A cell-permeable, potent, fast-acting, and selective inhibitor of prolyl oligopeptidase (PREP) (Ki = 23 pM). Reported to cross the blood-brain barrier. Inhibits about 85% PREP activity within 10 minutes of administration and exhibits a half-life of about 4.8h. Exhibits higher lipophilicity that increases its penetration across biological membranes in vivo. Maximum plasma and brain levels are achieved within 10 minutes following its i.p. administration. Shown to block oxidative-stress induced alpha-synuclein aggregation and clearance in cellular and animal models of Parkinson's disease. Also shown to improve cognitive performance in young rats (1-5mg/kg) in a dose-dependent manner.
Synonyms:(S)-1-((S)-1-(4-phenylbutanoyl)-pyrrolidine-2-carbonyl)pyrrolidine-2-carbonitrile, 4-phenylbutanoyl-Lprolyl-2(S)-cyanopyrrolidine, PREP inhibitor III, KYP-2047
Molecular Formula:C₂₀H₂₅N₃O₂
Solubility:DMSO
Molar Mass:339.4
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
