| 中文名称 | L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE |
| 英文名称 | CA-074 |
| CAS号 | 134448-10-5 |
| 分子式 | C18H29N3O6 |
| 分子量 | 383.44 |
| EINECS号 | 200-258-5 |
| 沸点 | 728.9±60.0 °C(Predicted) |
| 密度 | 1.267±0.06 g/cm3(Predicted) |
| 溶解度 | 溶于甲醇，浓度为 1mg/ml。也溶于DMSO或乙醇。 |
| 形态 | 固体 |
| 酸度系数(pKa) | 3.43±0.20(Predicted) |
| 颜色 | 白色至黄色 |
| WGK Germany | 3 |
Ki: 2 to 5 nM (Cathepsin B)
CA-074 is a synthetic analogue of E-64, a natural peptidyl epoxide that irreversibly inhibits most known lysosomal cysteine proteinases, and is developed by means of rational drug design, exploiting the dipeptidylcarboxypeptidase activity of cathepsin B. CA-074 can be used to selectively inhibit cathepsin B within living cells, as long as the experimental conditions permit significant fluid-phase endocytosis of the drug. CA-074 inhibits cathepsin B with a K i of 2 to 5 nM, whereas the initial K i s for cathepsin H and L are about 40-200 μM. CA-074 exhibits 10000-30000 times greater inhibitory effects on purified rat cathepsin B than on cathepsin H and L.
Intraperitoneally injection of compound CA-074 into rats potently and selectively inhibits cathepsin B activity. Intravenously administration of CA-074 immediately after the ischaemic insult saves 67% of CA1 neurons from delayed neuronal death on day 5 in eight monkeys undergoing 20 min brain ischaemia: the extent of inhibition is excellent in three of eight and good in five of eight monkeys.