產品屬性：
產品名稱 | PF-04449613 |
規格 | 1 mg、5 mg、10 mg、25 mg |
貨號 | EY-01Y16898 |
Cas No.: 1236858-52-8
別名: N/A
化學名: N/A
分子式: C21H25N5O3
分子量: 395.5
溶解度: DMSO: 10 mg/ml
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).1 It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.2 It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-9068(2012)
2.Lai, B., Li, M., Hu, A., et al.The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learningDev. Neurobiol.78(9)859-872(2018)
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