EMAIL THIS PAGE TO A FRIEND
PZ0349 Sigma-Aldrich

PF-04449613

≥98% (HPLC)

Synonym: (R)-6-(1-(3-Phenoxyazetidin-1-yl)ethyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one, 1,5-Dihydro-6-[(1R)-1-(3-phenoxy-1-azetidinyl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one, 6-[(1R)-1-(3-Phenoxyazetidin-1-yl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, PF 4449613, PF-9613

  • CAS Number 1236858-52-8

  • Empirical Formula (Hill Notation) C21H25N5O3

  • Molecular Weight 395.45

Purchase

Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Cyclic Nucleotide Metabolism,
Quality Level   100
assay   ≥98% (HPLC)
form   powder
mfr. no.   Pfizer®
color   white to beige
solubility   DMSO: 10 mg/mL, clear
originator   Pfizer
shipped in   wet ice
storage temp.   −20°C

Description

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

PF-04449613 is a potent and selective cGMP-competitive PDE9A inhibitor (IC50 = 24 nM; IC50 >800 nM against other PDE members), displaying more than 1000-fold selectivity over the majority of 79 non-PDE targets investigated with the exception of cytochrome P450 2C19 (IC50 = 1600 nM), dopamine transporter (Ki = 110 nM), μ-opioid receptor (Ki = 3500 nM), and sodium channel binding site 2 (Ki = 470 nM). PF-4449613 is shown to effectively increase cGMP levels in brain (1-10 mg/kg s.c.; mice) and CSF (1-32 mg/kg s.c.; rats and cynomolgus macaques) in vivo with good brain penetration (brain/plasma ratio of 0.8 in mice). PF-04449613 is effective against D-amphetamine-induced auditory gating deficit (by 43% with 1 mg/kg PF-04449613 s.c.; 1 mg/kg AMP i.v.) and transverse aortic constriction-caused cardiac dysfunction (30 mg/kg/12 h p.o.) in mice in a NOS-independent manner.

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

Pfizer is a registered trademark of Pfizer, Inc.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

Please Enter a Lot Number
Protocols & Articles

Articles

Pfizer Compounds for Cyclic Nucleotides

From our library of Articles, Sigma-Aldrich presents Pfizer Compounds for Cyclic Nucleotides

Peer-Reviewed Papers
15

References

Related Products

Technical Service:

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Bulk Ordering & Pricing:

Need larger quantities for your development, manufacturing or research applications?