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生物活性
(-)-Blebbistatin is a small molecule inhibitor and preferentially binds to the myosin-ADP-Pi complex to slow down phosphate release. The inhibitor completely eliminate contraction of activity of actin-activated Mg-ATPase and motility of myosins II for several species in vitro (IC50 = 0.5-5.0 μM), but it has poor effects on smooth muscle myosin II (IC50 =80 μM) and myosins I,V, and X. Furthermore, blebbistatin can potently inhibit mammalian arterial smooth muscle (IC50=5 μM). The property that blebbistatin blocks myosin II in an actin-detached state and prevents rigid actomyosin cross-linking is a great advantage in vivo applications.
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体外研究
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体内研究
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激酶实验
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细胞实验
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动物实验
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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] Straight AF, et al. Science, 2003, 299(5613), 1743-1747.
[2] Limouze, J., et al. 2004. J. Mus. Res. Cell Motil. 25: 337-41.
分子式
C18H16N2O2 |
分子量
292.33 |
CAS号
856925-71-8 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
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DMSO
100 mM |
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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