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537012 Prolyl Endopeptidase Inhibitor III, KYP-2047 - Calbiochem

537012
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₀H₂₅N₃O₂

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537012-5MG
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      Glass bottle 5 mg
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      Description
      OverviewA 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 4.8 hours. 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 α-synuclein aggregation and clearance in cellular and animal models of Parkinson's disease. Also shown to improve cognitive performance in young rats (1-5 mg/kg) in a dose-dependent manner.
      Catalogue Number537012
      Brand Family Calbiochem®
      Synonyms(S)-1-((S)-1-(4-phenylbutanoyl)-pyrrolidine-2-carbonyl)pyrrolidine-2-carbonitrile, 4-phenylbutanoyl-Lprolyl-2(S)-cyanopyrrolidine, PREP inhibitor III, KYP-2047
      References
      ReferencesJarho, E., et al. 2004. J. Med. Chem. 47, 5605.
      Venalainen, J., et al. 2011. Biochem. Pharmacol. 71, 683.
      Jalkanen, A., et al. 2006. Basic & Clin. Pharmac. & Tox. 100, 132.
      Jalkanen, A., et al. 2011. Basic & Clin. Pharmac. & Tox. 109, 443.
      Klimaviciusa, L., et al. 2012. Journ. Neuros. Methods. 204, 104.
      Myohanen, T., et al. 2012. Brit. J. Pharm. 166, 1097.
      Product Information
      FormClear, colorless oil
      Hill FormulaC₂₀H₂₅N₃O₂
      Chemical formulaC₂₀H₂₅N₃O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Prolyl Endopeptidase Inhibitor III, KYP-2047 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Prolyl Endopeptidase Inhibitor III, KYP-2047 - Calbiochem Certificates of Analysis

      TitleLot Number
      537012

      References

      Reference overview
      Jarho, E., et al. 2004. J. Med. Chem. 47, 5605.
      Venalainen, J., et al. 2011. Biochem. Pharmacol. 71, 683.
      Jalkanen, A., et al. 2006. Basic & Clin. Pharmac. & Tox. 100, 132.
      Jalkanen, A., et al. 2011. Basic & Clin. Pharmac. & Tox. 109, 443.
      Klimaviciusa, L., et al. 2012. Journ. Neuros. Methods. 204, 104.
      Myohanen, T., et al. 2012. Brit. J. Pharm. 166, 1097.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision16-November-2012 JSW
      Synonyms(S)-1-((S)-1-(4-phenylbutanoyl)-pyrrolidine-2-carbonyl)pyrrolidine-2-carbonitrile, 4-phenylbutanoyl-Lprolyl-2(S)-cyanopyrrolidine, PREP inhibitor III, KYP-2047
      DescriptionA 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 4.8 hours. 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 α-synuclein aggregation and clearance in cellular and animal models of Parkinson's disease. Also shown to improve cognitive performance in young rats (1-5 mg/kg) in a dose-dependent manner.
      FormClear, colorless oil
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₀H₂₅N₃O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesJarho, E., et al. 2004. J. Med. Chem. 47, 5605.
      Venalainen, J., et al. 2011. Biochem. Pharmacol. 71, 683.
      Jalkanen, A., et al. 2006. Basic & Clin. Pharmac. & Tox. 100, 132.
      Jalkanen, A., et al. 2011. Basic & Clin. Pharmac. & Tox. 109, 443.
      Klimaviciusa, L., et al. 2012. Journ. Neuros. Methods. 204, 104.
      Myohanen, T., et al. 2012. Brit. J. Pharm. 166, 1097.