the translocation of Nrf2 to the nucleus, thereby expediting the binding of Nrf2 to the ARE for the transcription process.AChE-IN-2 (7 μM) significantly induces the expression of antioxidant-related enzymes by activating Nrf2 in BV-2 cells.AChE-IN-2 (1, 3, 7 μM) protects cells from H2O2-induced damage and inhibits ROS accumulation.AChE-IN-2 (1, 3, 7 μM) attenuates inflammatory responses.
AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD).
体内研究：
AChE-IN-24 (compound 4c2) (oral; 0, 625, 1250, and 2500 mg/kg) is well tolerated and no toxicity in KM mice.AChE-IN-24 (7.5 mg/kg, 15 mg/kg and 30mg/kg; once) ameliorates cognitive deficit induced by Scopolamine, suggesting a practicable therapeutic effect on AD.Animal Model:KM mice
Dosage:0, 625, 1250, and 2500 mg/kg
Administration:oral; 0, 625, 1250, and 2500 mg/kg
Result:Not discovered abnormal behavior and acute toxicity were monitored for the first 4 hafter administration, no acute neurological toxicities inclusive of tremor, convulsion,and death and no obvious signs of poisoning in the heart, liver, lungs, kidneys,and brain.
Animal Model:The cognitive deficit mice model
Dosage:7.5 mg/kg, 15 mg/kg and 30mg/kg
Administration:7.5 mg/kg, 15 mg/kg and 30mg/kg; once
Result:Reversed the step-down latency and number of errors in a concentration-dependent manner.
体外研究：
AChE-IN-24 (compound 4c2) has good hAChE inhibitory activity with IC50values of 0.053 μM but owns little inhibition to hBuChE.AChE-IN-2 has inhibitory activity for electric eel acetylcholinesterase (eeAChE) and equine serum butyrylcholinesterase (eqBuChE) with IC50values of 0.088 μM and 7.5μM, respectively.AChE-IN-24 (0-0.2 μM) can cross the BBB comfortably by means of passive diffusion.AChE-IN-2 (0-40 μM) triggers the translocation of Nrf2 to the nucleus, thereby expediting the binding of Nrf2 to the ARE for the transcription process.AChE-IN-2 (7 μM) significantly induces the expression of antioxidant-related enzymes by activating Nrf2 in BV-2 cells.AChE-IN-2 (1, 3, 7 μM) protects cells from H2O2-induced damage and inhibits ROS accumulation.AChE-IN-2 (1, 3, 7 μM) attenuates inflammatory responses.
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