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[CAS NO. ] Pepstatin Trifluoroacetate
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-P0018A |
| Brand: | MCE |
| CAS: | - |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 799.92 |
| Molecular Formula | C36H64F3N5O11 |
| SMILES | - |
17 Publications Citing Use of MCE
- [1]Adv Sci (Weinh). 2022 Oct 10;e2203831.
- [2]Sci Adv. 2022 Nov 11;8(45):eabn6579.
- [3]Cell Rep. 2021 Nov 2;37(5):109931.
- [4]Environ Sci Technol. 2017 Dec 5;51(23):13938-13948.
- [5]Cancer Lett. 2022 Mar 9;215629.
- [6]Cell Death Dis. 2022 Dec 16;13(12):1048.
- [7]Pharmacol Res. 2021 Dec 1;175:105985.
- [8]FASEB J. 2022 Jan;36(1):e22121.
- [9]Int J Antimicrob Agents. 2019 Dec;54(6):814-819.
- [10]J Virol. 2021 Sep 22;JVI0153721.
- [11]Int J Oncol. 2019 Jul;55(1):331-339.
- [12]Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171.
- [13]Eur J Pharmacol. 2022 Feb 11;920:174823.
- [14]Biochem Bioph Res Co. 2020 Sep 10;530(1):292-300.
- [15]Mol Med Rep. 2019 Jan;19(1):41-50.
- [16]Biol Pharm Bull. 2022 Feb 3.
- [17]Pharmaceuticals. 2022, 15(12), 1509
Summary
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 & Target
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]
In Vitro
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.
In Vivo
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. |
Appearance
Solid
Source
culture filtrates of several actinomycetes
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
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)
Solvent & Solubility
DMSO : 32 mg/mL ( 40.00 mM ; Need warming)
H 2 O : 1.1 mg/mL ( 1.38 mM ; Need ultrasonic)
Stock Solutions
| 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 |
References
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