PZ0349

PF-04449613

≥98% (HPLC)

• Synonym(e): (R)-6-(1-(3-Phenoxyazetidin-1-yl)ethyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one, 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, 6-[(1R)-1-(3-Phenoxyazetidin-1-yl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, PF 4449613, PF-9613
• Empirische Formel (Hill-System): C₂₁H₂₅N₅O₃
• CAS-Nummer: 1236858-52-8
• Molekulargewicht: 395.45
• UNSPSC-Code: 51111800
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 10 mg/mL, clear
• Versandbedingung: wet ice
• Lagertemp.: −20°C

Beschreibung

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable