1. Metabolic Enzyme/Protease
  2. Proteasome
    HIV Protease
  3. Pepstatin Trifluoroacetate

Pepstatin Trifluoroacetate (Synonyms: Pepstatin A Trifluoroacetate)

Cat. No.: HY-P0018A Purity: 99.11%
Handling Instructions

Pepstatin Trifluoroacetate 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.

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

Pepstatin Trifluoroacetate Chemical Structure

Pepstatin Trifluoroacetate Chemical Structure

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 50 In-stock
Estimated Time of Arrival: December 31
50 mg USD 170 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Pepstatin Trifluoroacetate:

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Description

Pepstatin Trifluoroacetate 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 & 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 Trifluoroacetate 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].

In Vivo

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].

Molecular Weight

799.92

Formula

C₃₆H₆₄F₃N₅O₁₁

Sequence

IsoValeryl-Val-Val-Sta-Ala-Sta-OH

Sequence Shortening

IsoVeryl-VV-Sta-A-Sta-OH

SMILES

O=C(O)C(F)(F)F.CC(C[[email protected]](NC([[email protected]@H](NC([[email protected]@H](NC(CC(C)C)=O)C(C)C)=O)C(C)C)=O)[[email protected]@H](O)CC(N[[email protected]@H](C)C(N[[email protected]@H](CC(C)C)[[email protected]@H](O)CC(O)=O)=O)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

H2O : < 0.1 mg/mL (insoluble)

H2O : < 0.1 mg/mL (insoluble)

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 provided by MCE.
References
Cell Assay
[2]

Pepstatin A is freshly dissolved in DMSO at 7 mM. It is very slowly diluted (1:100) into the medium of HIV-infected H9 suspension cultures so that no pepstatin A precipitated (final concentration, 70 μM pepstatin A and 1% DMSO), and the cultures are incubated without change of culture medium for 48 hr. As control, uninfected H9 cells are also incubated with pepstatin and in addition HIV infected and uninfected cells are incubated with 1% DMSO but without pepstatin[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.11%

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Keywords:

PepstatinPepstatin AProteasomeHIV ProteaseInhibitorinhibitorinhibit

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Pepstatin Trifluoroacetate
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