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CA-074

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Chemical Structure| 134448-10-5 同义名 : -
CAS号 : 134448-10-5
货号 : A976403
分子式 : C18H29N3O6
纯度 : 99%+
分子量 : 383.44
MDL号 : MFCD00797531
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(312.96 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Cathepsin B is a lysosomal cysteine protease of the papain family. It functions in intracellular protein catabolism and in certain situations may also be involved in other physiological processes, such as processing of antigens in the immune response, hormone activation and bone turnover. Cathepsin B is implicated in the pathology of chronic inflammatory diseases of airways and joints, and in cancer and pancreatitis[1]. 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[2].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[3].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[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00856661 Stroke Phase 3 Terminated(The recruitment int... 展开 >>o DIAS4 has been stopped as the result of DIAS 3 indicates that the study is unlikely to reach its primary endpoint with the current protocol) 收起 << - -
NCT02585934 Alzheimer's Disease Phase 3 Completed - -
NCT02723240 Cancer Phase 1 Recruiting June 30, 2019 United Kingdom ... 展开 >> Belfast City Hospital Not yet recruiting Belfast, United Kingdom, BT9 7AB Principal Investigator: Richard H Wilson, MD          Beatson, West of Scotland Cancer Centre Recruiting Glasgow, United Kingdom, G12 OYN Principal Investigator: Jeffry Evans, MD, FRCP          Oxford University Hospitals NHS Trust Recruiting Oxford, United Kingdom, OX3 7LE Principal Investigator: Sarah P Blagden, Phd, FRCP 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL
参考文献

[1]J S Mort , D J Buttle. Int J Biochem Cell Biol. 1997 May;29(5):715-20.

[2]Towatari T, et al. Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo. FEBS Lett. 1991 Mar 25;280(2):311-5.

[3] Montaser M, et al. CA-074, but not its methyl ester CA-074Me, is a selective inhibitor of cathepsin B within living cells. Biol Chem. 2002 Jul-Aug;383(7-8):1305-8.

[4] Yamashima T, et al. Inhibition of ischaemic hippocampal neuronal death in primates with cathepsin B inhibitor CA-074: a novel strategy for neuroprotection based on 'calpain-cathepsin hypothesis'. Eur J Neurosci. 1998 May;10(5):1723-33.