JNK3 inhibitor-3
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2873465-25-7
- 分子式: C26H25N7O2
- 分子量:467.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
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JNK3 4.1 nM (IC50) |
JNK2 44 nM (IC50) |
JNK1 147.8 nM (IC50) |
体外実験
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[1]. JNK3 inhibitor-3 (20 μM; 24 and 48 h) demonstrates neuroprotective effects in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Rat cortical neurons
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Concentration:20 μM
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Incubation Time:24 and 48 hours
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Result:Protected rat cortical neurons against 10 μM Aβ1-42 induced neurotoxicity.
体内実験
| Rats IV 1 mg/kg |
Rats PO 3 mg/kg |
|
| AUC (hr•ng/mL) | 1085.24 | 2806.77 |
| Cmax (ng/mL) | 1238.85 | |
| Tmax (hr) | 0.67 | |
| T1/2 (hr) | 0.36 | 1.14 |
| BA (%) | 86.21 | |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Homozygous 3xTg and APPswe/PS1dE9 double-transgenic mice model of Alzheimer’s disease[1]
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Dosage:30 and 60 mg/kg
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Administration:Oral administration; once daily for 2 or 2.2 month
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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.
化学情報
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CAS 番号 2873465-25-7
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分子量 467.52
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分子式 C26H25N7O2
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SMILES
N#CCC1=CN=C(N1C2=NC(N[C@H]3CCCN(C3)C(C4CC4)=O)=NC=C2)C5=CC6=C(OC=C6)C=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)