生物活性
LDN-214117是ALK2高效选择性抑制剂，IC50值为22nM，也能抑制BMP6，IC50值为100nM，对ALK5抑制力弱100倍。LDN-214117 may be useful as highly selective probes of BMP-mediated cellular physiology that may provide a useful complement to the dorsomorphin class of compounds. Furthermore, this class of BMP inhibitors offers a structurally distinct template for the development of therapeutics for the treatment of BMP signaling-mediated diseases such as FOP.
化学数据
| 分子量 | 419.52 |
| 分子式 | C25H29N3O3 |
| CAS号 | 1627503-67-6 |
| 纯度 | 99.91% |
| 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 | HepG2 hepatocarcinoma cells |
| 方法 | Seeding cells at 25000 cells per well in 96-well plates and incubatng for 2 h at 37℃ and 5% CO2. Diluting compounds of LDN-214117 or DMSO are in DMEM and adding at final compound concentrations of 1, 10, and 100 μM.Incubating cells for 4 and 24 h, after which the media is discarded. Cells are lysed by adding 30 μL of passive lysis buffer and shaken at RT for 15 min. Cell viability is determined by quantifying the ATP present in each well by adding 10 μL of Cell Titer Glo per well and measuring the light output by Spectramax L luminometer. Data is normalized to 100% viability for cells receiving only DMSO. |
| 浓度 | 100 μM |
| 处理时间 | 24 h |
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 | 2.3837 mL | 11.9184 mL | 23.8368 mL |
| 5 mM | 0.4767 mL | 2.3837 mL | 4.7674 mL |
| 10 mM | 0.2384 mL | 1.1918 mL | 2.3837 mL |
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