Millipore Sigma Vibrant Logo

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

SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: 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
View Products on Sigmaaldrich.com
538337
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1082744-20-4C₂₀H₂₅N₇O₂

Preis & Verfügbarkeit

Bestellnummer VerfügbarkeitVerpackung St./Pkg. Preis Menge
5383370001
Verfügbarkeit wird abgerufen...
—
Eingeschränkte Verfügbarkeit Eingeschränkte Verfügbarkeit
Lieferbar 
Produkt wurde eingestellt
Begrenzter Lagerbestand
Bestätigung der Verfügbarkeit erforderlich
    Restmenge: Angebot folgt
      Restmenge: Angebot folgt
      Bitte erfragen
      Kontakt zum Kundenservice
      Contact Customer Service

      		 Glasflasche 10 mg
      Preis wird abgerufen...
      Preis nicht abrufbar
      Die Mindestmenge muss ein Vielfaches sein von
      Maximum Quantity is
      Bei Bestätigung Weitere Informationen
      Sie haben () gespart
       
      —
      Bitte erfragen
      		 —
      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
      Bestellnummer GTIN
      5383370001 04054839059438

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      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.
      Datenblatt

      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.