PF-04447943


CAS No. : 1082744-20-4

PF-04447943,1082744-20-4
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000359
Synonyms:6-(4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(2H)-one
Molecular Formula:C₂₀H₂₅N₇O₂
Molecular Weight:395.46
Target:PDE
IC50:2.8 nM (Human recombinant PDE9)
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Appearance:Solid powder
Purity: > 98%
Cat No:I000359
Cas No:1082744-20-4
Product-Name:PF-04447943
InChI: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/h2,5-6,9,13-14,16,23H,3-4,7-8,10-12H2,1H3/t13-,16-/m1/s1
InChIKey:ACXPOEVOYNJCHF-CZUORRHYSA-N
SMILES:CC1CN(CC1C2=NC(=O)C3=CNN(C3=N2)C4CCOCC4)CC5=NC=CC=N5

PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor (Ki of 2.8, 4.5 and 18 nM) for human, rhesus and rat recombinant PDE9 respectively and high selectivity for PDE9 versus PDEs1-8 and 10-11.
IC50 value: 2.8 nM (Human recombinant PDE9)
Target: PDE 9
PF-04447943 increased indicators of hippocampal synaptic plasticity and improved cognitive function in a variety of cognition models in both rats and mice. PF-04447943 was found to have high affinity (Ki of 2.8, 4.5 and 18 nM) for human, rhesus and rat recombinant PDE9 respectively and high selectivity for PDE9 versus PDEs1-8 and 10-11. Inhibition of phosphodiesterase 9 (PDE9) has been reported to enhance rodent cognitive function and may represent a potential novel approach to improving cognitive dysfunction in Alzheimer/'s disease.


1:A multicenter, double-blind, placebo-controlled trial of the PDE9A inhibitor, PF-04447943, in Alzheimer/'s disease. Schwam EM, Nicholas T, Chew R, Billing CB, Davidson W, Ambrose D, Altstiel LD.Curr Alzheimer Res. 2014;11(5):413-21. PMID: 24801218
2:Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders. Verhoest PR, Fonseca KR, Hou X, Proulx-Lafrance C, Corman M, Helal CJ, Claffey MM, Tuttle JB, Coffman KJ, Liu S, Nelson F, Kleiman RJ, Menniti FS, Schmidt CJ, Vanase-Frawley M, Liras S.J Med Chem. 2012 Nov 8;55(21):9045-54. doi: 10.1021/jm3007799. Epub 2012 Jul 25. PMID: 22780914
3:The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943 attenuates a scopolamine-induced deficit in a novel rodent attention task. Vardigan JD, Converso A, Hutson PH, Uslaner JM.J Neurogenet. 2011 Dec;25(4):120-6. doi: 10.3109/01677063.2011.630494. Epub 2011 Nov 9. PMID: 22070409
4:The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943 (6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents. Hutson PH, Finger EN, Magliaro BC, Smith SM, Converso A, Sanderson PE, Mullins D, Hyde LA, Eschle BK, Turnbull Z, Sloan H, Guzzi M, Zhang X, Wang A, Rindgen D, Mazzola R, Vivian JA, Eddins D, Uslaner JM, Bednar R, Gambone C, Le-Mair W, Marino MJ, Sachs N, Xu G, Parmentier-Batteur S.Neuropharmacology. 2011 Sep;61(4):665-76. doi: 10.1016/j.neuropharm.2011.05.009. Epub 2011 May 19. PMID: 21619887
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