134448-10-5
134448-10-5 结构式
基本信息
(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
CA-074 >=99% (TLC)
CATHEPSIN B INHIBITOR III
INHIBITOR FOR CATHEPSIN B
L-trans-Epoxysuccinyl(propylamide)-Ile-Pro
L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE
L-TRANS-EPOXYSUCCINYL (PROPYLAMIDE)-ILE-PRO-OH
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-(PROPYLCARBOMOYL)OXIRANE-2-CARBONYL]-L-ISOLEUCYL-L-PROLINE
物理化学性质
常见问题列表
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.