[CAS NO. ]  Pepstatin Trifluoroacetate

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PRODUCTS SPECIFICATIONS

Distributor
Catalog
HY-P0018A
Brand
MCE
CAS
-

DESCRIPTION

Overview

MDL-
Molecular Weight799.92
Molecular FormulaC36H64F3N5O11
SMILES-

For research use only. We do not sell to patients.


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

In Vitro:

DMSO : 32 mg/mL ( 40.00 mM ; Need warming)

H 2 O : 1.1 mg/mL ( 1.38 mM ; Need ultrasonic)

Preparing
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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (2.60 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.60 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.60 mM); Clear solution

* All of the co-solvents are available by MCE.