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抑制剂/激活剂

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凋亡与自噬

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CA 074

CA-074是一种组织蛋白酶B抑制剂，其Ki值为2-5 nM。

货号：
TK0535
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	134448-10-5
生物活性	CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
分子式	C18H29N3O6
分子量	383.44
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder, -20°C ,3 years
溶解性数据	DMSO : 125 mg/mL (326.00 mM; Need ultrasonic)
体内研究	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.
体外研究	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.
纯度及产品资料	98%

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