Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 21,500 | |||
5 mg | 在庫あり | ¥ 51,000 | |||
10 mg | 在庫あり | ¥ 80,000 | |||
25 mg | 在庫あり | ¥ 160,000 | |||
50 mg | 在庫あり | ¥ 222,000 | |||
100 mg | 在庫あり | ¥ 294,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 43,000 |
説明 | 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. |
ターゲット&IC50 | Cathepsin B:2-5 nM(Ki) |
In vitro | 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]. |
In vivo | 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.
You can also refer to dose conversion for different animals. 詳細
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CA 074 134448-10-5 Proteases/Proteasome Cysteine Protease CA-074 CA074 Inhibitor inhibitor inhibit