Leupeptin hemisulfate

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Chemical Structure| 103476-89-7 同义名 : 亮肽素 ;Acetyl-L-leucyl-L-leucyl-L-argininal; Leupeptin (hemisulfate)
CAS号 : 103476-89-7
货号 : A663950
分子式 : C40H78N12O12S
纯度 : 97%
分子量 : 951.19
MDL号 : MFCD00037012
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 85 mg/mL(89.36 mM)，配合低频超声，并水浴加热至45℃助溶
生物活性
靶点

  • Cysteine Protease
描述 Leupeptin is a reversible and competitive serine/cysteine protease inhibitor which can inhibit proteolysis plasmin, trypsin and papain but not chymotrypsin. Oral administration of leupeptins exhibited an anti-inflammatory effect on edema. It inhibited thrombokinase reaction and coagulation of blood of human and rabbit, but not in rats and dogs[1]. Leupeptin is also used as a cathepsin B inhibitor[2]. Leupeptin inhibited calpain activity with IC50 of 0.14 μM[3].
作用机制 Leupeptin is competitive with substrates. The free aldehyde group plays a role in the activities.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.05mL

0.21mL

0.11mL

5.26mL

1.05mL

0.53mL

10.51mL

2.10mL

1.05mL
参考文献

[1]Aoyagi T, Miyata S, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68.

[2]Salminen A, et al. Effects of the protease inhibitor leupeptin on proteolytic activities and regeneration of mouse skeletal muscles after exercise injuries. Am J Pathol. 1984 Oct;117(1):64-70.

[3]Perrin C, Vergely C, et al. In vitro antioxidant properties of calpain inhibitors: leupeptin and calpain inhibitor-1. Cell Mol Biol (Noisy-le-grand). 2002;48 Online Pub:OL267-70.