产品信息
Pepstatin is a specific aspartic proteases inhibitor produced by actinomycetes, and inhibits the aspartic proteases cathepsin D, pepsin and renin.
|
CAS号
|
26305-03-3 |
| 分子式 |
C34H63N5O9 |
| 主要靶点 |
Amino Acids and Derivatives|Autophagy|Proteasome|HIV Protease |
| 主要通路 |
蛋白酶体|微生物学|代谢|自噬|泛素化 |
| 分子量 |
685.89 |
| 纯度 |
99.14%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服 |
| 储存条件 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| 别名 |
抑肽素|Pepstatin A|Ahpatinin C|Pepsin Inhibitor S 735A |
靶点活性
hemoglobin-proctase:6.2 nM|hemoglobin-pepsin:4.5 nM|Hemoglobin-acid protease:260 nM|casein-pepsin:150 nM|casein-acid protease:520 nM|casein-proctase:290 nM
体内活性
Pepstatin has very low toxicity, with LD50s of 1090 mg/kg, 875 mg/kg, 820 mg/kg and 450 mg/kg for mice, rats, rabbits, and dogs by i.p. route, and > 2000 mg/kg for all species by the oral route. Pepstatin (0.5-50 mg/kg, p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats [1]. The bacterial motility in the pepstatin-treated gastric juice was measured at the pH values of 2.0, 3.0, 4.0, 4.5, and 5.0 (n = 5 for each pH). The bacteria remained motile significantly longer than in the in vivo experiments without pepstatin [4].
体外活性
Pepstatin is a specific acid protease inhibitor with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease, and hemoglobin-acid protease, respectively [1]. Pepstatin inhibits the recombinant HIV protease (IC50: 250 μM). Pepstatin shows no effect on cellular protein synthesis and probably does not exert severe cell toxicity [2].
溶解度
DMSO:25 mg/mL,H2O:Insoluble,Ethanol:1 mg/mL (1.46 mM)
细胞实验
Pepstatin A is freshly dissolved in DMSO at 7 mM. It is very slowly diluted (1:100) into the medium of HIV-infected H9 suspension cultures so that no pepstatin A precipitated (final concentration, 70 μM pepstatin A and 1% DMSO), and the cultures are incubated without change of culture medium for 48 hr. As a control, uninfected H9 cells are also incubated with pepstatin and in addition HIV infected and uninfected cells are incubated with 1% DMSO but without pepstatin [2].
动物实验
To investigate the effect of pepsins on bacterial motility, similar experiments were performed, but the pepsin in the stomach was inactivated by rinsing the stomach with pepstatin (100 μl of a 2-mg/ml stock solution). Samples were taken and analyzed for bacterial motility at the test pH values of 2.0, 3.0, 4.0, 4.5, and 5.0 and at the same periods after application of the bacterial suspension as in the experiments with active pepsins [4].
