| MDL | - |
|---|---|
| Molecular Weight | 799.92 |
| Molecular Formula | C36H64F3N5O11 |
| SMILES | - |
Pepstatin (Pepstatin A) Trifluoroacetate is a specific, orally active aspartic 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 Trifluoroacetate also inhibits HIV protease [1] [2] .
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 (Pepstatin A) (7 μM; 48 h) affects the intracellular processing of HIV-specific gag protein [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Pepstatin (Pepstatin A) 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
[1]
.
Pepstatin (0.5-50 mg/kg, p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Pylorus ligated male Wistar rats [1] |
| Dosage: | 0.5, 1, 10 and 50 mg/kg |
| Administration: | Oral administration, 15 minutes after pyloric ligation |
| Result: | Effectively prevented stomach ulceration. |
Solid
culture filtrates of several actinomycetes
Room temperature in continental US; may vary elsewhere.
Sealed storage, away from moisture
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
DMSO : 32 mg/mL ( 40.00 mM ; Need warming)
H 2 O : 1.1 mg/mL ( 1.38 mM ; Need ultrasonic)
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.2501 mL | 6.2506 mL | 12.5013 mL |
| 5 mM | 0.2500 mL | 1.2501 mL | 2.5003 mL |
| 10 mM | 0.1250 mL | 0.6251 mL | 1.2501 mL |