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

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1082744-20-4C₂₀H₂₅N₇O₂

Products

Catalog NumberPackaging Qty/Pack
5.38337.0001 Glass bottle 10 mg
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
Catalog Number GTIN
5.38337.0001 04054839059438

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Reference overview
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.
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.

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.