产品
编 号：F128237
分子式：C18H29N3O6
分子量：383.44
分子式：C18H29N3O6
分子量：383.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 134448-10-5
产品详情
生物活性：
CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
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.
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 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.
CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
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.
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 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.
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