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513050 PDE10A Inhibitor, Cpd15 - Calbiochem

PDE10A Inhibitor, Cpd15 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: Phosphodiesterase 10A Inhibitor, (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol

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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      Empirical Formula
      C₁₈H₁₆ClN₅O
      Description
      Overview

      This product has been discontinued.



      A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5 nM against human PDE10A), while exhibiting >500-fold selectivity over other human PDEs 1-11 and little activity against CYP3A4 (IC50 >20 µM) or a panel of 23 kinases (IC50 >30 µM). Reported to be orally available in monkey and rat species and be efficacious in reversing NMDAR antagonist (+)-MK-801- (Cat. No. 475878) induced hyperactivity in a ratsl (MED = 10 mg/kg p.o.) in vivo.
      Catalogue Number513050
      Brand Family Calbiochem®
      SynonymsPhosphodiesterase 10A Inhibitor, (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol
      References
      ReferencesMcElroy, W., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1335.
      Product Information
      FormOff-white powder
      Hill FormulaC₁₈H₁₆ClN₅O
      Chemical formulaC₁₈H₁₆ClN₅O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Target K<sub>i</sub>≤5 nM
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Référence GTIN
      513050 0

      Documentation

      PDE10A Inhibitor, Cpd15 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      PDE10A Inhibitor, Cpd15 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      513050

      Références bibliographiques

      Aperçu de la référence bibliographique
      McElroy, W., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1335.
      Fiche technique

      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.

      Revision11-March-2013 JSW
      SynonymsPhosphodiesterase 10A Inhibitor, (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol
      DescriptionA cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5 nM against human PDE10A-catalyzed cAMP hydrolysis), while exhibiting >500-fold selectivity over other human PDEs 1-11 and much reduced or little activity against CYP3A4 (IC50 = 7.9 and >20 µM, respectively, with or without preincubation) as well as a panel of 23 kinases (IC50 >30 µM). Reported to be orally available in monkey (AUC0-6 h = 11,496 nM·h, T1/2 = 7.1 h; 3 mg/kg p.o.) and rat (AUC0-6 h475878) induced hyperactivity (1 h post p.o.) in a rat schizophrenia model (MED = 10 mg/kg p.o.) in vivo.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₈H₁₆ClN₅O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesMcElroy, W., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1335.