化学性质:
规格 | 5mg |
CAS | 1082744-20-4 |
别名 | PF 04447943;PF04447943 |
化学名 | 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 |
分子式 | C20H25N7O2 |
分子量 | 395.46 |
溶解度 | DMF: 25 mg/ml,DMSO: 25 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 12.5 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
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
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