537012 Prolyl Endopeptidase Inhibitor III, KYP-2047 - Calbiochem

537012
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₀H₂₅N₃O₂

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      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
          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.