Pepstatin

Aspartic Protease Inhibitor PeptideRx: ResearchCompound: Research

Also known as: Acetyl-pepstatin, Isovaleryl-Val-Val-Sta-Ala-Sta, Pepstatin A, Pepstatin I, Statine-containing hexapeptide

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

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Summary

Pepstatin is a hexapeptide (Pepstatin A) containing the unusual amino acid statine; it is widely used as a potent, specific inhibitor of aspartic proteases in biochemical research.

Mechanism of Action

Reversible competitive inhibition of aspartic proteases (e.g., pepsin, cathepsin D) by binding to the active site

Routes of Administration

IntravenousTopical

Goals & Uses

  • HIV protease inhibitionAntiviral ResearchLow
  • Anti-cancer (cathepsin D inhibition)Investigational TherapeuticLow
  • Protease inhibitor cocktail componentResearch ToolHigh
  • Neuroprotection in neurodegeneration modelsInvestigational TherapeuticLow
  • Protease inhibitionResearch ToolHigh
  • Inhibition of cathepsin D in lysosomal researchResearch ToolHigh

Contraindications

  • Clinical therapeutic use in humansRegulatoryHigh

Adverse Effects

  • Poor oral/systemic bioavailabilityPharmacokineticCommon
  • Non-selective aspartyl protease inhibitionPharmacodynamicCommon

Drug Interactions

  • Renin inhibitorsModerate

Population Constraints

  • Human clinical populationsGeneralAbsolute

Regulatory Status

  • European UnionUnapprovedNo EMA approval; sold as laboratory chemical.
  • United StatesUnapprovedAvailable only as a research reagent; no FDA approval or IND on record for therapeutic use.
  • United KingdomUnapprovedNo MHRA approval; available as research reagent only.

Not approved for any clinical indication; used only as a research reagent.

Evidence & Sources

No sources recorded yet.

Frequently Asked Questions

What is Pepstatin?

Pepstatin is a hexapeptide (Pepstatin A) containing the unusual amino acid statine; it is widely used as a potent, specific inhibitor of aspartic proteases in biochemical research.

What is Pepstatin used for?

Pepstatin is educationally associated with: HIV protease inhibition, Anti-cancer (cathepsin D inhibition), Protease inhibitor cocktail component, Neuroprotection in neurodegeneration models, Protease inhibition, Inhibition of cathepsin D in lysosomal research. Educational only — not medical advice.

How is Pepstatin administered?

Recorded routes of administration: Intravenous, Topical.

What are the potential side effects of Pepstatin?

Reported adverse effects include: Poor oral/systemic bioavailability, Non-selective aspartyl protease inhibition. This list is not exhaustive — consult a qualified clinician.

Who should avoid Pepstatin?

Recorded contraindications: Clinical therapeutic use in humans. Consult a qualified clinician before use.