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PF-05085727

PF-05085727
PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11. PF-05085727 is an effective, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM) .
Catalog No. T16482Cas No. 1415637-72-7

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PF-05085727

Catalog No. T16482Cas No. 1415637-72-7

PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11. PF-05085727 is an effective, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM) .
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2 mg$825 days
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Product Introduction

Bioactivity
Description
PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11. PF-05085727 is an effective, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM) .
Targets&IC50
PDE2A:2 nM
In vitro
PF-05085727 displays weak activity with IC50?of 162 μM to induce cell death in a cellular toxicity assay using transformed human liver endothelial (THLE) cells. PF-05085727 (10 μM) inhibits PDE1B, PDE4B, PDE7B and PDE10A with IC50 values of 12.146 μM, 22,503 μM, 13.157 μM and 6.515 μM, respectively. PF-05085727 (3 μM) shows a minimal inhibition of cytochrome P450 enzymes (CYPs) and it inhibits 1A2, 2C8, 2C9, 2D6 and 3A4 with percentage% of 16%, 18%, 7%, 4%, and 30%, respectively[1].
In vivo
In mice, PF-05085727 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. PF-05085727 (subcutaneous injection; 3.2 mg/kg/mice; 3 mg/kg/rat) gives a ratio of unbound brain to unbound plasma of ca. 0.27 and 0.37, respectively[1].
Chemical Properties
Molecular Weight413.4
FormulaC20H18F3N7
Cas No.1415637-72-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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