PF-05180999

产品编号 T16484Cas号 1394033-54-5

PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).

产品编号 T16484Cas号 1394033-54-5

PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).

大包装 & 定制

加入购物车

实验操作小课堂

联系我们获取更多批次信息

资源下载

TargetMol 的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

生物活性

产品描述	PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).
靶点活性	PDE7B:50.09 μM, PDE2A:1.6 nM, PDE11A4:26.969 μM, PDE10A1:2.03 μM
体外活性	PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2. PF-05180999 binds to the rat, dog and monkey PDE2A (Kis: 4.2, 8.4, and 5.5 nM and IC50s: 2.6, 5.2, and 3.4 nM, respectively). PF-05180999 displays weak activity against PDE, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively [1].
体内活性	PF-05180999 induces acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex, striatum, and hippocampus, but with no changes in cAMP and the associated downstream phospho-cAMP response element-binding protein (p-CREB) in mice. PF-05180999 (0.032-0.32 mg/kg mg/kg, s.c.) dramatically decreases the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats [1].

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 50 mg/mL (120.66 mM), Sonication is recommended.

溶液配制表

DMSO