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编 号：F756525
分子式：C26H25N7O2
分子量：467.52
分子式：C26H25N7O2
分子量：467.52
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CAS No: 2873465-25-7
产品详情
生物活性：
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease.
体内研究：
JNK3 inhibitor-3 (30 and 60 mg/kg; oral administration, once daily for 2 or 2.2 month) improves the memory of 3xTg mouse dementia model.1.19Pharmacokinetic Properties of JNK3 inhibitor-3 in Rats. RatsIV1 mg/kgRatsPO 3 mg/kg
AUC (hr?ng/mL)1085.242806.77
Cmax (ng/mL)1238.85
Tmax (hr)0.67
T1/2 (hr)0.361.14
BA (%)86.21
Animal Model:Homozygous 3xTg and APPswe/PS1dE9 double-transgenic mice model of Alzheimer’s disease
Dosage:30 and 60 mg/kg
Administration:Oral administration; once daily for 2 or 2.2 month
Result:Induced no abnormal symptoms or weight changes, significantly enhanced the spontaneous alteration in APP/PS1 and doses of 30 and 60 mg/kg than that of vehicle group in Y-maze test and showed a significant difference compared to the 3xTg vehicle control in the passive avoidance test.
体外研究：
JNK3 inhibitor-3 (0-10 μM) shows inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively.JNK3 inhibitor-3 (20 μM; 24 and 48 h) demonstrates neuroprotective effects in vitro.
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease.
体内研究：
JNK3 inhibitor-3 (30 and 60 mg/kg; oral administration, once daily for 2 or 2.2 month) improves the memory of 3xTg mouse dementia model.1.19Pharmacokinetic Properties of JNK3 inhibitor-3 in Rats. RatsIV1 mg/kgRatsPO 3 mg/kg
AUC (hr?ng/mL)1085.242806.77
Cmax (ng/mL)1238.85
Tmax (hr)0.67
T1/2 (hr)0.361.14
BA (%)86.21
Animal Model:Homozygous 3xTg and APPswe/PS1dE9 double-transgenic mice model of Alzheimer’s disease
Dosage:30 and 60 mg/kg
Administration:Oral administration; once daily for 2 or 2.2 month
Result:Induced no abnormal symptoms or weight changes, significantly enhanced the spontaneous alteration in APP/PS1 and doses of 30 and 60 mg/kg than that of vehicle group in Y-maze test and showed a significant difference compared to the 3xTg vehicle control in the passive avoidance test.
体外研究：
JNK3 inhibitor-3 (0-10 μM) shows inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively.JNK3 inhibitor-3 (20 μM; 24 and 48 h) demonstrates neuroprotective effects in vitro.
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