生物活性
Balicatib是一种有效的、选择性的组织蛋白酶K抑制剂;在基于细胞的酶占用试验中比对组织蛋白酶B, L和S的作用强10-100倍。
化学数据
分子量 | 411.54 |
分子式 | C23H33N5O2 |
CAS号 | 354813-19-7 |
纯度 | >98% |
溶解性(25°C) | DMSO 10 mM |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
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细胞系 | Hep G2 and SMMC-7721 cells |
方法 | Cell viability assay. The 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) assay was used to measure drug sensitivity. Briefly, Hep G2 and SMMC-7721 cells were seeded into 96-well plates (Corning, USA) at a density of 5 × 103cells per well, incubated overnight, and then treated with various concentrations (0, 10, 20, 40, and 80 μmol/L) of baicalin for 24, 48, and 72 h. Thereafter, 20 μl of MTT solution (5 mg/mL; Sigma-Aldrich, St. Louis, MO, USA) was added to each well, and the plates were incubated at 37°C for 4 h. The formed formazan crystals were dissolved in 100 μl of DMSO after removal of the supernatant. The optical density (OD) was recorded at 490 nm using a microplate reader (Bio-Tek, Winooski, VT, USA). The percentage of cell viability was calculated as: (OD of baicalin-treated group/OD of control group) × 100%. |
浓度 | 0, 10, 20, 40, and 80 μmol/L |
处理时间 | 24, 48 and 72 h |
动物实验 |
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动物模型 | Six-week old athymic nude mice bearing Hep G2 cells xenograft model |
配制 | 10% DMSO and 90% propylene glycol |
剂量 | 50 mg/kg and 100 mg/kg daily for 3 weeks |
给药处理 | i.p. |
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 |
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1 mM | 2.4299 mL | 12.1495 mL | 24.299 mL |
5 mM | 0.486 mL | 2.4299 mL | 4.8598 mL |
10 mM | 0.243 mL | 1.2149 mL | 2.4299 mL |