生物活性
TVP1022, the S-isomer of rasagiline, an anti-Parkinson drug, appears to have the same neuroprotective activity as the R-isomer, but is 1000-fold less active as an MAO-B inhibitor. TVP1022, a neuroprotective and cytoprotective molecule, is also cardioprotective in rat models. Its activity is believed to involve stabilization of mitochondrial membrane potential, induction of Bcl-2 and activation of the PKC signalling pathway, enhancing the phosphorylation of protein kinase C and glycogen synthase kinase-3β.
化学数据
| 分子量 | 171.24 |
| 分子式 | C12H13N |
| CAS号 | 185517-74-2 |
| 纯度 | >98% |
| 溶解性(25°C) | DMSO: ≥15 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 |
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 | 5.8398 mL | 29.1988 mL | 58.3976 mL |
| 5 mM | 1.168 mL | 5.8398 mL | 11.6795 mL |
| 10 mM | 0.584 mL | 2.9199 mL | 5.8398 mL |