生物活性 | Leupeptin hemisulfate is a membrane-permeable thiol protease inhibitor that inhibits Cathepsin B, Cathepsin H and Cathepsin L, and also impairs amphisome-lysosome fusion[1]. Leupeptin hemisulfate also exhibits anti-inflammatory effect[2]. |
IC50 & Target | Cathepsin[1] |
体内研究 (In Vivo) | Leupeptin (0-36 mg/kg; intraperitoneal injection; for 4 hours; C57BL/6NCrl male mice) is well tolerated by the animals and produces a strong, dose-dependent increase in LC3b-II in both the total tissue extracts and the lysosome and autophagosome-enriched pellet fraction[2].. Animal Model: | C57BL/6NCrl male mice (6-8 weeks old, 20-25 g)[2] | Dosage: | 0 mg/kg, 9 mg/kg, 18 mg/kg, 36 mg/kg | Administration: | Intraperitoneal injection; for 4 hours | Result: | Promoted the accumulation of LC3b-II in mouse liver. | |
分子量 | 475.59 |
Formula | C??H??N?O? . ?/?H?SO? |
CAS 号 | 103476-89-7 |
Sequence Shortening | Ac-LLR-CHO |
中文名称 | 亮肽素 |
SMILES | O=C[C@@H](NC([C@@H](NC([C@@H](NC(C)=O)CC(C)C)=O)CC(C)C)=O)CCCNC(N)=N.[0.5H2SO4] |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | - 80°C | 2 years | | -20°C | 1 year | In solvent | -80°C | 6 months | | -20°C | 1 month | |
溶解性数据 | In Vitro: H2O : ≥ 19 mg/mL (39.95 mM) * "≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.1027 mL | 10.5133 mL | 21.0265 mL | 5 mM | 0.4205 mL | 2.1027 mL | 4.2053 mL | 10 mM | 0.2103 mL | 1.0513 mL | 2.1027 mL | * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 |
参考文献 | [1]. Haspel J, et al. Characterization of macroautophagic flux in vivo using a leupeptin-based assay. Autophagy. 2011 Jun;7(6):629-42. [2]. Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68. |