Pepstatin Ammonium (Synonyms: Pepstatin A Ammonium) |
رقم الكتالوجGC36871 |
Pepstatin Ammonium هو مثبط بروتياز الأسبارتيك المحدد الذي تنتجه الفطريات الشعاعية ، مع IC50s من 4.5 نانومتر ، 6.2 نانومتر ، 150 نانومتر ، 290 نانومتر ، 520 نانومتر و 260 نانومتر للهيموجلوبين - البيبسين ، الهيموجلوبين - البروكتاز ، الكازين - البيبسين ، الكازين - البروكتاز ، الكازين - البروتياز الحمضي والبروتياز الهيموجلوبين الحمضي على التوالي
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Sample solution is provided at 25 µL, 10mM.
Pepstatin Ammonium is a specific 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 Ammonium also inhibits HIV protease. IC50: 4.5 nM (Hemoglobin-pepsin), 6.2 nM (Hemoglobin-proctase), 150 nM (Casein-pepsin), 260 nM (Hemoglobin-acid protease), 290 nM (Casein-proctase), 520 nM (Casein-acid protease)[1]
Pepstatin Ammonium is a specific acid 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[1]. Pepstatin (Pepstatin A) inhibits the recombinant HIV protease with an IC50 of 250 μM. Pepstatin shows no effect on cellular protein synthesis and probably does not exert severe cell toxicity[2].
Pepstatin 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[1].
[1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62. [2]. Seelmeier S, et al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6.
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