Identification | Back Directory | [Name]
PF 04447943 | [CAS]
1082744-20-4 | [Synonyms]
EOS-62041 PF 4447943 PF 04447943 PF-04447943 PF 4447943;PF-4447943 PF04447943; PF 04447943 PF 04447943 - PF 4447943 PF-04447943 >=98% (HPLC) PDE9 Inhibitor, PF-04447943 - CAS 1082744-20-4 - Calbiochem (tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(oxan-4-yl)-2H-pyrazolo[3,4-d]pyrimidin-4-one 1,5-Dihydro-6-[(3S,4S)-4-methyl-1-(2-pyrimidinylmethyl)-3-pyrrolidinyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one 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 4H-Pyrazolo[3,4-d]pyrimidin-4-one, 1,5-dihydro-6-[(3S,4S)-4-methyl-1-(2-pyrimidinylmethyl)-3-pyrrolidinyl]-1-(tetrahydro-2H-pyran-4-yl)- | [Molecular Formula]
C20H25N7O2 | [MOL File]
1082744-20-4.mol | [Molecular Weight]
395.46 |
Chemical Properties | Back Directory | [Boiling point ]
599.8±60.0 °C(Predicted) | [density ]
1.52±0.1 g/cm3(Predicted) | [storage temp. ]
-20C | [solubility ]
Soluble in DMSO | [form ]
Off-white solid | [pka]
7.22±0.60(Predicted) | [color ]
Light yellow to yellow |
Hazard Information | Back Directory | [Biological Activity]
pf-04447943 is a potent and selective inhibitor of pde9 [1].phosphodiesterase 9 (pde9) selectively degrades cgmp and limits the cgmp-mediated signal transduction which occurs following glutamate binding to nmda receptors. pde9 in cortex and hippocampus of rodents and humans play an important role in memory and learning [1].pf-04447943 have high affinity with 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. in cultured hippocampal neurons, pf-04447943 (30-100 nm) significantly increased neurite outgrowth and synapse formation. also, pf-04447943 (100 nm) significantly facilitated hippocampal slice ltp evoked by a weak tetanic stimulus [1].in mice model, pf-04447943 (1 mg/kg) significantly reduced the time spent interacting with the female mouse during the second encounter 24 h later compared to the first encounter, which suggested that pf-04447943 enhanced recognition memory. while, pf-04447943 (3 or 10 mg/kg) didn’t change the interaction times for each encounter. these results suggested that pf-04447943 enhanced memory with an inverted u-shaped dose-response efficacy curve [1]. | [References]
[1]hutson ph, finger en, magliaro bc, 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. |
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Company Name: |
SPIRO PHARMA
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Website: |
www.spiropharma.com.cn |
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