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B8385 Sigma-Aldrich

Bestatin hydrochloride

≥98% (HPLC)

Synonym: N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine hydrochloride

  • CAS Number 65391-42-6

  • Empirical Formula (Hill Notation) C16H24N2O4 · HCl

  • Molecular Weight 344.83

  •  Beilstein/REAXYS Number 4628066

  •  MDL number MFCD00058004

  •  PubChem Substance ID 24278278



General description

Chemical structure: amino acid derivatives


1, 5 mg in glass bottle

10, 25 mg in poly bottle

100 mg in glass bottle

Biochem/physiol Actions

A metalloprotease inhibitor selective for aminopeptidase. Bestatin is a competitive and specific inhibitor of leucine aminopeptidase, aminopeptidase B, and triamino peptidase. It inhibits aminopeptidase B at 60 nM (using arginine-β-naphthylamide as substrate) and leucine aminopeptidase at 20 nM (leucine-β-naphthylamide as substrate). It showed no inhibition of aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, or themolysin. It offers promise as a novel analgesic because it protects endogenous opioid peptides against degradation.

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

Preparation Note

Solubility testing in water at 25 mg/ml yields a clear solution. Stock solutions at 1 mM are expected to be stable at least one month stored at -20 °C.

Legal Information

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Safety & Documentation

Safety Information

NONH for all modes of transport
WGK Germany 


Certificate of Analysis (COA)

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Certificate of Origin (COO)

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