All Photos(1)
Synonym(s):
PDE9 Inhibitor, PF-04447943, 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
Empirical Formula (Hill Notation):
C20H25N7O2
CAS Number:
Molecular Weight:
395.46
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Assay
≥97% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 50 mg/mL
storage temp.
−20°C
InChI
1S/C20H25N7O2/c1-13-10-26(12-17-21-5-2-6-22-17)11-16(13)18-24-19-15(20(28)25-18)9-23-27(19)14-3-7-29-8-4-14/h2,5-6,9,13-14,16H,3-4,7-8,10-12H2,1H3,(H,24,25,28)/t13-,16-/m1/s1
InChI key
IWXUVYOOUMLUTQ-CZUORRHYSA-N
General description
A 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.
A 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.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PDE9
PDE9
Reversible: yes
Target IC50: 2.8 nM, 4.5 nM and 18 nM for human, rhesus and rat PDE9A inhibition respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
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.
Verhoest, P. R., et al. 2012. J. Med. Chem.55, 9045.
Hutson, P.H., et al. 2011. Neuropharmacology.61, 665.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
13 - Non Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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