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Leupeptin Hemisulfate(NK381)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Leupeptin Hemisulfate(NK381)图片
CAS NO:103476-89-7
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)475.59
FormulaC20H38N6O4.1/2H2SO4
CAS No.103476-89-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 95 mg/mL (199.8 mM)
Water: 95 mg/mL (199.8 mM)
Ethanol: 95 mg/mL (199.8 mM)
SMILES Code CC(C)C[C@@H](C(N)=O)N(C([C@H](CC(C)C)NC(C)=O)=O)[C@H](C=O)CCCNC(N)=N.CC(C)C[C@@H](C(N)=O)N(C([C@H](CC(C)C)NC(C)=O)=O)[C@H](C=O)CCCNC(N)=N.O=S(O)(O)=O
SynonymsNK-381; NK 381; Leupeptin hemisulfate; NK381;

Chemical Name: (S)-2-acetamido-N-((S)-1-amino-4-methyl-1-oxopentan-2-yl)-N-((S)-5-guanidino-1-oxopentan-2-yl)-4-methylpentanamide hemisulfate

InChi Key: HFKRKHUDDFQRJB-VFFZMTJFSA-N

InChi Code: InChI=1S/2C20H38N6O4.H2O4S/c2*1-12(2)9-16(25-14(5)28)19(30)26(17(18(21)29)10-13(3)4)15(11-27)7-6-8-24-20(22)23;1-5(2,3)4/h2*11-13,15-17H,6-10H2,1-5H3,(H2,21,29)(H,25,28)(H4,22,23,24);(H2,1,2,3,4)/t2*15-,16-,17-;/m00./s1

实验参考方法
In Vitro

In vitro activity: Leupeptin, produced by various species of actinomycetes, strongly inhibit proteolysis. Leupeptin hemisulfate protects tubulin from endogenous proteolytic activities during the isolation procedure and results in increased tubulin purity. Leupeptin hemisulfate could restore up to 50% of hepatitis B surface antigen (HBsAg) expression in cell suspension cultures.


Cell Assay: In cultures of MRC-C cells, Leupeptin prevented multiplication of the human coronavirus strain 229E. The IC50 value of Leupeptin in plaque tests was 0.4 μg/mL, whilst growth of host cells was unaffected by Leupeptin at 50 μg/mL. In single-cycle growth experiments, Leupeptin (100 μg/mL) reduced virus yield only if added within 2 hrs of infection, indicating its action on an early stage of virus replication.

In VivoLeupeptin was well tolerated by the animals and dose-dependently produced a substantial increase in LC3b-II in both the total tissue extracts and the lysosome enriched fraction (LE fraction). At the electron microscopy (EM) level, leupeptin induced the accumulation of electron-dense vesicular structures that, in hepatocytes, were visible by 60 min after treatment (40 mg/kg). The results suggested that Leupeptin enhanced LC3b-II levels in vivo by protecting this protein from being degraded inside lysosomes, and thus the leupeptin-based assay could be potentially used for studying the dynamics of macroautophagy in mice.
Animal model C57BL/6NCrl male mice
Formulation & Dosage0, 9, 18 36 and 40 mg/kg; i.p. injection
References

J Antibiot (Tokyo). 1969 Nov;22(11):558-68; Cell Biol Int Rep. 1985 Sep;9(9):849-57; Plant Cell Rep. 2007 Sep;26(9):1575-84.