Pepstatin Trifluoroacetate

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)

Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific acid protease inhibitor produced by actinomycetes, with IC ₅₀ s 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 (Pepstatin A) inhibits the recombinant HIV protease with an IC ₅₀ of 250 μM. Pepstatin shows no effect on cellular protein synthesis and probably does not exert severe cell toxicity.

Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) has a very low toxicity, with LD ₅₀ s 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.