PF-05085727 是一种强效的 cGMP 依赖性的 PDE2A (IC50=2 nM) 选择性和具有脑通透性的抑制剂。PF-05085727 对 PDE2A 的选择性是 PDE1 和 PDE3-11 的 4000 倍。
货号:ajcx38720
CAS:1415637-72-7
分子式:C20H18F3N7
分子量：413.4
溶解度:DMSO : 62.5 mg/mL (151.19 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11[1].

PF-05085727 shows weak activity with IC50 of 162 μM to induce cell death in a cellular toxicity assay using transformed human liver endothelial (THLE) cells[1].
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[1].
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[1].

PF-05085727 (subcutaneous injection; 3.2 mg/kg/mice; 3 mg/kg/rat) gives a ratio of unbound brain (Cbu) to unbound plasma (Cpu) of ca. 0.27 and 0.37, respectively[1].
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[1].

[1]. Helal CJ, et al. Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor. J Med Chem. 2017 Jul 13;60(13):5673-5698.

Protocol:

PDE2A 2nM(IC50)