生物活性
Aminooxyacetic acid hemihydrochloride 是苹果酸-天冬氨酸穿梭 (MAS) 抑制剂, 也能抑制 GABA 降解酶 GABA-T。
Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T. AOA hemihydrochloride dose-dependently decreases the survival of C6 glioma cells. Aminooxyacetic acid hemihydrochloride treatment produces a significant increase in the percentage of the cells arrested in the stage of G0/G1, as well as a significant decrease in the percentage of the cells at S phase and G2/M phase.
The accumulation of GABA in cerebellum and whole brain is initially very rapid, being significantly increased already 5 min after the injection of Aminooxyacetic acid hemihydrochloride (AOAA). The rapid initial accumulation becomes gradually slower and maximal levels (400 to 600 % of the control levels) are reached 2 to 6 h after Aminooxyacetic acid hemihydrochloride. Still 24 h after Aminooxyacetic acid hemihydrochloride the GABA levels are elevated by about 250%.
化学数据
分子量 | 109.3 |
分子式 | NH2OCH2COOH · 0.5HCl |
CAS号 | 2921-14-4 |
纯度 | >98% |
溶解性(25°C) | DMSO: 40 mg/mL |
储存和运输条件 | 4°C, protect from light, dry, sealed 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 | 9.1491 mL | 45.7457 mL | 91.4913 mL |
5 mM | 1.8298 mL | 9.1491 mL | 18.2983 mL |
10 mM | 0.9149 mL | 4.5746 mL | 9.1491 mL |