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Products are for research use only. Not for human use. We do not sell to patients.
(PF 04447943; PF04447943)
PF-04447943 Chemical Structure
|Product name: PF-04447943|
|Cat. No.: HY-15441|
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.
|M.Wt||395.46||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 54.6 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.5287 mL||12.6435 mL||25.2870 mL|
|5 mM||0.5057 mL||2.5287 mL||5.0574 mL|
|10 mM||0.2529 mL||1.2644 mL||2.5287 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|PF-04447943||Pfizer Inc||Alzheimers disease||30-SEP-09||30-SEP-10||Phase 2||22-APR-13|
|Pfizer Inc||Alzheimers disease||30-APR-10||01-JUL-10||Phase 1||14-SEP-13|
|Pfizer Inc||Alzheimers disease||31-OCT-09||31-JUL-10||Phase 1||13-SEP-13|
|Pfizer Inc||Cognitive disorder||31-AUG-09||01-NOV-09||Phase 1||14-SEP-13|
|Pfizer Inc||Cognitive disorder||31-JAN-09||01-MAY-09||Phase 1||14-SEP-13|
|Pfizer Inc||Cognitive disorder||30-APR-09||01-MAY-09||Phase 1||14-SEP-13|
. Hutson, P. H, et al. 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. Neuropharmacology (2011), 61(4), 665-676.
. Claffey, Michelle M, et al. Application of Structure-Based Drug Design and Parallel Chemistry to Identify Selective, Brain Penetrant, In Vivo Active Phosphodiesterase 9A Inhibitors. Journal of Medicinal Chemistry (2012), 55(21), 9055-9068.
. Verhoest, Patrick R, et al. 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. Journal of Medicinal Chemistry (2012), 55(21), 9045-9054.
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Bay 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human); 50-fold more selective for PDE2 compared to PDE1 and greater than 100-fold selective compared to PDE5, PDE3B, PDE4B, PDE7B, PDE8A, PDE9A, PDE10A, and PDE11A.
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