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Pepstatin A
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。
Pepstatin A图片
CAS NO:26305-03-3
规格:98%
分子量:685.9
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议
500mg电议
1g电议

产品介绍
Aspartic proteinases inhibitor
CAS:26305-03-3
分子式:C34H63N5O9
分子量:685.9
纯度:98%
存储:Store at -20°C

Background:

Pepstatin A is a well-known inhibitor of aspartic proteinases with IC50 values of 15 μM, 2 μM,< 5 nM and< 40 nM for human renin, HIV protease, pepsin and cathepsin D, respectively [1, 2].


Pepstatin A is a pentapeptide. It was originally isolated from the microbe. As a most potent renin inhibitor, pepstatinA inhibited porcine renin and human renin at weak acid pH value with IC50 values of 0.32 and 15 μM, respectively. The disadvantage is that, pepstatin Ais hydrophobic. To couple the charged hydrophilic residues to the C-terminal of pepstatinA can increase its solubility. Besides the renin, pepstatin A was also reported to have inhibitory effects on HIV protease and subsequently suppressed the virus replication. In cultured H9 cells, pepstatinA treatment blocked the proteolytic processing of the virus gag precursor and inhibited the production of infectious HIV. Moreover, pepstatin A was found to inhibit osteoclast differentiation due to its inhibitory efficacy of cathepsin D and E [1, 3 and 4].


参考文献:
1. Eid M, Evin G, Castro B, et al.New renin inhibitors homologous with pepstatin.Biochem. J, 1981, 197: 465-471.
2. Sarubbi E, Seneci P F, Angelastro M R, et al. Peptide aldehydes as inhibitors of HIV protease. FEBS letters, 1993, 319(3): 253-256.
3. von der Helm K, Gürtler L, Eberle J, et al. Inhibition of HIV replication in cell culture by the specific aspartic protease inhibitor pepstatin A. FEBS letters, 1989, 247(2): 349-352.
4. Yoshida H, Okamoto K, Iwamoto T, et al. Pepstatin A, an aspartic proteinase inhibitor, suppresses RANKL-induced osteoclast differentiation. Journal of biochemistry, 2006, 139(3): 583-590.
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