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 |
|---|
| 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 |
|---|
| 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 |
|---|
| 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 |
