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生物活性
U0126 was screened out as an anti-inflammatory agent that inhibited AP-1 transcription with IC50 value of 1關M and had no interactions with GREs. U0126 binds MEK1/2 in a unique site. This inhibition of MEK1/2 is noncompetitive with ERK and ATP. U0126 showed no effects on other MAPKKs. In HT22 cells, U0126 treatment significantly inhibited the cell injury caused by oxidative glutamate toxicity and remarkably blocked the phosphorylation of ERK1/2. Besides that, U0126 exerted no neuroprotection against other stimuli such as TNF慣 and actinomycin D. U0126 treatment also protected the primary cultured cortical neurons from oxidative glutamate toxicity and hypoxia/reoxygenation.
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体外研究
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体内研究
2% Cremophor EL, 2% N,N-dimethylacetamide
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激酶实验
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细胞实验
~50 μM
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动物实验
~400 μg/kg 静脉注射
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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 |
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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] Duncia JV, et al. Bioorg Med Chem Lett. 1998, 8(20), 2839-2844.
分子式
C20H22N6OS2 |
分子量
426.56 |
CAS号
1173097-76-1 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
|
DMSO
80 mg/mL |
Water
<1 mg/mL |
Ethanol
<1 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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