| Identification | Back Directory | [Name]
FHBANDDJQJAZOQ-CQSZACIVSA-N | [CAS]
1236858-52-8 | [Synonyms]
PF-04449613
PF 04449613,PF04449613
PF-04449613 >=98% (HPLC)
FHBANDDJQJAZOQ-CQSZACIVSA-N
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)- | [Molecular Formula]
C21H25N5O3 | [MDL Number]
MFCD28963901 | [MOL File]
1236858-52-8.mol | [Molecular Weight]
395.45 |
| Hazard Information | Back Directory | [Uses]
PF 04449613 (cas# 1236858-52-8) is a useful research chemical. Potent PDE9 inhibitor. | [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. | [IC 50]
PDE9A: 22 nM (IC50) | [storage]
Store at -20°C |
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