Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 745 | 现货 | ||
2 mg | ¥ 1,190 | 现货 | ||
5 mg | ¥ 2,220 | 现货 | ||
10 mg | ¥ 3,280 | 现货 | ||
25 mg | ¥ 5,380 | 现货 | ||
50 mg | ¥ 7,590 | 现货 | ||
100 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,880 | 现货 |
产品描述 | CA 074 is a potent inhibitor of cathepsin B with a Ki value of 2 to 5 nM.CA 074 inhibits ischemic hippocampal neuronal death in primates and attenuates retinopathy and optic neuritis in experimental autoimmune encephalomyelitis induced by SJL/J mice. |
靶点活性 | Cathepsin B:2-5 nM(Ki) |
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]. |
分子量 | 383.44 |
分子式 | C18H29N3O6 |
CAS No. | 134448-10-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (260.80 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.608 mL | 13.0398 mL | 26.0797 mL | 65.1992 mL |
5 mM | 0.5216 mL | 2.608 mL | 5.2159 mL | 13.0398 mL | |
10 mM | 0.2608 mL | 1.304 mL | 2.608 mL | 6.5199 mL | |
20 mM | 0.1304 mL | 0.652 mL | 1.304 mL | 3.26 mL | |
50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.304 mL | |
100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.652 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CA 074 134448-10-5 Proteases/Proteasome Cysteine Protease CA-074 CA074 Inhibitor inhibitor inhibit