化合物CA 074 T21509

Product Introduction
Bioactivity


英文名: CA 074

描述: CA 074 是一种高效的组织蛋白酶B (cathepsin B) 抑制剂， Ki 值为2 to 5 nM。CA 074 抑制灵长类动物缺血性海马神经元死亡，可减轻 SJL/J 小鼠诱导的实验性自身免疫性脑脊髓炎的视网膜病变和视神经炎。

体外活性: CA-074, a synthetic analogue of E-64 developed through rational drug design, is an irreversible inhibitor of most lysosomal cysteine proteinases. It exploits the dipeptidylcarboxypeptidase activity of cathepsin B. With a Ki of 2 to 5 nM, CA-074 selectively inhibits cathepsin B within living cells, provided that experimental conditions allow significant fluid-phase endocytosis of the drug[2]. Notably, CA-074 demonstrates significantly greater inhibitory effects on purified rat cathepsin B (10000-30000 times) compared to cathepsin H and L, for which the initial Kis are about 40-200 μM[3].

体内活性: The intraperitoneal injection of compound CA-074 into rats effectively and selectively inhibits cathepsin B activity[1]. Following intravenous administration of CA-074 immediately after the ischemic insult, it preserves 67% of CA1 neurons from delayed neuronal death on day 5 in eight monkeys undergoing 20 minutes of brain ischemia. The extent of inhibition is excellent in three of eight monkeys and good in five of eight monkeys[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (260.80 mM)


关键字: CA-074 | CA074 | CA 074

相关产品: Aurantiamide acetate | 3-Epiursolic acid | Z-FA-FMK | MIV-247 | N-Ethylmaleimide | Dazcapistat | K777 | Tacalcitol monohydrate | LV-320 | Cathepsin X-IN-1

相关库: Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途