PF-05085727

PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A ( IC 50 =2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 In Vitro PF-05085727 shows weak activity with IC 50 of 162 μM to induce cell death in a cellular toxicity assay using transformed human liver endothelial (THLE) cells. PF-05085727 (3 μM) shows a minimal inhibition of cytochrome P450 enzymes (CYPs), inhibits 1A2, 2C8, 2C9, 2D6 and 3A4 with percentage% of 16%, 18%, 7%, 4%, and 30%, respectively. PF-05085727 (10 μM) inhibits PDE1B, PDE4B, PDE7B and PDE10A with IC 50 values of 12.146 μM, 22,503 μM, 13.157 μM and 6.515 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PF-05085727 (subcutaneous injection; 3.2 mg/kg/mice; 3 mg/kg/rat) gives a ratio of unbound brain (C bu ) to unbound plasma (C pu ) of ca. 0.27 and 0.37, respectively . PF-05085727 in mice leads to an acute and exposure-dependent elevation in the accumulation of bulk levels of cGMP in cortex, striatum, and hippocampus as measured by enzyme-linked immunosorbent assay . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:PDE2A 2 nM (IC 50 )

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