L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE
| 中文名称 | L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE |
|---|---|
| 中文同义词 | (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;CATHEPSIN B抑制剂(CA-074);(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;L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH;CA-074(L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE);N-((2S,3S)-3-(丙基氨基甲酰基)环氧乙烷-2-羰基)-L-异亮氨酰-L-脯氨酸;化合物 T21509;L-反式-环氧丁二酰基(丙胺)-IP |
| 英文名称 | CA-074 |
| 英文同义词 | N-(L-3-TRANS-PROPYLCARBAMOYL-OXIRANE-2-CARBONYL)-ILE-PRO-OH;L-trans-Epoxysuccinyl(propylamide)-Ile-Pro;N-(L-3-trans-PropylcarbaMoyl-oxirane-2-carbonyl)-Ile-Pro-OH, CA-074, L-trans-Epoxysuccinyl(propylaMide)-Ile-Pro-OH;INHIBITOR FOR CATHEPSIN B;CATHEPSIN B INHIBITOR III;CA-074;[L-3-TRANS-(PROPYLCARBAMOYL)OXIRANE-2-CARBONYL]-L-ISOLEUCYL-L-PROLINE;(L-3-TRANS-(PROPYLCARBAMYL)OXIRANE-2-CARBONYL)-L-ISOLEUCYL-L-PROLINE |
| CAS号 | 134448-10-5 |
| 分子式 | C18H29N3O6 |
| 分子量 | 383.44 |
| EINECS号 | 200-258-5 |
| 相关类别 | 细胞生物学试剂;peptides;Pepetides;Inhibitor |
| Mol文件 | 134448-10-5.mol |
| 结构式 |  |
L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE 性质
| 沸点 | 728.9±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.267±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 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) |
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.
安全信息
| WGK Germany | 3 |
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| 提供商 | 语言 |
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英文
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-103350 | L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE CA-074 | 134448-10-5 | 1mg | 900元 |
| 2024/04/30 | HY-103350 | L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE CA-074 | 134448-10-5 | 5mg | 2700元 |