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538337 PDE9 Inhibitor, PF-04447943 - CAS 1082744-20-4 - Calbiochem

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Synonymes: 6-((3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one, PF04447943, PF 04447943, Phosphodiesterase 9A Inhibitor, PF-04447943

Primary Target: PDE9
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538337
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Tableau de caractéristiques principal

CAS #Empirical Formula
1082744-20-4C₂₀H₂₅N₇O₂

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      Description
      OverviewA cell-permeable, blood-brain barrier permeant, pyrazolo[3,4 d]pyrimidinone compound that acts as a highly potent, selective, and active site-targeting inhibitor of phosphodiesterase 9A (PDE9A; Ki = 2.8 nM, 4.5 nM, and 18 nM for human, rhesus monkey, and rat recombinant PDE9A, respectively). Exhibits high selectivity over other phosphodiesterases (Ki = 8.6, 99, 50, 29, 14.9, 5.3, 75, 50, 51.2, and 80 µM for PDE1, PDE2A3, PDE3A, PDE4A, PDE5A, PDE6C, PDE7A2, PDE8A, PDE10, PDE11, respectively). Does not affect the activity of 60 other enzymes and receptors. Shown to diminish ANP-stimulated cGMP levels in human embryonic kidney cells expressing rhesus PDE9A2 (IC50 = 375 nM). Shown to improve performance in novel object recognition in rats (~ 3 mg/kg, p.o.). Exhibits desirable pharmacokinetic properties with t1/2 = 4.9 h, Tmax = 0.3 h in rat.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number538337
      Brand Family Calbiochem®
      Synonyms6-((3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one, PF04447943, PF 04447943, Phosphodiesterase 9A Inhibitor, PF-04447943
      DescriptionPDE9 Inhibitor, PF-04447943
      References
      ReferencesLee, D., et al. 2015. Nature. 519, 472
      Verhoest, P. R., et al. 2012. J. Med. Chem. 55, 9045.
      Hutson, P.H., et al. 2011. Neuropharmacology. 61, 665.
      Product Information
      CAS number1082744-20-4
      FormOff-white solid
      Hill FormulaC₂₀H₂₅N₇O₂
      Chemical formulaC₂₀H₂₅N₇O₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPDE9
      Primary Target IC<sub>50</sub>2.8 nM, 4.5 nM and 18 nM for human, rhesus and rat PDE9A inhibition respectively
      Purity≥97% 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 -20°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
      5.38337.0001 04054839059438

      Documentation

      PDE9 Inhibitor, PF-04447943 - CAS 1082744-20-4 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Lee, D., et al. 2015. Nature. 519, 472
      Verhoest, P. R., et al. 2012. J. Med. Chem. 55, 9045.
      Hutson, P.H., et al. 2011. Neuropharmacology. 61, 665.
      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.

      Revision25-June-2016 JSW
      Synonyms6-((3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one, PF04447943, PF 04447943, Phosphodiesterase 9A Inhibitor, PF-04447943
      DescriptionA cell-permeable, blood-brain barrier permeant, pyrazolo[3,4 d]pyrimidinone compound that acts as a highly potent, selective, and active site-targeting inhibitor of phosphodiesterase 9A (PDE9A; Ki = 2.8 nM, 4.5 nM, and 18 nM for human, rhesus monkey, and rat recombinant PDE9A, respectively). Exhibits high selectivity over other phosphodiesterases (Ki = 8.6, 99, 50, 29, 14.9, 5.3, 75, 50, 51.2, and 80 µM for PDE1, PDE2A3, PDE3A, PDE4A, PDE5A, PDE6C, PDE7A2, PDE8A, PDE10, PDE11, respectively). Does not affect the activity of 60 other enzymes and receptors. Shown to diminish ANP-stimulated cGMP levels in human embryonic kidney cells expressing rhesus PDE9A2 (IC50 = 375 nM). Shown to improve performance in novel object recognition in rats (~ 3 mg/kg, p.o.). Exhibits desirable pharmacokinetic properties with t1/2 = 4.9 h, Tmax = 0.3 h in rat.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1082744-20-4
      Chemical formulaC₂₀H₂₅N₇O₂
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      -20°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
      ReferencesLee, D., et al. 2015. Nature. 519, 472
      Verhoest, P. R., et al. 2012. J. Med. Chem. 55, 9045.
      Hutson, P.H., et al. 2011. Neuropharmacology. 61, 665.