Bestatin

CAS Number : 65391-42-6

Empirical Formula (Hill Notation) : C₁₆H₂₄N₂O₄ · HCl

Molecular Weight : 344.83

Beilstein Registry Number : 4628066

MDL number : MFCD00058004

PubChem Substance ID : 24278278

Packaging

1, 5 mg in glass bottle

10, 25 mg in poly bottle

100 mg in glass bottle

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.

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  peptides against degradation.