CA 074

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CA-074是组织蛋白酶B (cathepsin B) 的有效抑制剂， Ki 值为2 to 5 nM。

CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.

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.

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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Proteasome/Ubiquitin

Cysteine Protease

Cysteine Protease

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134448-10-5

383.44

C18H29N3O6

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (326.00 mM; 超声助溶 )

[H][C@](NC(=O)[C@H]1O[C@@H]1C(=O)NCCC)([C@@H](C)CC)C(=O)N1CCC[C@H]1C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years