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生物活性
JSH-23 is developed to inhibit NF-κB transcriptional activity in LPS-stimulated macrophages RAW 264.7. It shows a dose-dependent inhibition. This effect is not due to its cytotoxicity. In the same condition, JSH-23 is found to significantly decrease the LPS-induced DNA binding activity of NF-κB while decrease nuclear amount of NF-κB p65. JSH-23 plays these roles without affecting IκB degradation. In addition, JSH-23 also shows inhibition effects on the expression of the pro-inflammatory transcripts and enzymes, including IL-6, IL-1β, COX-2 and TNF-α. Furthermore, JSH-23 inhibits LPS-induced apoptotic chromatin condensation.
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体外研究
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体内研究
0.5%羧甲基纤维素钠
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激酶实验
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细胞实验
~300 μM
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动物实验
~3mg/kg 口服给药
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
|
例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Shin HM, et al. FEBS Lett. 2004, 571(1-3), 50-54.
分子式
C16H20N2 |
分子量
240.34 |
CAS号
749886-87-1 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
|
DMSO
>20 mg/mL |
Water
<1 mg/mL |
Ethanol
20 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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