生物活性
TA-01是一种有效的CK1和p38 MAPK抑制剂，对CK1ε，CK1δ和p38 MAPK的IC50值分别为6.4 nM，6.8 nM和6.7 nM。当在5μM下施用时，TA-01抑制剂抑制心脏发育。TA-01显示所有测试的中胚层标记物和心脏前标志物Isl-1的表达降低。
化学数据
| 分子量 | 351.32 |
| 分子式 | C20H12F3N3 |
| CAS号 | 1784751-18-3 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO ≥ 30 mg/mL |
| 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 | Human pluripotent stemcell lines HES-3 and H7 |
| 方法 | Human pluripotent stemcell lines HES-3 and H7 were seeded at 2.5 × 106cells/12-ULA well in BSFS medium with cell line optimized concentrations of CHIR99021 for 24 h (Supplemental Fig. S7). Thereafter the 2,4,5-trisubstituted azoles or IWP-2 or IWR-1 were added at a concentration of 5 μM (2.5 μM for IWR-1) either from 1-8 days or from 4-8 days. Dissociated EBs showed an average of 50–60% NKX2-5+cells on day 11 when either 2,4,5-trisubstituted azoles, IWP-2 and IWR-1 were applied from 4-8 days i.e. at the post mesoderm stage. In comparison to premesoderm treatment only HES-3 showed high cardiomyocyte expansion fold with SB203580 (days 1-8) (Fig. 3A). To confirm that 2,4,5-trisubstituted azoles had no negative impact on cell viability, we analyzed the cell growth kinetics. EBs treated with IWP-2 and IWR-1 generated significantly fewer cells compared to 2,4,5-trisubstituted azoles in both cell lines (Fig. 3A). Metabolismrates of EBs measured with MTT showed an increase with TA-01 but not with IWR-1 and IWP-2 during the compound induction period. |
| 浓度 | 5 μM |
| 处理时间 | - |
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 | 2.8464 mL | 14.232 mL | 28.4641 mL |
| 5 mM | 0.5693 mL | 2.8464 mL | 5.6928 mL |
| 10 mM | 0.2846 mL | 1.4232 mL | 2.8464 mL |
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