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PF-04449613,≥98% (HPLC)

别名:PF-04449613;PF 4449613;(R)-6-(1-(3-Phenoxyazetidin-1-yl)ethyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo3,4-dpyrimidin-4(5H)-one, 6-(1R)-1-(3-Phenoxyazetidin-1-yl)ethyl-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo3,4-dpyrimidin-4-one, 1,5-Dihydro-6-(1R)-1-(3-phenoxy-1-azetidinyl)ethyl-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo3,4-dpyrimidin-4-one, PF-9613

Empirical Formula (Hill Notation): C21H25N5O3 CAS号: 1236858-52-8 分子量: 395.45
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): PZ0349
CAS号: 1236858-52-8
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$354.21

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 vivo with 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.
 
PF-04449613 是一种有效且选择性的 cGMP 竞争性 PDE9A 抑制剂(IC50 = 24 nM;对其他 PDE 成员的 IC50 >800 nM),对所研究的 79 个非 PDE 靶点中的大多数具有超过 1000 倍的选择性 细胞色素 P450 2C19 (IC50 = 1600 nM)、多巴胺转运蛋白 (Ki = 110 nM)、μ-阿片受体 (Ki = 3500 nM) 和钠通道结合位点 2 (Ki = 470 nM)。 PF-4449613 显示可在体内有效增加大脑(1-10 mg/kg sc;小鼠)和 CSF(1-32 mg/kg sc;大鼠和食蟹猴)的 cGMP 水平,并具有良好的脑渗透(脑/血浆比率) 在小鼠中为 0.8)。 PF-04449613 对 D-苯丙胺引起的听觉门控缺陷(1 mg/kg PF-04449613 sc;1 mg/kg AMP iv)和横向主动脉收缩引起的心脏功能障碍(30 mg/kg/12 h po) 在小鼠中以不依赖于 NOS 的方式。
 

法律信息

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.
 

属性

质量水平

100

测定

≥98% (HPLC)

形式

powder

mfr. no.

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°C

 

安全信息

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16