Other grades of this product :
| FHBANDDJQJAZOQ-CQSZACIVSA-N Basic information |
| Product Name: | FHBANDDJQJAZOQ-CQSZACIVSA-N | | Synonyms: | FHBANDDJQJAZOQ-CQSZACIVSA-N;PF-04449613;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;4H-Pyrazolo[3,4-d]pyrimidin-4-one, 1,5-dihydro-6-[(1R)-1-(3-phenoxy-1-azetidinyl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-;PF-04449613 >=98% (HPLC) | | CAS: | 1236858-52-8 | | MF: | C21H25N5O3 | | MW: | 395.45 | | EINECS: | | Product Categories: | | Mol File: | 1236858-52-8.mol |
| FHBANDDJQJAZOQ-CQSZACIVSA-N Chemical Properties |
| storage temp. | -20°C | | form | powder | | color | white to beige |
| FHBANDDJQJAZOQ-CQSZACIVSA-N Usage And Synthesis |
| 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. |
| FHBANDDJQJAZOQ-CQSZACIVSA-N Preparation Products And Raw materials |
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