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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
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MedChemExpress LLC
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2278.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥900.0 |
| 规格： | 5 mg | 产品价格： | ￥2700.0 |
| 规格： | 10 mg | 产品价格： | ￥3780.0 |
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CA-074
CAS No. : 134448-10-5
MCE 国际站：CA-074
产品活性：CA-074是组织蛋白酶B (cathepsin B) 的有效抑制剂， Ki 值为2 to 5 nM。
研究领域：Metabolic Enzyme/Protease
作用靶点：Cathepsin
In Vitro: 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 Ki of 2 to 5 nM, whereas the initial Kis 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.
In Vivo: 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.
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