半岛bd体育手机客户端 说明
包装
5, 25 mg in glass bottle
生化/生理作用
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 vivowith 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.
法律信息
Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.
基本信息
经验(实验)分子式 | C21H25N5O3 |
分子量 | 395.45 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
manufacturer/tradename | Pfizer? |
颜色 | white to beige |
溶解性 | DMSO: 10 mg/mL, clear |
创始人 | Pfizer |
运输 | wet ice |
储存温度 | ?20℃ |
安全信息
储存分类代码 | 13 - Non Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich