生物活性
(±)-Blebbistatin (BLEB) is a small cell permeable selective myosin II inhibitor which potently relaxed normal detrusor smooth muscle. Rabbit arterial SM was potently inhibited by BLEB (IC50 ~5 μM) although this tissue does not express significant amounts of NMM II. Blebbistatin (BLEB) inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly. Blebbistatin (BLEB) rapidly and reversibly blocks cell blebbing, and disrupts directed cell migration and cytokinesis in vertebrate cells.
Due to the known light sensitivity of Blebbistatin (BLEB), it was always kept in the dark in the refrigerator until just prior to usage.
化学数据
分子量 | 292.34 |
分子式 | C18H16N2O2 |
CAS号 | 674289-55-5 |
纯度 | >99% |
溶解性(25°C) | DMSO ≥ 15 mg/mL |
储存和运输条件 | -20°C, protect from light, dry, sealed 常温运输及临时存放 |
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)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
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,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.4207 mL | 17.1034 mL | 34.2067 mL |
5 mM | 0.6841 mL | 3.4207 mL | 6.8413 mL |
10 mM | 0.3421 mL | 1.7103 mL | 3.4207 mL |