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编 号:F305538
分子式:C36H67N5O11
分子量:745.94
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生物活性:
Pepstatin (Pepstatin A) acetate is a specific, orally active aspartic protease inhibitor produced by actinomycetes, 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. Pepstatin acetate also inhibits HIV protease.

体内研究:
Pepstatin (Pepstatin A) has a 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 oral route.Pepstatin (0.5-50 mg/kg, p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats.Animal Model:Pylorus ligated male Wistar rats
Dosage:0.5, 1, 10 and 50 mg/kg
Administration:Oral administration, 15 minutes after pyloric ligation
Result:Effectively prevented stomach ulceration.

体外研究:
Pepstatin (Pepstatin A) (7 μM; 48 h) affects the intracellular processing of HIV-specific gag protein.
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