PF-05085727

产品编号 T16482Cas号 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) .

PF-05085727

产品编号 T16482Cas号 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) .

规格	价格	库存
2 mg	¥ 484	5日内发货
5 mg	¥ 792	6-8周
100 mg	¥ 5,470	6-8周

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产品介绍

生物活性

产品描述	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) .
靶点活性	PDE2A:2 nM
体外活性	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].
体内活性	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].