YM 511 目录号M7503
化学数据
分子量分子式CAS号储存条件
354.2C16H12BrN5148869-05-03年 -20°C 粉末状
溶解性(25°C)
DMSO Water Ethanol
生物活性
YM 511 is a orally active, potent aromatase (CYP19) inhibitor (IC50values are 0.4 and 0.12 nM at rat ovary and human placenta cells respectively) that only weakly inhibits the synthesis of other steroid hormones. Reduces plasma estrogen levels into ranges induced by ovariectomy and inhibits testosterone-induced breast cancer cell growth in vitro(IC50= 0.13 nM).
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
重量 (kg)体表面积 (m2)Km系数
0.020.0073
动物 B的Km系数动物 A的Km系数
大鼠0.150.0256
兔1.80.1512
豚鼠0.40.058
仓鼠0.080.025
狗100.520
动物 A (mg/kg) = 动物 B (mg/kg) ×
例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
参考文献
The mapping of the Lyn kinase binding site of the common β subunit of IL-3/granulocyte-macrophage colony-stimulating factor/IL-5 receptor.Adachi, et al. J Immunol. 1999;162: 1496. PMID: 9973406.