中文名 | CA-074 |
英文名 | L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE |
别名 | CATHEPSIN B抑制剂(CA-074) (L-3-反式-(丙基氨基甲酰基)环氧乙烷-2-羰基)-L-异亮氨酰-L-脯氨酸 (S)-1-((2S,3S)-3-甲基-2-((2S,3S)-3-(丙基氨基甲酰基)环氧乙烷-2-甲酰胺基)戊酰基)吡咯烷-2-羧酸 |
英文别名 | CA-074 INHIBITOR FOR CATHEPSIN B CATHEPSIN B INHIBITOR III L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH L-trans-Epoxysuccinyl(propylamide)-Ile-Pro L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE CA-074(L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE) N-(L-3-TRANS-PROPYLCARBAMOYL-OXIRANE-2-CARBONYL)-ILE-PRO-OH (L-3-TRANS-(PROPYLCARBAMYL)OXIRANE-2-CARBONYL)-L-ISOLEUCYL-L-PROLINE [L-3-TRANS-(PROPYLCARBAMOYL)OXIRANE-2-CARBONYL]-L-ISOLEUCYL-L-PROLINE N-(L-3-trans-PropylcarbaMoyl-oxirane-2-carbonyl)-Ile-Pro-OH, CA-074, L-trans-Epoxysuccinyl(propylaMide)-Ile-Pro-OH |
CAS | 134448-10-5 |
EINECS | 200-258-5 |
化学式 | C18H29N3O6 |
分子量 | 383.44 |
密度 | 1.267±0.06 g/cm3(Predicted) |
沸点 | 728.9±60.0 °C(Predicted) |
溶解度 | 1mg/ml溶于甲醇。也可溶于DMSO或乙醇。 |
酸度系数 | 3.43±0.20(Predicted) |
存储条件 | -20°C |
外观 | 固体 |
体外研究 | 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. |
体内研究 | 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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.608 ml | 13.04 ml | 26.08 ml |
5 mM | 0.522 ml | 2.608 ml | 5.216 ml |
10 mM | 0.261 ml | 1.304 ml | 2.608 ml |
5 mM | 0.052 ml | 0.261 ml | 0.522 ml |
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